View : 41 Download: 0

PDK1 disruptors and modulators: a patent review

Title
PDK1 disruptors and modulators: a patent review
Authors
Hossen, Muhammad JahangirKim, Seung CheolYang, SungjaeKim, Han GyungJeong, DeokYi, Young-SuSung, Nak YoonLee, Jeong-OogKim, Jong-HoonCho, Jae Youl
Ewha Authors
김승철
SCOPUS Author ID
김승철scopus
Issue Date
2015
Journal Title
EXPERT OPINION ON THERAPEUTIC PATENTS
ISSN
1354-3776JCR Link1744-7674JCR Link
Citation
vol. 25, no. 5, pp. 513 - 537
Keywords
3-phosphoinositide-dependent kinase 13-phosphoinositide-dependent kinase 1 inhibitors3-phosphoinositide-dependent kinase 1 modulators
Publisher
INFORMA HEALTHCARE
Indexed
SCIE; SCOPUS WOS scopus
Abstract
Introduction: 3-Phosphoinositide-dependent kinase 1 (PDK1) is a master regulator of the AGC protein kinase family and is a critical activator of multiple pro-survival and oncogenic protein kinases, for which it has garnered considerable interest as an oncology drug target. Areas covered: This manuscript reviews small molecule patent literature disclosures between October 2011 and September 2014 for both PDK1 activators and inhibitors and restates the selective patents published before September 2011. PDK1 modulators are organized according to pharmaceutical company and chemical structural class. Expert opinion: Many academic institutions and pharmaceutical companies continue to research into the development of small molecules that can function as PDK1 inhibitors or modulators. To date, > 50 patent publications on PDK1 disruptors and modulators have been published since the protein was first discovered in 1998. Most of these molecules act as ATP mimetics, forming similar hydrogen bonding patterns to PDK1 as ATP and functioning as hydrophobic pharmacophores. To achieve selectivity in PDK1 inhibition, the discovery of binding pockets structurally distinctive from the ATP site is a challenging but promising strategy.
DOI
10.1517/13543776.2015.1014801
Appears in Collections:
의과대학 > 의학과 > Journal papers
Files in This Item:
There are no files associated with this item.
Export
RIS (EndNote)
XLS (Excel)
XML


qrcode

Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.

BROWSE