PDK1 disruptors and modulators: A patent review

Muhammad Jahangir Hossen, Seung Cheol Kim, Sungjae Yang, Han Gyung Kim, Deok Jeong, Young Su Yi, Nak Yoon Sung, Jeong Oog Lee, Jong Hoon Kim, Jae Youl Cho

Research output: Contribution to journalReview articlepeer-review

20 Scopus citations


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.

Original languageEnglish
Pages (from-to)513-537
Number of pages25
JournalExpert Opinion on Therapeutic Patents
Issue number5
StatePublished - 1 May 2015

Bibliographical note

Funding Information:
The authors were supported by a grant of the Korean Health Technology R&D Project, Ministry of Health & Welfare, Republic of Korea (HI12C0050). The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed. Writing assistance was utilized in the production of this manuscript from E-word editing company and funded by Sunkyunkwan University.

Publisher Copyright:
© Informa UK, Ltd.


  • 3-phosphoinositide-dependent kinase 1
  • 3-phosphoinositide-dependent kinase 1 inhibitors
  • 3-phosphoinositide-dependent kinase 1 modulators


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