PDGFRs bind type II TKI

Stable Identifier
R-HSA-9674095
Type
Reaction [binding]
Species
Homo sapiens
Compartment
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Wild-type PDGFRA and PDGFRB can be bound and inhibited by class II tyrosine kinase inhibitors including imatinib, nilotinib, sorafenib, sunitinib, ripretinib and others (Lombardo et al, 2004; Chen et la, 2006; Matsui et al, 2008; Liu et al, 2011; Hilberg et al, 2008; Hilberg et al 2017; Wilhelm et al 2002; Strumberg et al, 2005; Mendel et al, 2003; Roskoski, 2007; Smith et al, 2019). Type II inhibitors bind to the inactive conformation of the kinase and prevent its activation (reviewed in Roskoski, 2018; Papadopoulos and Lennartsson, 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
21251937 Inhibition of PDGF, TGF-β, and Abl signaling and reduction of liver fibrosis by the small molecule Bcr-Abl tyrosine kinase antagonist Nilotinib

Liu, Y, Wang, Z, Kwong, SQ, Lui, ELH, Friedman, SL, Li, FR, Lam, RWC, Zhang, GC, Zhang, H, Ye, T

J. Hepatol. 2011
16436588 Potent inhibition of platelet-derived growth factor-induced responses in vascular smooth muscle cells by BMS-354825 (dasatinib)

Chen, Z, Lee, FY, Bhalla, KN, Wu, J

Mol. Pharmacol. 2006
18559524 BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy

Hilberg, F, Roth, GJ, Krssak, M, Kautschitsch, S, Sommergruber, W, Tontsch-Grunt, U, Garin-Chesa, P, Bader, G, Zoephel, A, Quant, J, Heckel, A, Rettig, WJ

Cancer Res. 2008
17943726 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

Matsui, J, Yamamoto, Y, Funahashi, Y, Tsuruoka, A, Watanabe, T, Wakabayashi, T, Uenaka, T, Asada, M

Int J Cancer 2008
31085175 Ripretinib (DCC-2618) Is a Switch Control Kinase Inhibitor of a Broad Spectrum of Oncogenic and Drug-Resistant KIT and PDGFRA Variants

Smith, BD, Kaufman, MD, Lu, WP, Gupta, A, Leary, CB, Wise, SC, Rutkoski, TJ, Ahn, YM, Al-Ani, G, Bulfer, SL, Caldwell, TM, Chun, L, Ensinger, CL, Hood, MM, McKinley, A, Patt, WC, Ruiz-Soto, R, Su, Y, Telikepalli, H, Town, A, Turner, BA, Vogeti, L, Vogeti, S, Yates, K, Janku, F, Abdul Razak, AR, Rosen, O, Heinrich, MC, Flynn, DL

Cancer Cell 2019
12369853 BAY 43-9006: preclinical data

Wilhelm, S, Chien, DS

Curr. Pharm. Des. 2002
15615512 Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays

Lombardo, LJ, Lee, FY, Chen, P, Norris, D, Barrish, JC, Behnia, K, Castaneda, S, Cornelius, LA, Das, J, Doweyko, AM, Fairchild, C, Hunt, JT, Inigo, I, Johnston, K, Kamath, A, Kan, D, Klei, H, Marathe, P, Pang, S, Peterson, R, Pitt, S, Schieven, GL, Schmidt, RJ, Tokarski, J, Wen, ML, Wityak, J, Borzilleri, RM

J. Med. Chem. 2004
12538485 In vivo antitumor activity of SU11248, a novel tyrosine kinase inhibitor targeting vascular endothelial growth factor and platelet-derived growth factor receptors: determination of a pharmacokinetic/pharmacodynamic relationship

Mendel, DB, Laird, AD, Xin, X, Louie, SG, Christensen, JG, Li, G, Schreck, RE, Abrams, TJ, Ngai, TJ, Lee, LB, Murray, LJ, Carver, J, Chan, E, Moss, KG, Haznedar, JO, Sukbuntherng, J, Blake, RA, Sun, L, Tang, C, Miller, T, Shirazian, S, McMahon, G, Cherrington, JM

Clin. Cancer Res. 2003
29263244 Triple Angiokinase Inhibitor Nintedanib Directly Inhibits Tumor Cell Growth and Induces Tumor Shrinkage via Blocking Oncogenic Receptor Tyrosine Kinases

Hilberg, F, Tontsch-Grunt, U, Baum, A, Le, AT, Doebele, RC, Lieb, S, Gianni, D, Voss, T, Garin-Chesa, P, Haslinger, C, Kraut, N

J. Pharmacol. Exp. Ther. 2018
17367763 Sunitinib: a VEGF and PDGF receptor protein kinase and angiogenesis inhibitor

Roskoski, R

Biochem. Biophys. Res. Commun. 2007
29137923 The PDGF/PDGFR pathway as a drug target

Papadopoulos, N, Lennartsson, J

Mol. Aspects Med. 2018
16474853 Preclinical and clinical development of the oral multikinase inhibitor sorafenib in cancer treatment

Strumberg, D

Drugs Today 2005
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