DGIdb - PDGFRA Gene Record

PDGFRA 5156 Druggable GenomeClinically ActionableDrug Resistance

Alternate Names:

5156
PLATELET DERIVED GROWTH FACTOR RECEPTOR ALPHA
PDGFRA
CD140A
PDGFR-2
PDGFR2
173490
8803
ENSG00000134853
OTTHUMG00000128699
RHEPDGFRA
Platelet-derived growth factor receptor alpha
Alpha platelet-derived growth factor receptor
Platelet-derived growth factor receptor 2
Platelet-derived growth factor alpha receptor
Alpha-type platelet-derived growth factor receptor
PDGF-R-alpha
PDGFR-alpha
CD140a antigen
CD140 antigen-like family member A
CD_antigen=CD140a
PGFRA_HUMAN
P16234
ALPHA PLATELET-DERIVED GROWTH FACTOR RECEPTOR PRECURSOR (EC 2.7.1.112) (PDGF-R-ALPHA) (CD140A ANTIGEN). [SOURCE:UNIPROT/SWISSPROT;ACC:P16234]
1803
NM_006206
NP_006197
BE0000852
PDGFR
GAS9
38
PA33147
T53524

Gene Info:

Human Readable Name	DRUGGABLE GENOME
GuideToPharmacology Gene Category Name	Type III RTKs: PDGFR, CSFR, Kit, FLT3 receptor family
GuideToPharmacology Gene Category ID	322
Target Subclass	PDGFR
Target Subclass	KInase
Target Main Class	Receptors
Transmembrane Helix Count	1
Target Class	Receptors
Target Subclass	EC:2.7.10.1
Interpro Name	Serine-threonine/tyrosine-protein kinase catalytic domain
Uniprot Evidence	1: Evidence at protein level
Uniprot Status	Swiss-Prot
Interpro Acc	IPR001245
Interpro Short Name	Ser-Thr/Tyr_kinase_cat_dom
Interpro Type	Domain
Human Readable Name	KINASE
Gene Biotype	PROTEIN_CODING

(26 More Sources)

Gene Categories: Category Details

KINASE
TYROSINE KINASE
DRUG RESISTANCE
EXTERNAL SIDE OF PLASMA MEMBRANE
DRUGGABLE GENOME
CLINICALLY ACTIONABLE

Publications:

