Literature DB >> 19854648

Discovery of the first known small-molecule inhibitors of heme-regulated eukaryotic initiation factor 2alpha (HRI) kinase.

Mark D Rosen1, Craig R Woods, Steven D Goldberg, Michael D Hack, A Dawn Bounds, Young Yang, Pamela C Wagaman, Victor K Phuong, Angela P Ameriks, Terrance D Barrett, Kimon C Kanelakis, Jui Chang Chuang, Jui Chang, Nigel P Shankley, Michael H Rabinowitz.   

Abstract

A series of indeno[1,2-c]pyrazoles were discovered to be the first known inhibitors of heme-regulated eukaryotic initiation factor 2alpha (HRI) kinase. The synthesis, structure-activity relationship profile, and in-vitro pharmacological characterization of this inaugural series of HRI kinase inhibitors are detailed.

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Year:  2009        PMID: 19854648     DOI: 10.1016/j.bmcl.2009.10.033

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


  12 in total

Review 1.  Comprehensive survey of chemical libraries for drug discovery and chemical biology: 2009.

Authors:  Roland E Dolle; Bertrand Le Bourdonnec; Karin Worm; Guillermo A Morales; Craig J Thomas; Wei Zhang
Journal:  J Comb Chem       Date:  2010-10-05

2.  The eIF2α Kinase Heme-Regulated Inhibitor Protects the Host from Infection by Regulating Intracellular Pathogen Trafficking.

Authors:  Wael Bahnan; Justin C Boucher; Petoria Gayle; Niraj Shrestha; Mark Rosen; Bertal Aktas; Becky Adkins; Arba Ager; Wasif N Khan; Kurt Schesser
Journal:  Infect Immun       Date:  2018-02-20       Impact factor: 3.441

Review 3.  Heme-regulated inhibitor: an overlooked eIF2α kinase in cancer investigations.

Authors:  Azmi Yerlikaya
Journal:  Med Oncol       Date:  2022-05-15       Impact factor: 3.064

Review 4.  The integrated stress response: From mechanism to disease.

Authors:  Mauro Costa-Mattioli; Peter Walter
Journal:  Science       Date:  2020-04-24       Impact factor: 47.728

Review 5.  Bacterial Manipulation of the Integrated Stress Response: A New Perspective on Infection.

Authors:  Alex Knowles; Susan Campbell; Neil Cross; Prachi Stafford
Journal:  Front Microbiol       Date:  2021-04-22       Impact factor: 5.640

6.  Glutamatergic stimulation induces GluN2B translation by the nitric oxide-Heme-Regulated eIF2α kinase in cortical neurons.

Authors:  Eva Ramos-Fernández; Marta Tajes; Gerard Ill-Raga; Lina Vargas; Arnau Busquets-García; Mònica Bosch-Morató; Biuse Guivernau; Victòria Valls-Comamala; Maria Gomis; Cristina Grau; César Fandos; Mark D Rosen; Michael H Rabinowitz; Nibaldo Inestrosa; Rafael Maldonado; Xavier Altafaj; Andrés Ozaita; Alejandra Alvarez; Rubén Vicente; Miguel A Valverde; Francisco J Muñoz
Journal:  Oncotarget       Date:  2016-09-13

Review 7.  The integrated stress response.

Authors:  Karolina Pakos-Zebrucka; Izabela Koryga; Katarzyna Mnich; Mila Ljujic; Afshin Samali; Adrienne M Gorman
Journal:  EMBO Rep       Date:  2016-09-14       Impact factor: 8.807

Review 8.  Targeting the integrated stress response in ophthalmology.

Authors:  Hsiao-Sang Chu; Cornelia Peterson; Albert Jun; James Foster
Journal:  Curr Eye Res       Date:  2021-01-21       Impact factor: 2.555

9.  The host-encoded Heme Regulated Inhibitor (HRI) facilitates virulence-associated activities of bacterial pathogens.

Authors:  Niraj Shrestha; Justin Boucher; Wael Bahnan; Emily S Clark; Roland Rosqvist; Kenneth A Fields; Wasif N Khan; Kurt Schesser
Journal:  PLoS One       Date:  2013-07-10       Impact factor: 3.240

10.  Triazolo[4,5-d]pyrimidines as Validated General Control Nonderepressible 2 (GCN2) Protein Kinase Inhibitors Reduce Growth of Leukemia Cells.

Authors:  Lea Lough; Dan Sherman; Manuel Beccera-Flores; Olga Lavinda; Eric Ni; Hong Wang; Raoul Tibes; Timothy Cardozo
Journal:  Comput Struct Biotechnol J       Date:  2018-09-28       Impact factor: 7.271

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