PDGFRs bind type I TKI

Stable Identifier
Reaction [binding]
Homo sapiens
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Wild-type PDGFRA and PDGFRB can be bound and inhibited by class I tyrosine kinase inhibitors including pazopanib, avapritinib, and crenolanib (Gril et al, 2013; Wang et al, 2014; Mathias et al, 2015; Meliau et al, 2017; reviewed in Klug et al, 2018). Type I inhibitors bind in the ATP binding site of the active conformation and prevent full activation of the kinase (reviewed in Roskoski, 2018).
Literature References
PubMed ID Title Journal Year
29408302 The role of small molecule platelet-derived growth factor receptor (PDGFR) inhibitors in the treatment of neoplastic disorders

Roskoski, R

Pharmacol. Res. 2018
23583652 Pazopanib inhibits the activation of PDGFRβ-expressing astrocytes in the brain metastatic microenvironment of breast cancer cells

Liewehr, DJ, Anwar, T, Fernández, P, Palmieri, D, Qian, Y, Steinberg, SM, Masana, D, Gril, B, Andreu, Z, Steeg, PS, Vidal-Vanaclocha, F

Am. J. Pathol. 2013
25597754 The FLT3 and PDGFR inhibitor crenolanib is a substrate of the multidrug resistance protein ABCB1 but does not inhibit transport function at pharmacologically relevant concentrations

Natarajan, K, Ambudkar, SV, Doshi, KA, Shukla, S, Mathias, TJ, Baer, MR, Singh, ZN

Invest New Drugs 2015
29964125 Structural and clinical consequences of activation loop mutations in class III receptor tyrosine kinases

Heinrich, MC, Kent, JD, Klug, LR

Pharmacol. Ther. 2018
29093181 A precision therapy against cancers driven by KIT/PDGFRA mutations

Heinrich, MC, Zhang, Y, Hodous, BL, Shutes, A, Lengauer, C, Evans, EK, Kohl, N, Wolf, B, Schöffski, P, Zhu, XJ, Kim, JL, Gebreyohannes, YK, Gardino, AK, Wozniak, A, DiPietro, L, Lydon, N, Wilson, K, Brooijmans, N, Schmidt-Kittler, O, Boral, A, Miller, S, LaBranche, TP, Deangelo, DJ, Davis, A, Guzi, T, Wilson, D

Sci Transl Med 2017
25328409 Crenolanib, a PDGFR inhibitor, suppresses lung cancer cell proliferation and inhibits tumor growth in vivo

Jiang, Y, Ge, H, Jin, P, Hu, W, Song, L, Geng, N, Wang, P

Onco Targets Ther 2014
28435517 Inhibition of the platelet-derived growth factor receptor beta (PDGFRB) using gene silencing, crenolanib besylate, or imatinib mesylate hampers the malignant phenotype of mesothelioma cell lines

Sensi, E, Cipollini, M, Cristaudo, A, Guazzelli, A, Catalano, C, Melaiu, O, De Santi, C, Gemignani, F, Foddis, R, Barone, E, Bonotti, A, Mutti, L, Evangelista, M, Pellè, L, Boldrini, L, Landi, S, Fontanini, G, Figlioli, G

Genes Cancer 2017
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