MacConaill et al., 2014, Prospective enterprise-level molecular genotyping of a cohort of cancer patients., J Mol Diagn
Heinrich et al., 2003, Kinase mutations and imatinib response in patients with metastatic gastrointestinal stromal tumor., J. Clin. Oncol.
Heinrich et al., 2006, Molecular correlates of imatinib resistance in gastrointestinal stromal tumors., J. Clin. Oncol.
Heinrich et al., 2012, Crenolanib inhibits the drug-resistant PDGFRA D842V mutation associated with imatinib-resistant gastrointestinal stromal tumors., Clin. Cancer Res.
Dewaele et al., 2008, Activity of dasatinib, a dual SRC/ABL kinase inhibitor, and IPI-504, a heat shock protein 90 inhibitor, against gastrointestinal stromal tumor-associated PDGFRAD842V mutation., Clin. Cancer Res.
Corless et al., 2005, PDGFRA mutations in gastrointestinal stromal tumors: frequency, spectrum and in vitro sensitivity to imatinib., J. Clin. Oncol.
Yoo et al., 2016, Efficacy of Imatinib in Patients with Platelet-Derived Growth Factor Receptor Alpha-Mutated Gastrointestinal Stromal Tumors., Cancer Res Treat
Lasota et al., 2004, A great majority of GISTs with PDGFRA mutations represent gastric tumors of low or no malignant potential., Lab. Invest.
Debiec-Rychter et al., 2005, Mechanisms of resistance to imatinib mesylate in gastrointestinal stromal tumors and activity of the PKC412 inhibitor against imatinib-resistant mutants., Gastroenterology
Hirota et al., 2003, Gain-of-function mutations of platelet-derived growth factor receptor alpha gene in gastrointestinal stromal tumors., Gastroenterology
Cassier et al., 2012, Outcome of patients with platelet-derived growth factor receptor alpha-mutated gastrointestinal stromal tumors in the tyrosine kinase inhibitor era., Clin. Cancer Res.
Prenen et al., 2006, Efficacy of the kinase inhibitor SU11248 against gastrointestinal stromal tumor mutants refractory to imatinib mesylate., Clin. Cancer Res.
Dai et al., 2013, Large-scale analysis of PDGFRA mutations in melanomas and evaluation of their sensitivity to tyrosine kinase inhibitors imatinib and crenolanib., Clin. Cancer Res.
Yi et al., 2005, Epithelioid gastrointestinal stromal tumor with PDGFRA activating mutation and immunoreactivity., Appl. Immunohistochem. Mol. Morphol.
Borbényi, 2005, [Disorders with eosinophilia, treatment of hypereosinophilic syndrome]., Orv Hetil
Tefferi, 2005, Modern diagnosis and treatment of primary eosinophilia., Acta Haematol.
Chen et al., 2005, Imatinib resistance in gastrointestinal stromal tumors., Curr Oncol Rep
Trempat et al., 2003, Chronic myeloproliferative disorders with rearrangement of the platelet-derived growth factor alpha receptor: a new clinical target for STI571/Glivec., Oncogene
Chalmers et al., 2015, Comprehensive genomic profiling identifies a novel TNKS2-PDGFRA fusion that defines a myeloid neoplasm with eosinophilia that responded dramatically to imatinib therapy., Blood Cancer J
Metzgeroth G et al., 2012, Limited clinical activity of nilotinib and sorafenib in FIP1L1-PDGFRA positive chronic eosinophilic leukemia with imatinib-resistant T674I mutation., Leukemia
Srinivas et al., 2014, Complete response of monoblastic myeloid sarcoma with FIP1L1- PDGFRA rearrangement to imatinib monotherapy., Br. J. Haematol.
Cools et al., 2003, A tyrosine kinase created by fusion of the PDGFRA and FIP1L1 genes as a therapeutic target of imatinib in idiopathic hypereosinophilic syndrome., N. Engl. J. Med.
Klion et al., 2004, Molecular remission and reversal of myelofibrosis in response to imatinib mesylate treatment in patients with the myeloproliferative variant of hypereosinophilic syndrome., Blood
Zick et al., 2017, Treatment inferred from mutations identified using massive parallel sequencing leads to clinical benefit in some heavily pretreated cancer patients., Medicine (Baltimore)
Hammerman et al., 2011, Mutations in the DDR2 kinase gene identify a novel therapeutic target in squamous cell lung cancer., Cancer Discov
Holtkamp et al., 2006, Mutation and expression of PDGFRA and KIT in malignant peripheral nerve sheath tumors, and its implications for imatinib sensitivity., Carcinogenesis
Szerlip et al., 2012, Intratumoral heterogeneity of receptor tyrosine kinases EGFR and PDGFRA amplification in glioblastoma defines subpopulations with distinct growth factor response., Proc. Natl. Acad. Sci. U.S.A.
Elling et al., 2011, Novel imatinib-sensitive PDGFRA-activating point mutations in hypereosinophilic syndrome induce growth factor independence and leukemia-like disease., Blood
Ramos AH et al., 2009, Amplification of chromosomal segment 4q12 in non-small cell lung cancer., Cancer Biol Ther
Mazzocca A et al., 2019, New frontiers in the medical management of gastrointestinal stromal tumours., Ther Adv Med Oncol
Villanueva MT, 2019, Ripretinib turns off the switch in GIST., Nat Rev Drug Discov
Koschmann C et al., 2016, Characterizing and targeting PDGFRA alterations in pediatric high-grade glioma., Oncotarget
van der Graaf, 2016, Olaratumab in soft-tissue sarcomas., Lancet
Doi et al., 2014, Phase I study of olaratumab in Japanese patients with advanced solid tumors., Cancer Sci.
Gebreyohannes YK et al., 2019, Robust Activity of Avapritinib, Potent and Highly Selective Inhibitor of Mutated KIT, in Patient-derived Xenograft Models of Gastrointestinal Stromal Tumors., Clin Cancer Res
Sonpavde et al., 2007, Pazopanib: a novel multitargeted tyrosine kinase inhibitor., Curr Oncol Rep
Wind S et al., 2019, Clinical Pharmacokinetics and Pharmacodynamics of Nintedanib., Clin Pharmacokinet
Hilberg et al., 2008, BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy., Cancer Res.
Kollàr et al., 2014, Regorafenib treatment for advanced, refractory gastrointestinal stromal tumor: a report of the UK managed access program., Clin Sarcoma Res
Gozgit et al., 2011, Potent activity of ponatinib (AP24534) in models of FLT3-driven acute myeloid leukemia and other hematologic malignancies., Mol. Cancer Ther.
McDermott et al., 2009, Ligand-dependent platelet-derived growth factor receptor (PDGFR)-alpha activation sensitizes rare lung cancer and sarcoma cells to PDGFR kinase inhibitors., Cancer Res.
Heinrich et al., 2008, Primary and secondary kinase genotypes correlate with the biological and clinical activity of sunitinib in imatinib-resistant gastrointestinal stromal tumor., J. Clin. Oncol.
Sadovnik et al., 2014, Identification of Ponatinib as a potent inhibitor of growth, migration, and activation of neoplastic eosinophils carrying FIP1L1-PDGFRA., Exp. Hematol.
Huang et al., 2010, Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including the T315I gatekeeper mutant., J. Med. Chem.
O'Hare et al., 2009, AP24534, a pan-BCR-ABL inhibitor for chronic myeloid leukemia, potently inhibits the T315I mutant and overcomes mutation-based resistance., Cancer Cell
Ebert et al., 1995, Induction of platelet-derived growth factor A and B chains and over-expression of their receptors in human pancreatic cancer., Int. J. Cancer
Yu et al., 2003, Platelet-derived growth factor (PDGF) receptor-alpha-activated c-Jun NH2-terminal kinase-1 is critical for PDGF-induced p21WAF1/CIP1 promoter activity independent of p53., J. Biol. Chem.
Abdiu et al., 1998, Human malignant fibrous histiocytomas in vitro: growth characteristics and their association with expression of mRNA for platelet-derived growth factor, transforming growth factor-alpha and their receptors., Eur. J. Cancer
Miller-Kasprzak et al., 2002, [Structure and function of PDGF-R-alpha and its expression in normal kidney and kidney diseases]., Prz. Lek.
Heidaran et al., 1991, Deletion or substitution within the alpha platelet-derived growth factor receptor kinase insert domain: effects on functional coupling with intracellular signaling pathways., Mol. Cell. Biol.
Millward MJ et al., 2006, The multikinase inhibitor midostaurin (PKC412A) lacks activity in metastatic melanoma: a phase IIA clinical and biologic study., Br J Cancer
Basu et al., 2015, First-in-Human Pharmacokinetic and Pharmacodynamic Study of the Dual m-TORC 1/2 Inhibitor AZD2014., Clin. Cancer Res.
Matsui et al., 2008, E7080, a novel inhibitor that targets multiple kinases, has potent antitumor activities against stem cell factor producing human small cell lung cancer H146, based on angiogenesis inhibition., Int. J. Cancer
Rolf MG et al., 2015, In vitro pharmacological profiling of R406 identifies molecular targets underlying the clinical effects of fostamatinib., Pharmacol Res Perspect

