Volume 20 No 15 (2022)
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COMBRETASTATINS: POTENTIAL TUBULIN INHIBITORS
Ayushi chawla, Ganesh Prasad Mishra,Ayushi Chawla
Abstract
Combretastatin is a tubulin inhibitor that distinguishes from many other naturally occurring, synthetic,
and semi-synthetic tubulin inhibitors discovered in the past. Several pro-drugs have undergone
thorough clinical testing as vascular targeting medicines, such as combretastatin A4 phosphate derived
from combretastatins (Vascular disrupting Agents). The clinical study of combretastatins as Vascular
Disrupting Agents was prompted by their improved selectivity towards endothelial cells as well as their
intrinsic capacity to swiftly cause vascular shutdown and inhibit tumour development. The molecular
target of combretastatins and the huge majority of their tubulin, synthetic variants, is well known.
Disruption of the microtubule by combretastatins that target it reduces cell growth and causes aberrant
mitotic spindles in the G2-M phase of cell cycle. Combretastatin A-4 inhibits tubulin polymerization by
engaging with the microtubule's colchicine binding site and has shown a significant lethal impact in a
broad range of preclinical tumour types. By altering the dynamics of tubulin, such as depolymerization
and polymerization combretastatin has an impact. Numerous analogues made from combretastatin
have also been created due to their structural simplicity and have shown strong promise as inhibitors of
tubulin polymerization. In this review, the pharmacological properties of combretastatin as a category of
effective antimitotic anticancer agents are presented and discussed.
Keywords
Antitumour agents, Combretastatin, Microtubule, Tubulin, Tubulin inhibitor
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