KIT as a therapeutic target for non-oncological diseases

A Martinez-Anton, D Gras, A Bourdin, P Dubreuil… - Pharmacology & …, 2019 - Elsevier
KIT is a receptor tyrosine kinase that after binding to its ligand stem cell factor activates
signaling cascades linked to biological processes such as proliferation, differentiation …

Inhibition of KIT tyrosine kinase activity: a novel molecular approach to the treatment of KIT-positive malignancies

MC Heinrich, CD Blanke, BJ Druker… - Journal of clinical …, 2002 - ascopubs.org
PURPOSE: Activation of the KIT tyrosine kinase by somatic mutation has been documented
in a number of human malignancies, including gastrointestinal stromal tumor (GIST) …

Therapeutic targeting of c-KIT in cancer

LK Ashman, R Griffith - Expert opinion on investigational drugs, 2013 - Taylor & Francis
Introduction: Mutated forms of the receptor tyrosine kinase c-KIT are “drivers” in several
cancers and are attractive targets for therapy. While benefits have been obtained from use of …

[HTML][HTML] Inhibition of KIT tyrosine kinase activity: two decades after the first approval

LR Klug, CL Corless, MC Heinrich - Journal of Clinical Oncology, 2021 - ncbi.nlm.nih.gov
In 2002, we published a review in Journal of Clinical Oncology examining the potential of
KIT inhibition to treat advanced cancer. 1 At that time, imatinib was the first and only US …

Kit: molecule of interest for the diagnosis and treatment of mastocytosis and other neoplastic disorders

MM Patnaik, A Tefferi… - Current cancer drug targets, 2007 - ingentaconnect.com
Kit a type III receptor tyrosine kinase, along with its ligand the stem cell factor, play a critical
role in normal cell growth, differentiation, development and survival. Ligand independent …

Targeting c-Kit mutations: basic science to novel therapies

M Sattler, R Salgia - Leukemia research, 2004 - Elsevier
The Kit receptor tyrosine kinase is a transmembrane receptor that is expressed in a variety of
different tissues and mediates pleiotropic biological effects through its ligand stem cell factor …

Receptor tyrosine kinase (c-Kit) inhibitors: a potential therapeutic target in cancer cells

M Abbaspour Babaei, B Kamalidehghan… - Drug design …, 2016 - Taylor & Francis
c-Kit, a receptor tyrosine kinase, is involved in intracellular signaling, and the mutated form
of c-Kit plays a crucial role in occurrence of some cancers. The function of c-Kit has led to the …

[HTML][HTML] A holistic view on c-Kit in cancer: Structure, signaling, pathophysiology and its inhibitors

S Pathania, OT Pentikäinen, PK Singh - Biochimica et Biophysica Acta …, 2021 - Elsevier
Receptor tyrosine kinases play an important role in many cellular processes, and their
dysregulation leads to diseases, most importantly cancer. One such receptor tyrosine kinase …

KIT-D816V oncogenic activity is controlled by the juxtamembrane docking site Y568-Y570

A Chaix, ML Arcangeli, S Lopez, E Voisset, Y Yang… - Oncogene, 2014 - nature.com
Mutation of KIT receptor tyrosine kinase at residue D816 results in ligand-independent
constitutive kinase activity. This mutation occurs in most patients with mastocytosis, a …

Inhibition of constitutively active forms of mutant kit by multitargeted indolinone tyrosine kinase inhibitors

AT Liao, MB Chien, N Shenoy… - Blood, The Journal …, 2002 - ashpublications.org
Mutations in the proto-oncogene c-kit, including point mutations, deletions, or duplications in
the negative regulatory juxtamembrane (JM) domain or point mutations in the catalytic …