OLARATUMAB PDGFRA

Interaction Score: 8.35

Interaction Types & Directionality:

antibody (inhibitory)

antagonist (inhibitory)

Interaction Info:

Trial Name IMC-3G3

Novel drug target Established target

Direct Interaction yes

PMIDs:
27291995 24816152

Sources:
DrugBank MyCancerGenome TdgClinicalTrial ChemblInteractions GuideToPharmacology PharmGKB TTD FDA
TOVETUMAB PDGFRA

Interaction Score: 2.51

Interaction Types & Directionality:

antibody (inhibitory)

Interaction Info:

Notes

PMIDs:
None found

Sources:
TALC MyCancerGenome TTD
BECAPLERMIN PDGFRA

Interaction Score: 2.51

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Platelet-derived growth factor receptor agonist

Direct Interaction yes

Trial Name becaplermin,Regranex

PMIDs:
7665222 14506245 10070317 12632922 1702511

Sources:
DrugBank TdgClinicalTrial ChemblInteractions TEND
CRENOLANIB PDGFRA

Interaction Score: 2.19

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Drug family FLT3 inhibitor

Alteration PDGFRA:D842V

Alteration PDGFRA:V658A,P577S,R841K,H845Y,G853D

PMIDs:
25157968 14645423 16954519 22745105 18794084 15928335 26130666 15146165 15685537 12949711 22718859 16638875 24132921

Sources:
MyCancerGenome JAX-CKB ChemblInteractions CGI DoCM CIViC GuideToPharmacology TTD
AVAPRITINIB PDGFRA

Interaction Score: 1.67

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Phase I

Response Type sensitive

PMIDs:
30274985

Sources:
JAX-CKB CIViC TTD
RIPRETINIB PDGFRA

Interaction Score: 0.7

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Indication/Tumor Type glioblastoma multiforme

Response Type sensitive

Approval Status Phase I

PMIDs:
31205499 31267077

Sources:
DrugBank JAX-CKB TTD
IMATINIB PDGFRA

Interaction Score: 0.5

Interaction Types & Directionality:

antagonist (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Clinical Status preclinical

Pathway activation

Variant Effect gain-of-function

PMIDs:
25157968 14645423 16954519 22745105 18794084 15928335 26130666 15146165 15685537 12949711 22718859 16638875 24132921 15894928 15921304 15995325 15946589 12944919 25658984 21818111 24456122 12660384 14504092 28514312 22328973 16357008 22323597 21224473 19755855

Sources:
DTC DrugBank MyCancerGenome TdgClinicalTrial JAX-CKB CGI TEND DoCM COSMIC CIViC FDA OncoKB
SUNITINIB PDGFRA

Interaction Score: 0.49

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Indication/Tumor Type Advanced Solid Tumor

Response Type resistant

Approval Status Preclinical - Cell culture

PMIDs:
19366796 18955458 16638875 22718859 25157968 14645423 16954519 22745105 18794084 15928335 26130666 15146165 15685537 12949711 21482694 19755855

Sources:
DrugBank TdgClinicalTrial JAX-CKB CGI TEND DoCM COSMIC CIViC MyCancerGenomeClinicalTrial
AMUVATINIB PDGFRA

Interaction Score: 0.48

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name MP-470

Mechanism of Interaction Platelet-derived growth factor receptor alpha inhibitor

PMIDs:
None found

Sources:
DrugBank MyCancerGenome TdgClinicalTrial ChemblInteractions
X-82 PDGFRA

Interaction Score: 0.33

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Platelet-derived growth factor receptor inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
MyCancerGenome ChemblInteractions
MOTESANIB PDGFRA

Interaction Score: 0.31

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Platelet-derived growth factor receptor inhibitor

Direct Interaction yes

Novel drug target Established target

PMIDs:
None found

Sources:
MyCancerGenome TdgClinicalTrial ChemblInteractions
NINTEDANIB PDGFRA

Interaction Score: 0.3

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes

Specific Action of the Ligand Inhibition

Endogenous Drug? False

PMIDs:
31016670 18559524

Sources:
TALC DrugBank MyCancerGenome TdgClinicalTrial ClearityFoundationClinicalTrial GuideToPharmacology
XL-820 PDGFRA

Interaction Score: 0.28

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Platelet-derived growth factor receptor inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions TTD
RAMUCIRUMAB PDGFRA

Interaction Score: 0.28

Interaction Types & Directionality:

antibody (inhibitory)

Interaction Info:

Notes

PMIDs:
None found

Sources:
TALC MyCancerGenome
MASITINIB PDGFRA

Interaction Score: 0.24

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name masitinib, AB1010

Mechanism of Interaction Platelet-derived growth factor receptor inhibitor

PMIDs:
None found

Sources:
TdgClinicalTrial ChemblInteractions GuideToPharmacology MyCancerGenomeClinicalTrial
FAMITINIB PDGFRA

Interaction Score: 0.24

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Platelet-derived growth factor receptor inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions TTD
PONATINIB PDGFRA

Interaction Score: 0.22

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Indication/Tumor Type lung small cell carcinoma

Response Type sensitive

Approval Status Preclinical

PMIDs:
24407160 20513156 19878872 22328973

Sources:
DTC DrugBank JAX-CKB CIViC
VISTUSERTIB PDGFRA

Interaction Score: 0.21

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type pancreatic cancer

Response Type predicted – sensitive

Approval Status Phase I

PMIDs:
25805799

Sources:
JAX-CKB
DASATINIB PDGFRA

Interaction Score: 0.21

Interaction Types & Directionality:

n/a

Interaction Info:

