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Selective and potent small-molecule inhibitors of PI3Ks

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Title
Selective and potent small-molecule inhibitors of PI3Ks
Author(s)
Yujeong Jeong; Daeil Kwon; Sung Woo Hong
Publication Date
2014-05
Journal
FUTURE MEDICINAL CHEMISTRY, v.6, no.7, pp.737 - 756
Publisher
FUTURE SCI LTD
Abstract
Class I PI3Ks are composed of four catalytic subunit variants (p110, p110, p110 and p110). The PI3K pathway is among the most frequently activated pathways in many diseases, and has emerged as an attractive target for drug development, in particular for the treatment of many human cancers including breast, prostate, ovarian, gastric, colon and hepatocellular cancers. One of the challenges in the discovery of drugs that target kinases is designing small-molecule inhibitors that are sufficiently selective to minimize off-target activity and reduce the risk of potential toxicity. This review explores the current landscape of PI3K-selective inhibitor development and highlights recent advances in achieving selectivity for PI3Ks over other protein kinases, with an emphasis on available structural information.
URI
https://pr.ibs.re.kr/handle/8788114/1038
ISSN
1756-8919
Appears in Collections:
Center for Catalytic Hydrocarbon Functionalizations(분자활성 촉매반응 연구단) > Journal Papers (저널논문)
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