Evolution of PIKK family kinase inhibitors: a new age cancer therapeutics

Show simple item record

dc.contributor.author Shaik, Althaf
dc.contributor.author Kirubakaran, Sivapriya
dc.date.accessioned 2020-03-12T08:51:48Z
dc.date.available 2020-03-12T08:51:48Z
dc.date.issued 2020-03
dc.identifier.citation Shaik, Althaf and Kirubakaran, Sivapriya, “Evolution of PIKK family kinase inhibitors: a new age cancer therapeutics”, Frontiers in Bioscience, Landmark Edition, DOI: 10.2741/4866, vol. 25, no. 8, pp. 1510-1537, Mar. 2020. en_US
dc.identifier.issn 1093-9946
dc.identifier.issn a1093-4715
dc.identifier.uri https://dx.doi.org/10.2741/4866
dc.identifier.uri https://repository.iitgn.ac.in/handle/123456789/5256
dc.description.abstract Phosphatidylinositol-3 kinase-related kinases (PIKKs) belong to a family of atypical serine/threonine kinases in humans. They actively participate in a diverse set of cellular functions such as meiotic, V(D)J recombination, chromosome maintenance, DNA damage sensing and repair, cell cycle progression and arrest. ATR, ATM, DNA-PKcs, mTOR and hSMG are the members of the PIKK family that play an important role in in cancer cell proliferation, autophagy, and cell survival to radio and chemotherapy. Thereby targeting these PIKK kinases in cancer along with chemo/radiotherapy agents, can help in differential cytotoxicity towards cancer cell over the normal cell. In this review, we compile the various small molecule kinase inhibitors with respect to structural and strategic targeting of PIKK family members. Rapalogs, AZD8055, AZD2014, OSI-027, INK-128, MLN0128, VX970, NVP-BEZ235, Torin2, AZ20, and AZ31 are the diverse scaffolds which have successfully made into the pre-clinical trials either as mono or combinatorial therapy for the treatment of various human cancers. Their synthesis and pre-clinical trial highlight the challenges associated in the development process.
dc.description.statementofresponsibility by Althaf Shaik and Sivapriya Kirubakaran
dc.format.extent vol. 25, pp. 1510-1537
dc.language.iso en_US en_US
dc.publisher Frontiers in Bioscience en_US
dc.title Evolution of PIKK family kinase inhibitors: a new age cancer therapeutics en_US
dc.type Article en_US
dc.relation.journal Frontiers in Bioscience

Files in this item

Files Size Format View

There are no files associated with this item.

This item appears in the following Collection(s)

Show simple item record

Search Digital Repository


My Account