Variant Effect gain-of-function

Pathway activation

Clinical Status preclinical

PMIDs:
25157968 14645423 16954519 22745105 18794084 15928335 26130666 15146165 15685537 12949711 22718859 16638875 22328973 27582545

Sources:
DTC JAX-CKB CGI DoCM CIViC OncoKB
VATALANIB PDGFRA

Interaction Score: 0.19

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Platelet-derived growth factor receptor inhibitor

Direct Interaction yes

Trial Name vatalanib, PTK 787

PMIDs:
None found

Sources:
DTC TdgClinicalTrial ChemblInteractions
NILOTINIB PDGFRA

Interaction Score: 0.19

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Indication/Tumor Type Advanced Solid Tumor

Response Type resistant

Approval Status Preclinical - Cell culture

PMIDs:
18794084

Sources:
JAX-CKB MyCancerGenomeClinicalTrial
QUIZARTINIB PDGFRA

Interaction Score: 0.19

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
ChemblInteractions GuideToPharmacology
LENVATINIB PDGFRA

Interaction Score: 0.18

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name E7080

Novel drug target Established target

PMIDs:
17943726

Sources:
DrugBank TdgClinicalTrial
REGORAFENIB PDGFRA

Interaction Score: 0.18

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Platelet-derived growth factor receptor inhibitor

Drug family Pan-kinase inhibitor

PMIDs:
25905001

Sources:
DrugBank JAX-CKB ChemblInteractions CGI MyCancerGenomeClinicalTrial
TAK-593 PDGFRA

Interaction Score: 0.17

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Platelet-derived growth factor receptor inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
TANDUTINIB PDGFRA

Interaction Score: 0.15

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
DTC MyCancerGenome
TELATINIB PDGFRA

Interaction Score: 0.14

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name telatinib

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial
PEGPLERANIB SODIUM PDGFRA

Interaction Score: 0.14

Interaction Types & Directionality:

n/a

Interaction Info:

Novel drug target Established target

Trial Name E-10030

PMIDs:
None found

Sources:
TdgClinicalTrial
MIDOSTAURIN PDGFRA

Interaction Score: 0.13

Interaction Types & Directionality:

inhibitor (inhibitory)

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Platelet-derived growth factor receptor inhibitor

Direct Interaction yes

PMIDs:
16969355

Sources:
DrugBank MyCancerGenome ChemblInteractions
PAZOPANIB PDGFRA

Interaction Score: 0.11

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes

PMIDs:
17288876

Sources:
TALC DTC DrugBank MyCancerGenome MyCancerGenomeClinicalTrial
ROMIPLOSTIM PDGFRA

Interaction Score: 0.1

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
SU-014813 PDGFRA

Interaction Score: 0.1

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Platelet-derived growth factor receptor inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
NINTEDANIB ESYLATE PDGFRA

Interaction Score: 0.09

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Platelet-derived growth factor receptor inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
BARASERTIB PDGFRA

Interaction Score: 0.09

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
SUNITINIB MALATE PDGFRA

Interaction Score: 0.09

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Platelet-derived growth factor receptor inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
ORANTINIB PDGFRA

Interaction Score: 0.08

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Platelet-derived growth factor receptor inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
PAZOPANIB HYDROCHLORIDE PDGFRA

Interaction Score: 0.08

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Platelet-derived growth factor receptor inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
XL-999 PDGFRA

Interaction Score: 0.08

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Platelet-derived growth factor receptor inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
LUCITANIB PDGFRA

Interaction Score: 0.07

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology
ENMD-2076 PDGFRA

Interaction Score: 0.07

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? True

PMIDs:
None found

Sources:
TdgClinicalTrial GuideToPharmacology
ERDAFITINIB PDGFRA

Interaction Score: 0.06

Interaction Types & Directionality:

substrate

Interaction Info:

PMIDs:
None found

Sources:
DrugBank
SITRAVATINIB PDGFRA

Interaction Score: 0.06

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Inhibition

PMIDs:
None found

Sources:
GuideToPharmacology
AXITINIB PDGFRA

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name axitinib, AG-013736

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial
FORETINIB PDGFRA

Interaction Score: 0.06

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Platelet-derived growth factor receptor inhibitor

PMIDs:
None found

Sources:
ChemblInteractions
CEDIRANIB PDGFRA

Interaction Score: 0.05

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Platelet-derived growth factor receptor inhibitor

Specific Action of the Ligand Inhibition

PMIDs:
None found

Sources:
DTC ChemblInteractions GuideToPharmacology
CHEMBL202721 PDGFRA

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
RABEPRAZOLE SODIUM PDGFRA

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
SORAFENIB PDGFRA

Interaction Score: 0.04

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
21482694

Sources:
DTC CIViC MyCancerGenomeClinicalTrial
AZD-1152-HQPA PDGFRA

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DOVITINIB PDGFRA

Interaction Score: 0.04

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Platelet-derived growth factor receptor inhibitor

Direct Interaction yes

Specific Action of the Ligand Inhibition

PMIDs:
None found

Sources:
DTC ClearityFoundationClinicalTrial ChemblInteractions GuideToPharmacology
ENMD-981693 PDGFRA

Interaction Score: 0.03

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Platelet-derived growth factor receptor inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
CHEMBL406845 PDGFRA

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
GEFITINIB PDGFRA

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Gefitinib + Imatinib

Indication/Tumor Type glioblastoma multiforme

Response Type sensitive

PMIDs:
22323597

Sources:
JAX-CKB
AST-487 PDGFRA

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
LINIFANIB PDGFRA

Interaction Score: 0.02

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Platelet-derived growth factor receptor inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
DTC ChemblInteractions
ILORASERTIB PDGFRA

Interaction Score: 0.02

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Details of the Assay for Interaction Measuring inhibition of kinase activity in a biochemical assay.

