Sorafenib-resistant KIT mutants do not bind sorafenib

Stable Identifier
Reaction [transition]
Homo sapiens
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KIT receptors with mutations at residue D816 are resistant to inhibition by sorafenib, while other activation loop mutations show variable sensitivity (Guida et al, 2007; Heinrich et al, 2012; Serrano et al, 2019).

Literature References
PubMed ID Title Journal Year
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
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
Normal reaction
Functional status

Loss of function of sorafenib resistant KIT mutants [plasma membrane]

Name Identifier Synonyms
cancer DOID:162 malignant tumor, malignant neoplasm, primary cancer
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