Literature DB >> 27774131

Development of a Potent and Selective HDAC8 Inhibitor.

Oscar J Ingham1, Ronald M Paranal2, William B Smith2, Randolph A Escobar1, Han Yueh1, Tracy Snyder1, John A Porco1, James E Bradner3, Aaron B Beeler1.   

Abstract

A novel, isoform-selective inhibitor of histone deacetylase 8 (HDAC8) has been discovered by the repurposing of a diverse compound collection. Medicinal chemistry optimization led to the identification of a highly potent (0.8 nM) and selective inhibitor of HDAC8.

Entities:  

Keywords:  HDAC; HDAC8; Histone deacetylase; epigenetic; histone deacetylase 8; triazole

Year:  2016        PMID： 27774131      PMCID： PMC5066159          DOI： 10.1021/acsmedchemlett.6b00239

Source DB:  PubMed          Journal:  ACS Med Chem Lett        ISSN： 1948-5875            Impact factor:   4.345


  29 in total

Review 1.  Histone deacetylase inhibitors and the promise of epigenetic (and more) treatments for cancer.

Authors:  Saverio Minucci; Pier Giuseppe Pelicci
Journal:  Nat Rev Cancer       Date:  2006-01       Impact factor: 60.716

Review 2.  Histone deacetylases and their inhibitors in cancer, neurological diseases and immune disorders.

Authors:  Katrina J Falkenberg; Ricky W Johnstone
Journal:  Nat Rev Drug Discov       Date:  2014-08-18       Impact factor: 84.694

3.  Variable active site loop conformations accommodate the binding of macrocyclic largazole analogues to HDAC8.

Authors:  Christophe Decroos; Dane J Clausen; Brandon E Haines; Olaf Wiest; Robert M Williams; David W Christianson
Journal:  Biochemistry       Date:  2015-03-20       Impact factor: 3.162

4.  HDAC8 Catalyzes the Hydrolysis of Long Chain Fatty Acyl Lysine.

Authors:  Pornpun Aramsangtienchai; Nicole A Spiegelman; Bin He; Seth P Miller; Lunzhi Dai; Yingming Zhao; Hening Lin
Journal:  ACS Chem Biol       Date:  2016-08-05       Impact factor: 5.100

5.  Discovery of the first histone deacetylase 6/8 dual inhibitors.

Authors:  David E Olson; Florence F Wagner; Taner Kaya; Jennifer P Gale; Nadia Aidoud; Emeline L Davoine; Fanny Lazzaro; Michel Weïwer; Yan-Ling Zhang; Edward B Holson
Journal:  J Med Chem       Date:  2013-05-29       Impact factor: 7.446

6.  Crystal structure of a eukaryotic zinc-dependent histone deacetylase, human HDAC8, complexed with a hydroxamic acid inhibitor.

Authors:  Alessandro Vannini; Cinzia Volpari; Gessica Filocamo; Elena Caroli Casavola; Mirko Brunetti; Debora Renzoni; Prasun Chakravarty; Chantal Paolini; Raffaele De Francesco; Paola Gallinari; Christian Steinkühler; Stefania Di Marco
Journal:  Proc Natl Acad Sci U S A       Date:  2004-10-11       Impact factor: 11.205