Specific Action of the Ligand Inhibition

Endogenous Drug? False

PMIDs:
None found

Sources:
DTC ChemblInteractions GuideToPharmacology
CARBOPLATIN PDGFRA

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Clinical Study

Response Type sensitive

PMIDs:
28514312

Sources:
JAX-CKB
CHEMBL1997335 PDGFRA

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
OSI-632 PDGFRA

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
PACLITAXEL PDGFRA

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Imatinib + Carboplatin + Paclitaxel

Indication/Tumor Type melanoma

Response Type sensitive

PMIDs:
28514312

Sources:
JAX-CKB
PD-0166285 PDGFRA

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
VANDETANIB PDGFRA

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
R-406 PDGFRA

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
RG-1530 PDGFRA

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
CYC-116 PDGFRA

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
TAE-684 PDGFRA

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
CENISERTIB PDGFRA

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
FOSTAMATINIB PDGFRA

Interaction Score: 0.01

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
26516587

Sources:
DrugBank

Ensembl: ENSG00000134853
- Version: 101_38
Alternate Names:

PDGFRA Ensembl Gene Name

Gene Info:

Gene Biotype PROTEIN_CODING

Publications:
HopkinsGroom: P16234
- Version: 11-September-2012
Alternate Names:

P16234 Uniprot Accession

5156 Entrez Gene Id

PDGFRA Uniprot Gene Name

Gene Info:

Interpro Name Serine-threonine/tyrosine-protein kinase catalytic domain

Uniprot Evidence 1: Evidence at protein level

Uniprot Status Swiss-Prot

Gene Categories:

KINASE, DRUGGABLE GENOME

Publications:
TEND: P16234
- Version: 01-August-2011
Alternate Names:

PDGFRA Gene Symbol

ENSG00000134853 Ensembl Gene Id

PGFRA_HUMAN Uniprot Id

Gene Info:

Target Subclass PDGFR

Target Subclass KInase

Target Main Class Receptors

Publications:

RussLampel: ENSG00000134853

Version: 26-July-2011

Alternate Names:

ENSG00000134853 Ensembl Gene Id

PDGFRA Display Id

ALPHA PLATELET-DERIVED GROWTH FACTOR RECEPTOR PRECURSOR (EC 2.7.1.112) (PDGF-R-ALPHA) (CD140A ANTIGEN). [SOURCE:UNIPROT/SWISSPROT;ACC:P16234] Description

Gene Info:

Human Readable Name DRUGGABLE GENOME

Gene Categories:

DRUGGABLE GENOME

Publications:

TdgClinicalTrial: P16234
- Version: January-2014
Alternate Names:

PDGFRA Gene Symbol

Gene Info:

Target Class Receptors

Target Subclass EC:2.7.10.1

Publications:
GuideToPharmacology: 5156
- Version: 29-September-2020
Alternate Names:

8803 HUGO Gene ID

8803 HUGO Gene Symbol

platelet derived growth factor receptor alpha HUGO Gene Name

Gene Info:

GuideToPharmacology Gene Category Name Type III RTKs: PDGFR, CSFR, Kit, FLT3 receptor family

GuideToPharmacology Gene Category ID 322

Publications:

JAX-CKB: PDGFRA

Version: 27-September-2017

Alternate Names:

5156 CKB Entrez Id

PDGFRA CKB Gene Synonym

CD140A CKB Gene Synonym

Gene Info:

Publications:

Hammerman et al., 2011, Mutations in the DDR2 kinase gene identify a novel therapeutic target in squamous cell lung cancer., Cancer Discov

Dai et al., 2013, Large-scale analysis of PDGFRA mutations in melanomas and evaluation of their sensitivity to tyrosine kinase inhibitors imatinib and crenolanib., Clin. Cancer Res.

Elling et al., 2011, Novel imatinib-sensitive PDGFRA-activating point mutations in hypereosinophilic syndrome induce growth factor independence and leukemia-like disease., Blood

CIViC: PDGFRA

Version: 14-September-2020

Alternate Names:

5156 Entrez Gene ID

38 CIViC Gene ID

Gene Info:

Gene Categories:

CLINICALLY ACTIONABLE, DRUG RESISTANCE

Publications:

Corless et al., 2005, PDGFRA mutations in gastrointestinal stromal tumors: frequency, spectrum and in vitro sensitivity to imatinib., J. Clin. Oncol.

Heinrich et al., 2006, Molecular correlates of imatinib resistance in gastrointestinal stromal tumors., J. Clin. Oncol.

Hirota et al., 2003, Gain-of-function mutations of platelet-derived growth factor receptor alpha gene in gastrointestinal stromal tumors., Gastroenterology

DrugBank: BE0000852

Version: 5.1.7

Alternate Names:

PDGFRA DrugBank Gene Name

P16234 UniProt Accession

5156 Entrez Gene Id

Gene Info:

Publications:

Heidaran et al., 1991, Deletion or substitution within the alpha platelet-derived growth factor receptor kinase insert domain: effects on functional coupling with intracellular signaling pathways., Mol. Cell. Biol.

Miller-Kasprzak et al., 2002, [Structure and function of PDGF-R-alpha and its expression in normal kidney and kidney diseases]., Prz. Lek.

Abdiu et al., 1998, Human malignant fibrous histiocytomas in vitro: growth characteristics and their association with expression of mRNA for platelet-derived growth factor, transforming growth factor-alpha and their receptors., Eur. J. Cancer

CGI: PDGFRA

Version: 27-September-2017

Alternate Names:

Gene Info:

Publications:

Cassier et al., 2012, Outcome of patients with platelet-derived growth factor receptor alpha-mutated gastrointestinal stromal tumors in the tyrosine kinase inhibitor era., Clin. Cancer Res.

