Reactome | KIT binds type II TKIs

KIT binds type II TKIs

Stable Identifier

R-HSA-9669854

Type

Reaction [binding]

Species

Homo sapiens

Compartment

plasma membrane, cytosol

ReviewStatus

5/5

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KIT can be bound and inhibited by class II tyrosine kinase inhibitors including imatinib, sunitinib, regorafenib and others. Type II inhibitors bind to the inactive conformation of the kinase and prevent its activation (reviewed in Roskoski, 2018; Abbaspour Babaei et al, 2016; Klug et al, 2018).

Literature References

PubMed ID	Title	Journal	Year
27536065	Receptor tyrosine kinase (c-Kit) inhibitors: a potential therapeutic target in cancer cells Ahmadipour, F, Abbaspour Babaei, M, Huri, HZ, Kamalidehghan, B, Saleem, M	Drug Des Devel Ther	2016
29704617	The role of small molecule Kit protein-tyrosine kinase inhibitors in the treatment of neoplastic disorders Roskoski, R	Pharmacol. Res.	2018
29964125	Structural and clinical consequences of activation loop mutations in class III receptor tyrosine kinases Heinrich, MC, Kent, JD, Klug, LR	Pharmacol. Ther.	2018