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

Clin. Cancer Res. 2007
22665524 Sorafenib inhibits many kinase mutations associated with drug-resistant gastrointestinal stromal tumors

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

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

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

Br. J. Cancer 2019
Participants
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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
Cross References
Mondo
Authored
Rothfels, K  (2020-04-01)
Reviewed
Serrano, C  (2020-03-13)
García-Valverde, A  (2020-03-13)
Pilco-Janeta, D  (2020-03-13)
Created
Rothfels, K  (2019-12-03)
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