Among different targets to design anticancer agents, caspase-3 is an important target as its cleavage and activation lead to apoptosis and finally, cancer cell death. Apart from some naturally occurring molecules, many small molecules have been reported as caspase-3 activators. Objectives: In view ...
Molecular Docking Analysis of Caspase-3 Activators as Potential Anticancer AgentsMolecular dockingcaspaseanti-cancerbinding affinityAutodock 4.2asparagineIntroduction: Caspase-3 plays a leading role in apoptosis and on activation, it cleaves many protein substrates in cells and causes cell death. Since ...
These results raise challenges to use of direct activators as anticancer therapeutic agents. It has been shown that EGF reduces PAC–1 induces caspase–3 activity in PC12 cells. If PAC–1 is a direct activator caspase–3, then caspase–3 depends upon up stream mechanism even when it is ...
The activated caspase-8 directly cleaves procaspase-3, an executioner caspase (Stennicke et al., 1998). In the meanwhile, DNA-damaging agents such as anticancer drugs or irradiation induces apoptosis initiated at the mitochondrion by the release of cytochrome c, the mechanisms of which is not ...
[43,44]. Targeting inhibitors ofcaspasescould potentially cause apoptosis of cancerous cells. Synthetic activators of caspases includeApoptinandIAP[68,71]. Caspase-3 and 9 are subject to inhibition byIAPssuch asLivin[44]. LikeBCL2inhibitors,XIAPinhibitors must block PPIs. When released from ...
3-activating compound 1 (PAC-1) may overcome this limitation. By activating procaspase-3 to generate caspase-3, the main apoptosis effector, PAC-1 bypasses the complex upstream pro-apoptotic signaling cascades and directly induces apoptotic cell death2. Procaspase-3 activators have since attracted...
Induction of apoptosis in cancer cell is the main strategy for the development of anticancer agents targeting apoptosis pathway. Procaspase-3 is one such target for the induction of apoptosis via activation of caspase 3. Novel molecules are needed as procaspase-3 activators which will induce ...
We thus conclude that pisiferdiol and pisiferic acid are novel PP2C activators, and the more specific activator, pisiferdiol, may be a useful chemical probe to study PP2C-mediated signaling pathways, and a lead compound for pharmaceutical agents....
therapies.3 Examples include drugs targeted to anti-apoptotic Bcl-2 family proteins and to inhibitors of apoptosis (IAP) proteins and activators of the TRAIL death receptor signalling pathway.2 In parallel to drug development, there is a clear requirement for biomarkers of tumor cell death ...
In both the cells, FRET loss initiated by around 12 h after PAC-1 treatment (scale bar: 100 mm) Cell Death and Disease Screening tools for direct caspase activators M Seervi et al 6 Figure 3 Induction of cell death in presence and absence of caspase-3 by PAC-1. (a) MCF7 (caspase-...