Prenen et al., 2006, Efficacy of the kinase inhibitor SU11248 against gastrointestinal stromal tumor mutants refractory to imatinib mesylate., Clin. Cancer Res.

DoCM: PDGFRA

Version: 27-September-2017

Alternate Names:

Gene Info:

Publications:

Dai et al., 2013, Large-scale analysis of PDGFRA mutations in melanomas and evaluation of their sensitivity to tyrosine kinase inhibitors imatinib and crenolanib., Clin. Cancer Res.

Prenen et al., 2006, Efficacy of the kinase inhibitor SU11248 against gastrointestinal stromal tumor mutants refractory to imatinib mesylate., Clin. Cancer Res.

Cassier et al., 2012, Outcome of patients with platelet-derived growth factor receptor alpha-mutated gastrointestinal stromal tumors in the tyrosine kinase inhibitor era., Clin. Cancer Res.

DTC: PDGFRA

Version: 02-September-2020

Alternate Names:

Gene Info:

Publications:

Huang et al., 2010, Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including the T315I gatekeeper mutant., J. Med. Chem.

HingoraniCasas: ENSG00000134853
- Version: 31-May-2017
Alternate Names:

ENSG00000134853 Gene Symbol

PDGFRA Ensembl Id

Gene Info:

Gene Categories:

DRUGGABLE GENOME

Publications:
MyCancerGenome: PDGFRA
- Version: 20-Jun-2017
Alternate Names:

5156 Entrez Gene Id

PDGFRA MyCancerGenome Gene Symbol

PDGFR-alpha MyCancerGenome Reported Gene Name

Gene Info:

Publications:
TALC: PDGFRA
- Version: 12-May-2016
Alternate Names:

PDGFRA Gene Symbol

Gene Info:

Publications:
ChemblInteractions: PDGFR2
- Version: chembl_23
Alternate Names:

PDGF-R-alpha UNIPROT

RHEPDGFRA GENE_SYMBOL

PDGFRA GENE_SYMBOL

Gene Info:

Publications:
OncoKB: PDGFRA
- Version: 23-July-2020
Alternate Names:

5156 OncoKB Entrez Id

PDGFR2 OncoKB Gene Synonym

RHEPDGFRA OncoKB Gene Synonym

Gene Info:

Publications:
PharmGKB: PDGFRA
- Version: 18-August-2020
Alternate Names:

PA33147 PharmGKB ID

Gene Info:

Publications:
Pharos: PDGFRA
- Version: 03-September-2020
Alternate Names:

Platelet-derived growth factor receptor alpha Gene Name

P16234 UniProt ID

Gene Info:

Gene Categories:

KINASE

Publications:
GO: PDGFRA
- Version: 05-September-2020
Alternate Names:

PDGFR2 GO Gene Synonym

RHEPDGFRA GO Gene Synonym

Gene Info:

Gene Categories:

EXTERNAL SIDE OF PLASMA MEMBRANE

Publications:
Tempus: PDGFRA
- Version: 11-November-2018
Alternate Names:

PDGFRA Gene Symbol

Gene Info:

Gene Categories:

CLINICALLY ACTIONABLE

Publications:
dGene: PDGFRA
- Version: 27-Jun-2013
Alternate Names:

5156 Gene ID

CD140A dGene Synonym

PDGFR-2 dGene Synonym

Gene Info:

Gene Categories:

KINASE, TYROSINE KINASE

Publications:
TTD: Platelet-derived growth factor receptor alpha
- Version: 2020.06.01
Alternate Names:

PDGFRA TTD Gene Abbreviation

T53524 TTD Target ID

Gene Info:

Publications:
ClearityFoundationClinicalTrial: PDGFRA
- Version: 15-June-2013
Alternate Names:

Gene Info:

Publications:
MyCancerGenomeClinicalTrial: PDGFRA
- Version: 30-February-2014
Alternate Names:

Gene Info:

Publications:
FoundationOneGenes: PDGFRA
- Version: 03-September-2020
Alternate Names:

Gene Info:

Gene Categories:

CLINICALLY ACTIONABLE

Publications:
CarisMolecularIntelligence: PDGFRA
- Version: 04-September-2020
Alternate Names:

Gene Info:

Gene Categories:

CLINICALLY ACTIONABLE

Publications:
FDA: PDGFRA
- Version: 04-September-2020
Alternate Names:

Gene Info:

Publications:
Oncomine: PDGFRA
- Version: v3
Alternate Names:

Gene Info:

Gene Categories:

CLINICALLY ACTIONABLE

Publications:
COSMIC: PDGFRA
- Version: 4-Sep-2020
Alternate Names:

Gene Info:

Gene Categories:

DRUG RESISTANCE

Publications:

Trial Name	IMC-3G3
Novel drug target	Established target
Direct Interaction	yes

Mechanism of Interaction	Platelet-derived growth factor receptor agonist
Direct Interaction	yes
Trial Name	becaplermin,Regranex

Drug family	FLT3 inhibitor
Alteration	PDGFRA:D842V
Alteration	PDGFRA:V658A,P577S,R841K,H845Y,G853D

Evidence Type	Actionable
Approval Status	Phase I
Response Type	sensitive

Indication/Tumor Type	glioblastoma multiforme
Response Type	sensitive
Approval Status	Phase I

Clinical Status	preclinical
Pathway	activation
Variant Effect	gain-of-function

Indication/Tumor Type	Advanced Solid Tumor
Response Type	resistant
Approval Status	Preclinical - Cell culture

Notes
Specific Action of the Ligand	Inhibition
Endogenous Drug?	False

Indication/Tumor Type	lung small cell carcinoma
Response Type	sensitive
Approval Status	Preclinical