7.  HDAC8 mutations in Cornelia de Lange syndrome affect the cohesin acetylation cycle.

Authors:  Matthew A Deardorff; Masashige Bando; Ryuichiro Nakato; Erwan Watrin; Takehiko Itoh; Masashi Minamino; Katsuya Saitoh; Makiko Komata; Yuki Katou; Dinah Clark; Kathryn E Cole; Elfride De Baere; Christophe Decroos; Nataliya Di Donato; Sarah Ernst; Lauren J Francey; Yolanda Gyftodimou; Kyotaro Hirashima; Melanie Hullings; Yuuichi Ishikawa; Christian Jaulin; Maninder Kaur; Tohru Kiyono; Patrick M Lombardi; Laura Magnaghi-Jaulin; Geert R Mortier; Naohito Nozaki; Michael B Petersen; Hiroyuki Seimiya; Victoria M Siu; Yutaka Suzuki; Kentaro Takagaki; Jonathan J Wilde; Patrick J Willems; Claude Prigent; Gabriele Gillessen-Kaesbach; David W Christianson; Frank J Kaiser; Laird G Jackson; Toru Hirota; Ian D Krantz; Katsuhiko Shirahige
Journal:  Nature       Date:  2012-09-13       Impact factor: 49.962

8.  Loss-of-function HDAC8 mutations cause a phenotypic spectrum of Cornelia de Lange syndrome-like features, ocular hypertelorism, large fontanelle and X-linked inheritance.

Authors:  Frank J Kaiser; Morad Ansari; Diana Braunholz; María Concepción Gil-Rodríguez; Christophe Decroos; Jonathan J Wilde; Christopher T Fincher; Maninder Kaur; Masashige Bando; David J Amor; Paldeep S Atwal; Melanie Bahlo; Christine M Bowman; Jacquelyn J Bradley; Han G Brunner; Dinah Clark; Miguel Del Campo; Nataliya Di Donato; Peter Diakumis; Holly Dubbs; David A Dyment; Juliane Eckhold; Sarah Ernst; Jose C Ferreira; Lauren J Francey; Ulrike Gehlken; Encarna Guillén-Navarro; Yolanda Gyftodimou; Bryan D Hall; Raoul Hennekam; Louanne Hudgins; Melanie Hullings; Jennifer M Hunter; Helger Yntema; A Micheil Innes; Antonie D Kline; Zita Krumina; Hane Lee; Kathleen Leppig; Sally Ann Lynch; Mark B Mallozzi; Linda Mannini; Shane McKee; Sarju G Mehta; Ieva Micule; Shehla Mohammed; Ellen Moran; Geert R Mortier; Joe-Ann S Moser; Sarah E Noon; Naohito Nozaki; Luis Nunes; John G Pappas; Lynette S Penney; Antonio Pérez-Aytés; Michael B Petersen; Beatriz Puisac; Nicole Revencu; Elizabeth Roeder; Sulagna Saitta; Angela E Scheuerle; Karen L Schindeler; Victoria M Siu; Zornitza Stark; Samuel P Strom; Heidi Thiese; Inga Vater; Patrick Willems; Kathleen Williamson; Louise C Wilson; Hakon Hakonarson; Fabiola Quintero-Rivera; Jolanta Wierzba; Antonio Musio; Gabriele Gillessen-Kaesbach; Feliciano J Ramos; Laird G Jackson; Katsuhiko Shirahige; Juan Pié; David W Christianson; Ian D Krantz; David R Fitzpatrick; Matthew A Deardorff
Journal:  Hum Mol Genet       Date:  2014-01-08       Impact factor: 5.121

9.  The functional interactome landscape of the human histone deacetylase family.

Authors:  Preeti Joshi; Todd M Greco; Amanda J Guise; Yang Luo; Fang Yu; Alexey I Nesvizhskii; Ileana M Cristea
Journal:  Mol Syst Biol       Date:  2013       Impact factor: 11.429

10.  Compromised structure and function of HDAC8 mutants identified in Cornelia de Lange Syndrome spectrum disorders.

Authors:  Christophe Decroos; Christine M Bowman; Joe-Ann S Moser; Karen E Christianson; Matthew A Deardorff; David W Christianson
Journal:  ACS Chem Biol       Date:  2014-07-30       Impact factor: 5.100
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  12 in total

Review 1.  A Genetically Encoded, Phage-Displayed Cyclic-Peptide Library.

