Abstract | INTRODUCTION:
Caspase-9 is the apoptotic initiator protease of the intrinsic or mitochondrial apoptotic pathway, which is activated at multi- protein activation platforms. Its activation is believed to involve homo-dimerization of the monomeric zymogens. It binds to the apoptosome to retain substantial catalytic activity. Variety of apoptotic stimuli can regulate caspase-9. However, the mechanism of action of various regulators of caspase-9 has not been summarized and compared yet. In this article, we elucidate the regulators of caspase-9 including microRNAs, natural compounds that are related to caspase-9 and ongoing clinical trials with caspase-9 to better understand the caspase-9 in suppressing cancer. AREAS COVERED: In this study, the basic mechanism of apoptosis pathways, regulators of caspase-9 and the development of drugs to regulate caspase-9 are reviewed. Also, ongoing clinical trials for caspase-9 are discussed. EXPERT OPINION: Apoptosis has crucial role in cancer, brain disease, aging and heart disease to name a few. Since caspase-9 is an initiator caspase of apoptosis, it is an important therapeutic target of various diseases related to apoptosis. Therefore, a deep understanding on the roles as well as regulators of caspase-9 is required to find more effective ways to conquer apoptosis-related diseases especially cancer.
|
Authors | Bonglee Kim, Sanjay K Srivastava, Sung-Hoon Kim |
Journal | Expert opinion on therapeutic targets
(Expert Opin Ther Targets)
Vol. 19
Issue 1
Pg. 113-27
(Jan 2015)
ISSN: 1744-7631 [Electronic] England |
PMID | 25256701
(Publication Type: Journal Article, Research Support, N.I.H., Extramural, Research Support, Non-U.S. Gov't, Review)
|
Chemical References |
- Biological Products
- Caspase 9
|
Topics |
- Animals
- Apoptosis
(physiology)
- Biological Products
(pharmacology)
- Caspase 9
(metabolism)
- Humans
- Neoplasms
(drug therapy, metabolism)
|