Sorafenib-resistant KIT mutants do not bind sorafenib

Stable Identifier
R-HSA-9669874
Type
Reaction [transition]
Species
Homo sapiens
Compartment
plasma membrane
ReviewStatus
5/5
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Sorafenib-resistant KIT mutants do not bind sorafenib
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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
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as an event of
Normal reaction
KIT binds type II TKIs (Homo sapiens)
Functional status

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

Normal Entity
Disease Entity
Status
Disease
Name Identifier Synonyms
cancer DOID:162 malignant tumor, malignant neoplasm, primary cancer
Authored
Rothfels, K  (2020-04-01)
Reviewed
Pilco-Janeta, D  (2020-03-13)
Serrano, C  (2020-03-13)
García-Valverde, A  (2020-03-13)
Created
Rothfels, K  (2019-12-03)
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