A2 Vertaisarvioitu katsausartikkeli tieteellisessä lehdessä
A holistic view on c-Kit in cancer: Structure, signaling, pathophysiology and its inhibitors
Tekijät: Pathania Shelly, Pentikäinen Olli T, Singh Pankaj Kumar
Kustantaja: ELSEVIER
Julkaisuvuosi: 2021
Journal: BBA - Reviews on Cancer
Tietokannassa oleva lehden nimi: BIOCHIMICA ET BIOPHYSICA ACTA-REVIEWS ON CANCER
Lehden akronyymi: BBA-REV CANCER
Artikkelin numero: ARTN 188631
Vuosikerta: 1876
Numero: 2
Sivujen määrä: 21
ISSN: 0304-419X
eISSN: 1879-2561
DOI: https://doi.org/10.1016/j.bbcan.2021.188631
Verkko-osoite: https://www.sciencedirect.com/science/article/pii/S0304419X21001293?via%3Dihub
Rinnakkaistallenteen osoite: https://research.utu.fi/converis/portal/detail/Publication/67765444
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 is c-Kit, a type-III receptor tyrosine kinase, which is involved in various intracellular signaling pathways. The role of different mutant isoforms of c-Kit has been established in several types of cancers. Accordingly, promising c-Kit inhibition results have been reported for the treatment of different cancers (e.g., gastrointestinal stromal tumors, melanoma, acute myeloid leukemia, and other tumors). Therefore, lots of effort has been put to target c-Kit for the treatment of cancer. Here, we provide a comprehensive compilation to provide an insight into c-Kit inhibitor discovery. This compilation provides key information regarding the structure, signaling pathways related to c-Kit, and, more importantly, pharmacophores, binding modes, and SAR analysis for almost all small-molecule heterocycles reported for their c-Kit inhibitory activity. This work could be used as a guide in understanding the basic requirements for targeting c-Kit, and how the selectivity and efficacy of the molecules have been achieved till today.
Ladattava julkaisu This is an electronic reprint of the original article. |  |
