Literature DB >> 20810279

Discovery of pyrrolopyrimidine inhibitors of Akt.

James F Blake1, Nicholas C Kallan, Dengming Xiao, Rui Xu, Josef R Bencsik, Nicholas J Skelton, Keith L Spencer, Ian S Mitchell, Richard D Woessner, Susan L Gloor, Tyler Risom, Stefan D Gross, Matthew Martinson, Tony H Morales, Guy P A Vigers, Barbara J Brandhuber.   

Abstract

The discovery and optimization of a series of pyrrolopyrimidine based protein kinase B (Pkb/Akt) inhibitors discovered via HTS and structure based drug design is reported. The compounds demonstrate potent inhibition of all three Akt isoforms and knockdown of phospho-PRAS40 levels in LNCaP cells and tumor xenografts.
Copyright © 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID： 20810279     DOI： 10.1016/j.bmcl.2010.08.053

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  9 in total

Review 1.  Inhibition of Akt with small molecules and biologics: historical perspective and current status of the patent landscape.

Authors:  Margrith E Mattmann; Sydney L Stoops; Craig W Lindsley
Journal:  Expert Opin Ther Pat       Date:  2011-06-02       Impact factor: 6.674

2.  Oncogene mimicry as a mechanism of primary resistance to BRAF inhibitors.

Authors:  Martin L Sos; Rebecca S Levin; John D Gordan; Juan A Oses-Prieto; James T Webber; Megan Salt; Byron Hann; Alma L Burlingame; Frank McCormick; Sourav Bandyopadhyay; Kevan M Shokat
Journal:  Cell Rep       Date:  2014-08-07       Impact factor: 9.423

3.  Combining ligand- and structure-based in silico methods for the identification of natural product-based inhibitors of Akt1.

Authors:  Priya Mahajan; Bhumika Wadhwa; Manas Ranjan Barik; Fayaz Malik; Amit Nargotra
Journal:  Mol Divers       Date:  2019-02-23       Impact factor: 2.943

4.  Single-molecule studies reveal regulatory interactions between master kinases PDK1, AKT1, and PKC.

Authors:  Moshe T Gordon; Brian P Ziemba; Joseph J Falke
Journal:  Biophys J       Date:  2021-10-19       Impact factor: 4.033

5.  New chemical scaffolds for human african trypanosomiasis lead discovery from a screen of tyrosine kinase inhibitor drugs.

Authors:  Ranjan Behera; Sarah M Thomas; Kojo Mensa-Wilmot
Journal:  Antimicrob Agents Chemother       Date:  2014-01-27       Impact factor: 5.191

6.  Efficient solution-phase synthesis of 4,5,7-trisubstituted pyrrolo[3,2-d]pyrimidines.

Authors:  Weihe Zhang; Jing Liu; Michael A Stashko; Xiaodong Wang
Journal:  ACS Comb Sci       Date:  2012-12-05       Impact factor: 3.784

7.  Efficient and cost effective production of active-form human PKB using silkworm larvae.

Authors:  Ryoko Maesaki; Ryosuke Satoh; Masato Taoka; Teppei Kanaba; Tsunaki Asano; Chiharu Fujita; Toshinobu Fujiwara; Yutaka Ito; Toshiaki Isobe; Toshio Hakoshima; Katsumi Maenaka; Masaki Mishima
Journal:  Sci Rep       Date:  2014-08-15       Impact factor: 4.379

8.  Kinome rewiring reveals AURKA limits PI3K-pathway inhibitor efficacy in breast cancer.

Authors:  Hayley J Donnella; James T Webber; Rebecca S Levin; Roman Camarda; Olga Momcilovic; Nora Bayani; Khyati N Shah; James E Korkola; Kevan M Shokat; Andrei Goga; John D Gordan; Sourav Bandyopadhyay
Journal:  Nat Chem Biol       Date:  2018-06-25       Impact factor: 15.040

Review 9.  Drug Discovery of Plausible Lead Natural Compounds That Target the Insulin Signaling Pathway: Bioinformatics Approaches.

Authors:  Siba Shanak; Najlaa Bassalat; Ahmad Barghash; Sleman Kadan; Mahmoud Ardah; Hilal Zaid
Journal:  Evid Based Complement Alternat Med       Date:  2022-03-20       Impact factor: 2.629
  9 in total

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