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PDGFRA Gene Record

  • Summary
  • Interactions
  • Claims
  • 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:

    Ramos AH et al., 2009, Amplification of chromosomal segment 4q12 in non-small cell lung cancer., Cancer Biol Ther
    Hammerman et al., 2011, Mutations in the DDR2 kinase gene identify a novel therapeutic target in squamous cell lung cancer., Cancer Discov
    Corless et al., 2005, PDGFRA mutations in gastrointestinal stromal tumors: frequency, spectrum and in vitro sensitivity to imatinib., J. Clin. Oncol.
    Borbényi, 2005, [Disorders with eosinophilia, treatment of hypereosinophilic syndrome]., Orv Hetil
    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
    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
    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
    Elling et al., 2011, Novel imatinib-sensitive PDGFRA-activating point mutations in hypereosinophilic syndrome induce growth factor independence and leukemia-like disease., Blood
    Yi et al., 2005, Epithelioid gastrointestinal stromal tumor with PDGFRA activating mutation and immunoreactivity., Appl. Immunohistochem. Mol. Morphol.
    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.
    Lasota et al., 2004, A great majority of GISTs with PDGFRA mutations represent gastric tumors of low or no malignant potential., Lab. Invest.
    Chen et al., 2005, Imatinib resistance in gastrointestinal stromal tumors., Curr Oncol Rep
    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)
    Holtkamp et al., 2006, Mutation and expression of PDGFRA and KIT in malignant peripheral nerve sheath tumors, and its implications for imatinib sensitivity., Carcinogenesis
    Hirota et al., 2003, Gain-of-function mutations of platelet-derived growth factor receptor alpha gene in gastrointestinal stromal tumors., Gastroenterology
    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.
    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
    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
    Yoo et al., 2016, Efficacy of Imatinib in Patients with Platelet-Derived Growth Factor Receptor Alpha-Mutated Gastrointestinal Stromal Tumors., Cancer Res Treat
    MacConaill et al., 2014, Prospective enterprise-level molecular genotyping of a cohort of cancer patients., J Mol Diagn
    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.
    Heinrich et al., 2003, Kinase mutations and imatinib response in patients with metastatic gastrointestinal stromal tumor., J. Clin. Oncol.
    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.
    Heinrich et al., 2006, Molecular correlates of imatinib resistance in gastrointestinal stromal tumors., J. Clin. Oncol.
    Srinivas et al., 2014, Complete response of monoblastic myeloid sarcoma with FIP1L1- PDGFRA rearrangement to imatinib monotherapy., Br. J. Haematol.
    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.
    Heinrich et al., 2012, Crenolanib inhibits the drug-resistant PDGFRA D842V mutation associated with imatinib-resistant gastrointestinal stromal tumors., Clin. Cancer Res.
    Tefferi, 2005, Modern diagnosis and treatment of primary eosinophilia., Acta Haematol.
    Villanueva MT, 2019, Ripretinib turns off the switch in GIST., Nat Rev Drug Discov
    Mazzocca A et al., 2019, New frontiers in the medical management of gastrointestinal stromal tumours., Ther Adv Med Oncol
    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
    Hilberg et al., 2008, BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy., Cancer Res.
    Wind S et al., 2019, Clinical Pharmacokinetics and Pharmacodynamics of Nintedanib., Clin Pharmacokinet
    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.
    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
    Sadovnik et al., 2014, Identification of Ponatinib as a potent inhibitor of growth, migration, and activation of neoplastic eosinophils carrying FIP1L1-PDGFRA., Exp. Hematol.
    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
    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.
    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
    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.
    Miller-Kasprzak et al., 2002, [Structure and function of PDGF-R-alpha and its expression in normal kidney and kidney diseases]., Prz. Lek.
    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:
    FDA PharmGKB TdgClinicalTrial TTD DrugBank MyCancerGenome GuideToPharmacology ChemblInteractions

  • TOVETUMAB   PDGFRA

    Interaction Score: 2.51

    Interaction Types & Directionality:
    antibody (inhibitory)

    Interaction Info:
    Notes

    PMIDs:
    None found


    Sources:
    TTD TALC MyCancerGenome

  • 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 1702511 10070317 14506245 12632922


    Sources:
    TEND TdgClinicalTrial DrugBank ChemblInteractions

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


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

  • 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:
    31267077 31205499


    Sources:
    JAX-CKB TTD DrugBank

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


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

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


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

  • 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:
    TdgClinicalTrial DrugBank MyCancerGenome 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:
    TdgClinicalTrial MyCancerGenome 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:
    18559524 31016670


    Sources:
    ClearityFoundationClinicalTrial TdgClinicalTrial DrugBank TALC MyCancerGenome 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:
    TTD ChemblInteractions

  • 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:
    MyCancerGenomeClinicalTrial TdgClinicalTrial GuideToPharmacology ChemblInteractions

  • 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:
    TTD ChemblInteractions

  • 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:
    22328973 20513156 19878872 24407160


    Sources:
    DTC JAX-CKB CIViC DrugBank

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


    Sources:
    DTC OncoKB DoCM JAX-CKB CIViC CGI

  • 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:
    MyCancerGenomeClinicalTrial JAX-CKB

  • 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:
    GuideToPharmacology ChemblInteractions

  • LENVATINIB   PDGFRA

    Interaction Score: 0.18

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Trial Name E7080
    Novel drug target Established target

    PMIDs:
    17943726


    Sources:
    TdgClinicalTrial DrugBank

  • 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:
    MyCancerGenomeClinicalTrial JAX-CKB DrugBank ChemblInteractions CGI

  • 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:
    antagonist (inhibitory)
    inhibitor (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:
    MyCancerGenomeClinicalTrial DTC DrugBank TALC MyCancerGenome

  • 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 GuideToPharmacology ChemblInteractions

  • 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:
    MyCancerGenomeClinicalTrial DTC CIViC

  • 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:
    ClearityFoundationClinicalTrial DTC GuideToPharmacology ChemblInteractions

  • 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 GuideToPharmacology ChemblInteractions

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

    Publications:
    Ramos AH et al., 2009, Amplification of chromosomal segment 4q12 in non-small cell lung cancer., Cancer Biol Ther
    Corless et al., 2005, PDGFRA mutations in gastrointestinal stromal tumors: frequency, spectrum and in vitro sensitivity to imatinib., J. Clin. Oncol.
    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

  • DrugBank: BE0000852

    • Version: 5.1.7

    Alternate Names:
    PDGFRA DrugBank Gene Name
    P16234 UniProt Accession
    5156 Entrez Gene Id

    Gene Info:

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

Disclaimer: This resource is intended for purely research purposes. It should not be used for emergencies or medical or professional advice.

A finding of a drug-gene interaction or potentially druggable category does not necessarily indicate effectiveness (or lack thereof) of any drug or treatment regimen. A finding of no interaction or no potentially druggable category does not necessarily indicate lack of effectiveness of any drug or treatment regimen. Drug-gene interactions or potentially druggable categories are not presented in ranked order of potential or predicted efficacy.

The dgidb.org website does not provide any medical or healthcare products, services or advice, and is not for medical emergencies or urgent situations. IF YOU THINK YOU MAY HAVE A MEDICAL EMERGENCY, CALL YOUR DOCTOR OR 911 IMMEDIATELY. Information contained on this website is not a substitute for a doctor's medical judgment or advice. We recommend that you discuss your specific, individual health concerns with your doctor or health care professional.

DGIdb (v4.2.0 - sha1 afd9f30b) • Last updated 2021-04-13