Authors:  Xiaoshan Shayna Wang; Peng-Hsun Chase Chen; J Trae Hampton; Jeffery M Tharp; Catrina A Reed; Sukant K Das; Duen-Shian Wang; Hamed S Hayatshahi; Yang Shen; Jin Liu; Wenshe Ray Liu
Journal:  Angew Chem Int Ed Engl       Date:  2019-09-09       Impact factor: 15.336

2.  Structure-based design generated novel hydroxamic acid based preferential HDAC6 lead inhibitor with on-target cytotoxic activity against primary choroid plexus carcinoma.

Authors:  Shaymaa E Kassab; Samar Mowafy; Aya M Alserw; Joustin A Seliem; Shahenda M El-Naggar; Nesreen N Omar; Mohamed M Awad
Journal:  J Enzyme Inhib Med Chem       Date:  2019-12       Impact factor: 5.051

3.  Selective inhibition of histone deacetylase 8 improves vascular hypertrophy, relaxation, and inflammation in angiotensin II hypertensive mice.

Authors:  Hae Jin Kee; Yuhee Ryu; Young Mi Seok; Sin Young Choi; Simei Sun; Gwi Ran Kim; Myung Ho Jeong
Journal:  Clin Hypertens       Date:  2019-06-15

4.  Chemical genomics reveals histone deacetylases are required for core regulatory transcription.

Authors:  Berkley E Gryder; Lei Wu; Girma M Woldemichael; Silvia Pomella; Taylor R Quinn; Paul M C Park; Abigail Cleveland; Benjamin Z Stanton; Young Song; Rossella Rota; Olaf Wiest; Marielle E Yohe; Jack F Shern; Jun Qi; Javed Khan
Journal:  Nat Commun       Date:  2019-07-08       Impact factor: 14.919

5.  Design and synthesis of diazine-based panobinostat analogues for HDAC8 inhibition.

Authors:  Sivaraman Balasubramaniam; Sajith Vijayan; Liam V Goldman; Xavier A May; Kyra Dodson; Sweta Adhikari; Fatima Rivas; Davita L Watkins; Shana V Stoddard
Journal:  Beilstein J Org Chem       Date:  2020-04-07       Impact factor: 2.883

Review 6.  Histone Deacetylase Inhibitors as Therapeutic Interventions on Cervical Cancer Induced by Human Papillomavirus.

Authors:  Natália Lourenço de Freitas; Maria Gabriela Deberaldini; Diana Gomes; Aline Renata Pavan; Ângela Sousa; Jean Leandro Dos Santos; Christiane P Soares
Journal:  Front Cell Dev Biol       Date:  2021-01-28

Review 7.  Next-generation of selective histone deacetylase inhibitors.

Authors:  Feifei Yang; Na Zhao; Di Ge; Yihua Chen
Journal:  RSC Adv       Date:  2019-06-24       Impact factor: 4.036

8.  Design, Synthesis and Biological Characterization of Histone Deacetylase 8 (HDAC8) Proteolysis Targeting Chimeras (PROTACs) with Anti-Neuroblastoma Activity.

Authors:  Salma Darwish; Ehab Ghazy; Tino Heimburg; Daniel Herp; Patrik Zeyen; Rabia Salem-Altintas; Johannes Ridinger; Dina Robaa; Karin Schmidtkunz; Frank Erdmann; Matthias Schmidt; Christophe Romier; Manfred Jung; Ina Oehme; Wolfgang Sippl
Journal:  Int J Mol Sci       Date:  2022-07-07       Impact factor: 6.208

9.  HDAC8 affects MGMT levels in glioblastoma cell lines via interaction with the proteasome receptor ADRM1.

Authors:  Irene Santos-Barriopedro; Yixuan Li; Sonali Bahl; Edward Seto
Journal:  Genes Cancer       Date:  2019

Review 10.  The Roles of Histone Deacetylases and Their Inhibitors in Cancer Therapy.

Authors:  Guo Li; Yuan Tian; Wei-Guo Zhu
Journal:  Front Cell Dev Biol       Date:  2020-09-29
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