Sorafenib-resistant KIT mutants

Stable Identifier
Homo sapiens
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Sorafenib is a type II tyrosine kinase inhibitor that is approved for use in hepatocellular and renal cell carcinoma. It is active against KIT receptors with mutations in the ATP-binding cleft and the activation loop, with the exception of substitutions at D816, which are resistant (Guida et al, 2007; Heinrich et al, 2012; Serrano et al, 2019; Weisberg et al, 2019; reviewed in Roskoski, 2018; Klug et al, 2012).

Literature References
PubMed ID Title Journal Year
29704617 The role of small molecule Kit protein-tyrosine kinase inhibitors in the treatment of neoplastic disorders

Roskoski, R

Pharmacol. Res. 2018
17545544 Sorafenib inhibits imatinib-resistant KIT and platelet-derived growth factor receptor beta gatekeeper mutants

Guida, T, Carlomagno, F, Provitera, L, Sullivan, E, Anaganti, S, Wilhelm, SM, Gedrich, R, Santoro, M

Clin. Cancer Res. 2007
31309543 Comparison of effects of midostaurin, crenolanib, quizartinib, gilteritinib, sorafenib and BLU-285 on oncogenic mutants of KIT, CBL and FLT3 in haematological malignancies

Griffin, JD, Yang, J, Buhrlage, SJ, Letard, S, Stone, RM, Tiv, HL, Meng, C, Case, AE, Gokhale, PC, Liu, X, Gray, N, Sattler, M, Dubreuil, P, Weisberg, E, Wang, J, Adamia, S

Br. J. Haematol. 2019
22665524 Sorafenib inhibits many kinase mutations associated with drug-resistant gastrointestinal stromal tumors

Fletcher, JA, Mariño-Enríquez, A, Heinrich, MC, Donsky, RS, Presnell, A, Griffith, DJ, McKinley, A, Liang, CW, Patterson, J, Taguchi, T

Mol. Cancer Ther. 2012
30792533 Complementary activity of tyrosine kinase inhibitors against secondary kit mutations in imatinib-resistant gastrointestinal stromal tumours

Heinrich, MC, Ketzer, J, Bauer, S, Zhu, M, Presnell, A, Raut, CP, George, S, Mannan, AM, Serrano, C, Yu, C, Sicinska, E, Tao, DL, Rubin, BP, Fletcher, JA, Mariño-Enríquez, A, Demetri, GD, Eilers, G, Czaplinski, JT, McKinley, A

Br. J. Cancer 2019
29964125 Structural and clinical consequences of activation loop mutations in class III receptor tyrosine kinases

Heinrich, MC, Kent, JD, Klug, LR

Pharmacol. Ther. 2018
Name Identifier Synonyms
cancer DOID:162 malignant tumor, malignant neoplasm, primary cancer
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