Indication/Tumor Type	pancreatic cancer
Response Type	predicted – sensitive
Approval Status	Phase I

antibody (inhibitory)
antagonist (inhibitory)

antagonist (inhibitory)
inhibitor (inhibitory)

Direct Interaction?	False
Endogenous Drug?	False
Specific Action of the Ligand	Inhibition

Trial Name	axitinib, AG-013736
Novel drug target	Established target

combination therapy	Gefitinib + Imatinib
Indication/Tumor Type	glioblastoma multiforme
Response Type	sensitive

Details of the Assay for Interaction	Measuring inhibition of kinase activity in a biochemical assay.
Specific Action of the Ligand	Inhibition
Endogenous Drug?	False

combination therapy	Imatinib + Carboplatin + Paclitaxel
Indication/Tumor Type	melanoma
Response Type	sensitive

P16234	Uniprot Accession
5156	Entrez Gene Id
PDGFRA	Uniprot Gene Name

PDGFRA	Gene Symbol
ENSG00000134853	Ensembl Gene Id
PGFRA_HUMAN	Uniprot Id

8803	HUGO Gene ID
8803	HUGO Gene Symbol
platelet derived growth factor receptor alpha	HUGO Gene Name

5156	CKB Entrez Id
PDGFRA	CKB Gene Synonym
CD140A	CKB Gene Synonym

PDGFRA	DrugBank Gene Name
P16234	UniProt Accession
5156	Entrez Gene Id

PDGFRA Gene Record

PDGFRA 5156 Druggable GenomeClinically ActionableDrug Resistance

Alternate Names:

Gene Info:

Gene Categories: Category Details

Publications:

Interaction Types & Directionality: antibody (inhibitory) antagonist (inhibitory)

Interaction Info: Trial Name IMC-3G3 Novel drug target Established target Direct Interaction yes

PMIDs: 27291995 24816152

Sources: DrugBank MyCancerGenome TdgClinicalTrial ChemblInteractions GuideToPharmacology PharmGKB TTD FDA

Interaction Types & Directionality: antibody (inhibitory)

Interaction Info: Notes

PMIDs: None found

Sources: TALC MyCancerGenome TTD

Interaction Types & Directionality: agonist (activating)

Interaction Info: Mechanism of Interaction Platelet-derived growth factor receptor agonist Direct Interaction yes Trial Name becaplermin,Regranex

PMIDs: 7665222 14506245 10070317 12632922 1702511

Sources: DrugBank TdgClinicalTrial ChemblInteractions TEND

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Drug family FLT3 inhibitor Alteration PDGFRA:D842V Alteration PDGFRA:V658A,P577S,R841K,H845Y,G853D

PMIDs: 25157968 14645423 16954519 22745105 18794084 15928335 26130666 15146165 15685537 12949711 22718859 16638875 24132921

Sources: MyCancerGenome JAX-CKB ChemblInteractions CGI DoCM CIViC GuideToPharmacology TTD

Interaction Types & Directionality: n/a

Interaction Info: Evidence Type Actionable Approval Status Phase I Response Type sensitive

PMIDs: 30274985

Sources: JAX-CKB CIViC TTD

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Indication/Tumor Type glioblastoma multiforme Response Type sensitive Approval Status Phase I

PMIDs: 31205499 31267077

Sources: DrugBank JAX-CKB TTD

Interaction Types & Directionality: antagonist (inhibitory) inhibitor (inhibitory)

Interaction Info: Clinical Status preclinical Pathway activation Variant Effect gain-of-function

PMIDs: 25157968 14645423 16954519 22745105 18794084 15928335 26130666 15146165 15685537 12949711 22718859 16638875 24132921 15894928 15921304 15995325 15946589 12944919 25658984 21818111 24456122 12660384 14504092 28514312 22328973 16357008 22323597 21224473 19755855

Sources: DTC DrugBank MyCancerGenome TdgClinicalTrial JAX-CKB CGI TEND DoCM COSMIC CIViC FDA OncoKB

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Indication/Tumor Type Advanced Solid Tumor Response Type resistant Approval Status Preclinical - Cell culture

PMIDs: 19366796 18955458 16638875 22718859 25157968 14645423 16954519 22745105 18794084 15928335 26130666 15146165 15685537 12949711 21482694 19755855

Sources: DrugBank TdgClinicalTrial JAX-CKB CGI TEND DoCM COSMIC CIViC MyCancerGenomeClinicalTrial

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Novel drug target Established target Trial Name MP-470 Mechanism of Interaction Platelet-derived growth factor receptor alpha inhibitor

PMIDs: None found

Sources: DrugBank MyCancerGenome TdgClinicalTrial ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Platelet-derived growth factor receptor inhibitor Direct Interaction yes

PMIDs: None found

Sources: MyCancerGenome ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Platelet-derived growth factor receptor inhibitor Direct Interaction yes Novel drug target Established target

PMIDs: None found

Sources: MyCancerGenome TdgClinicalTrial ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Notes Specific Action of the Ligand Inhibition Endogenous Drug? False

PMIDs: 31016670 18559524

Sources: TALC DrugBank MyCancerGenome TdgClinicalTrial ClearityFoundationClinicalTrial GuideToPharmacology

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Platelet-derived growth factor receptor inhibitor Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions TTD

Interaction Types & Directionality: antibody (inhibitory)

Interaction Info: Notes

PMIDs: None found

Sources: TALC MyCancerGenome

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Novel drug target Established target Trial Name masitinib, AB1010 Mechanism of Interaction Platelet-derived growth factor receptor inhibitor

PMIDs: None found

Sources: TdgClinicalTrial ChemblInteractions GuideToPharmacology MyCancerGenomeClinicalTrial

