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Pim kinase inhibitors in cancer: medicinal chemistry insights into their activity and selectivity.
- Source :
-
Drug discovery today [Drug Discov Today] 2020 Sep 21. Date of Electronic Publication: 2020 Sep 21. - Publication Year :
- 2020
- Publisher :
- Ahead of Print
-
Abstract
- The oncogenic Pim kinase proteins (Pim-1/2/3) regulate tumorigenesis through phosphorylating essential proteins that control cell cycle and proliferation. Pim kinase is a potential chemotherapeutic target in cancer and its inhibition is currently the focus of intensive drug design and development efforts. The distinctive presence of proline amino acids in the hinge region provides an opportunity to inhibit Pim kinase while conserving the physiological functions of other kinases and reducing the toxicity profiles of the inhibitors. Various Pim kinase inhibitors have been clinically evaluated for the treatment of hematological cancers, yet none has reached the clinic. In this review, we discuss the design and development of selective and potent Pim inhibitors with novel chemotypes focusing on structural features essential for high potency and selectivity.<br /> (Copyright © 2020 Elsevier Ltd. All rights reserved.)
Details
- Language :
- English
- ISSN :
- 1878-5832
- Database :
- MEDLINE
- Journal :
- Drug discovery today
- Publication Type :
- Academic Journal
- Accession number :
- 32971234
- Full Text :
- https://doi.org/10.1016/j.drudis.2020.09.017