Literature DB >> 25587754

Discovery of 1H-pyrazol-3(2H)-ones as potent and selective inhibitors of protein kinase R-like endoplasmic reticulum kinase (PERK).

Adrian L Smith1, Kristin L Andrews, Holger Beckmann, Steven F Bellon, Pedro J Beltran, Shon Booker, Hao Chen, Young-Ah Chung, Noel D D'Angelo, Jennifer Dao, Kenneth R Dellamaggiore, Peter Jaeckel, Richard Kendall, Katja Labitzke, Alexander M Long, Silvia Materna-Reichelt, Petia Mitchell, Mark H Norman, David Powers, Mark Rose, Paul L Shaffer, Michelle M Wu, J Russell Lipford.   

Abstract

The structure-based design and optimization of a novel series of selective PERK inhibitors are described resulting in the identification of 44 as a potent, highly selective, and orally active tool compound suitable for PERK pathway biology exploration both in vitro and in vivo.

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Year:  2015        PMID: 25587754     DOI: 10.1021/jm5017494

Source DB:  PubMed          Journal:  J Med Chem        ISSN: 0022-2623            Impact factor:   7.446


  25 in total

1.  When PERK inhibitors turn out to be new potent RIPK1 inhibitors: critical issues on the specificity and use of GSK2606414 and GSK2656157.

Authors:  Diego Rojas-Rivera; Tinneke Delvaeye; Ria Roelandt; Wim Nerinckx; Koen Augustyns; Peter Vandenabeele; Mathieu J M Bertrand
Journal:  Cell Death Differ       Date:  2017-04-28       Impact factor: 15.828

Review 2.  Unfolded Protein Response as a Therapeutic Target in Cardiovascular Disease.

Authors:  Guangyu Zhang; Xiaoding Wang; Thomas G Gillette; Yingfeng Deng; Zhao V Wang
Journal:  Curr Top Med Chem       Date:  2019       Impact factor: 3.295

Review 3.  Small molecule strategies to harness the unfolded protein response: where do we go from here?

Authors:  Julia M D Grandjean; R Luke Wiseman
Journal:  J Biol Chem       Date:  2020-09-04       Impact factor: 5.157

4.  The Unfolded Protein Response Mediator PERK Governs Myeloid Cell-Driven Immunosuppression in Tumors through Inhibition of STING Signaling.

Authors:  Eslam Mohamed; Rosa A Sierra; Jimena Trillo-Tinoco; Yu Cao; Patrick Innamarato; Kyle K Payne; Alvaro de Mingo Pulido; Jessica Mandula; Shuzhong Zhang; Paul Thevenot; Subir Biswas; Sarah K Abdalla; Tara Lee Costich; Kay Hänggi; Carmen M Anadon; Elsa R Flores; Eric B Haura; Shikhar Mehrotra; Shari Pilon-Thomas; Brian Ruffell; David H Munn; Juan R Cubillos-Ruiz; Jose R Conejo-Garcia; Paulo C Rodriguez
Journal:  Immunity       Date:  2020-04-14       Impact factor: 31.745

Review 5.  The eIF2-alpha kinase HRI: a potential target beyond the red blood cell.

Authors:  Nicholas Burwick; Bertal H Aktas
Journal:  Expert Opin Ther Targets       Date:  2017-10-30       Impact factor: 6.902

6.  Endorepellin evokes an angiostatic stress signaling cascade in endothelial cells.

Authors:  Aastha Kapoor; Carolyn G Chen; Renato V Iozzo
Journal:  J Biol Chem       Date:  2020-03-23       Impact factor: 5.157

Review 7.  The entangled ER-mitochondrial axis as a potential therapeutic strategy in neurodegeneration: A tangled duo unchained.

Authors:  Amit U Joshi; Opher S Kornfeld; Daria Mochly-Rosen
Journal:  Cell Calcium       Date:  2016-05-07       Impact factor: 6.817

8.  Identification of Novel, Potent, and Orally Available GCN2 Inhibitors with Type I Half Binding Mode.

Authors:  Jun Fujimoto; Osamu Kurasawa; Terufumi Takagi; Xin Liu; Hiroshi Banno; Takuto Kojima; Yasutomi Asano; Akito Nakamura; Tadahiro Nambu; Akito Hata; Tsuyoshi Ishii; Tomoya Sameshima; Yasuyuki Debori; Maki Miyamoto; Michael G Klein; Richard Tjhen; Bi-Ching Sang; Irena Levin; Scott Weston Lane; Gyorgy P Snell; Ke Li; Georgia Kefala; Isaac D Hoffman; Steve C Ding; Douglas R Cary; Ryo Mizojiri
Journal:  ACS Med Chem Lett       Date:  2019-09-19       Impact factor: 4.345

Review 9.  Endoplasmic reticulum stress signals in the tumour and its microenvironment.

Authors:  Xi Chen; Juan R Cubillos-Ruiz
Journal:  Nat Rev Cancer       Date:  2020-11-19       Impact factor: 60.716

Review 10.  Pharmacological Manipulation of Translation as a Therapeutic Target for Chronic Pain.

Authors:  Muhammad Saad Yousuf; Stephanie I Shiers; James J Sahn; Theodore J Price
Journal:  Pharmacol Rev       Date:  2021-01       Impact factor: 25.468

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