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Platelet-derived growth factor receptor inhibitor Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions TTD

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Indication/Tumor Type lung small cell carcinoma Response Type sensitive Approval Status Preclinical

PMIDs: 24407160 20513156 19878872 22328973

Sources: DTC DrugBank JAX-CKB CIViC

Interaction Types & Directionality: n/a

Interaction Info: Indication/Tumor Type pancreatic cancer Response Type predicted – sensitive Approval Status Phase I

PMIDs: 25805799

Sources: JAX-CKB

Interaction Types & Directionality: n/a

Interaction Info: Variant Effect gain-of-function Pathway activation Clinical Status preclinical

Interaction Types & Directionality:

antibody (inhibitory)

antagonist (inhibitory)

Interaction Info:

Trial Name IMC-3G3

Novel drug target Established target

Direct Interaction yes

PMIDs:
27291995 24816152

Sources:
DrugBank MyCancerGenome TdgClinicalTrial ChemblInteractions GuideToPharmacology PharmGKB TTD FDA

Interaction Types & Directionality:

antibody (inhibitory)

Interaction Info:

Notes

PMIDs:
None found

Sources:
TALC MyCancerGenome TTD

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Platelet-derived growth factor receptor agonist

Direct Interaction yes

Trial Name becaplermin,Regranex

PMIDs:
7665222 14506245 10070317 12632922 1702511

Sources:
DrugBank TdgClinicalTrial ChemblInteractions TEND

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Drug family FLT3 inhibitor

Alteration PDGFRA:D842V

Alteration PDGFRA:V658A,P577S,R841K,H845Y,G853D

PMIDs:
25157968 14645423 16954519 22745105 18794084 15928335 26130666 15146165 15685537 12949711 22718859 16638875 24132921

Sources:
MyCancerGenome JAX-CKB ChemblInteractions CGI DoCM CIViC GuideToPharmacology TTD

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Phase I

Response Type sensitive

PMIDs:
30274985

Sources:
JAX-CKB CIViC TTD

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Indication/Tumor Type glioblastoma multiforme

Response Type sensitive

Approval Status Phase I

PMIDs:
31205499 31267077

Sources:
DrugBank JAX-CKB TTD

Interaction Types & Directionality:

antagonist (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Clinical Status preclinical

Pathway activation

Variant Effect gain-of-function

PMIDs:
25157968 14645423 16954519 22745105 18794084 15928335 26130666 15146165 15685537 12949711 22718859 16638875 24132921 15894928 15921304 15995325 15946589 12944919 25658984 21818111 24456122 12660384 14504092 28514312 22328973 16357008 22323597 21224473 19755855

Sources:
DTC DrugBank MyCancerGenome TdgClinicalTrial JAX-CKB CGI TEND DoCM COSMIC CIViC FDA OncoKB

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Indication/Tumor Type Advanced Solid Tumor

Response Type resistant

Approval Status Preclinical - Cell culture

PMIDs:
19366796 18955458 16638875 22718859 25157968 14645423 16954519 22745105 18794084 15928335 26130666 15146165 15685537 12949711 21482694 19755855

Sources:
DrugBank TdgClinicalTrial JAX-CKB CGI TEND DoCM COSMIC CIViC MyCancerGenomeClinicalTrial

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name MP-470

Mechanism of Interaction Platelet-derived growth factor receptor alpha inhibitor

PMIDs:
None found

Sources:
DrugBank MyCancerGenome TdgClinicalTrial ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Platelet-derived growth factor receptor inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
MyCancerGenome ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Platelet-derived growth factor receptor inhibitor

Direct Interaction yes

Novel drug target Established target

PMIDs:
None found

Sources:
MyCancerGenome TdgClinicalTrial ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes

Specific Action of the Ligand Inhibition

Endogenous Drug? False

PMIDs:
31016670 18559524

Sources:
TALC DrugBank MyCancerGenome TdgClinicalTrial ClearityFoundationClinicalTrial GuideToPharmacology

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Platelet-derived growth factor receptor inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions TTD

Interaction Types & Directionality:

antibody (inhibitory)

Interaction Info:

Notes

PMIDs:
None found

Sources:
TALC MyCancerGenome

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name masitinib, AB1010

Mechanism of Interaction Platelet-derived growth factor receptor inhibitor

PMIDs:
None found

Sources:
TdgClinicalTrial ChemblInteractions GuideToPharmacology MyCancerGenomeClinicalTrial

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Platelet-derived growth factor receptor inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions TTD

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Indication/Tumor Type lung small cell carcinoma

Response Type sensitive

Approval Status Preclinical

PMIDs:
24407160 20513156 19878872 22328973

Sources:
DTC DrugBank JAX-CKB CIViC

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type pancreatic cancer

Response Type predicted – sensitive

Approval Status Phase I

PMIDs:
25805799

Sources:
JAX-CKB

Interaction Types & Directionality:

n/a

Interaction Info:

Variant Effect gain-of-function

Pathway activation

Clinical Status preclinical

PMIDs:
25157968 14645423 16954519 22745105 18794084 15928335 26130666 15146165 15685537 12949711 22718859 16638875 22328973 27582545

Sources:
DTC JAX-CKB CGI DoCM CIViC OncoKB

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Platelet-derived growth factor receptor inhibitor

Direct Interaction yes

Trial Name vatalanib, PTK 787

PMIDs:
None found

Sources:
DTC TdgClinicalTrial ChemblInteractions

5156	OncoKB Entrez Id
PDGFR2	OncoKB Gene Synonym
RHEPDGFRA	OncoKB Gene Synonym

Platelet-derived growth factor receptor alpha	Gene Name
P16234	UniProt ID