Literature DB >> 32551019

Discovery of CPI-1612: A Potent, Selective, and Orally Bioavailable EP300/CBP Histone Acetyltransferase Inhibitor.

Jonathan E Wilson1, Gaurav Patel2, Chirag Patel2, Francois Brucelle1, Annissa Huhn1, Anna S Gardberg1, Florence Poy1, Nico Cantone1, Archana Bommi-Reddy1, Robert J Sims1, Richard T Cummings1, Julian R Levell1.   

Abstract

The histone acetyltransferases, CREB binding protein (CBP) and EP300, are master transcriptional co-regulators that have been implicated in numerous diseases, such as cancer, inflammatory disorders, and neurodegeneration. A novel, highly potent, orally bioavailable EP300/CBP histone acetyltransferase (HAT) inhibitor, CPI-1612 or 17, was developed from the lead compound 3. Replacement of the indole scaffold of 3 with the aminopyridine scaffold of 17 led to improvements in potency, solubility, and bioavailability. These characteristics resulted in a 20-fold lower efficacious dose for 17 relative to lead 3 in a JEKO-1 tumor mouse xenograft study.
Copyright © 2020 American Chemical Society.

Entities:  

Year:  2020        PMID： 32551019      PMCID： PMC7294707          DOI： 10.1021/acsmedchemlett.0c00155

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


  12 in total

Review 1.  Protein lysine acetylation by p300/CBP.

Authors:  Beverley M Dancy; Philip A Cole
Journal:  Chem Rev       Date:  2015-01-16       Impact factor: 60.622

2.  Gene dosage-dependent embryonic development and proliferation defects in mice lacking the transcriptional integrator p300.

Authors:  T P Yao; S P Oh; M Fuchs; N D Zhou; L E Ch'ng; D Newsome; R T Bronson; E Li; D M Livingston; R Eckner
Journal:  Cell       Date:  1998-05-01       Impact factor: 41.582

3.  Abnormal skeletal patterning in embryos lacking a single Cbp allele: a partial similarity with Rubinstein-Taybi syndrome.

Authors:  Y Tanaka; I Naruse; T Maekawa; H Masuya; T Shiroishi; S Ishii
Journal:  Proc Natl Acad Sci U S A       Date:  1997-09-16       Impact factor: 11.205

4.  Early Drug-Discovery Efforts towards the Identification of EP300/CBP Histone Acetyltransferase (HAT) Inhibitors.

Authors:  Annissa J Huhn; Anna S Gardberg; Florence Poy; Francois Brucelle; Valerie Vivat; Nico Cantone; Gaurav Patel; Chirag Patel; Richard Cummings; Robert Sims; Julian Levell; James E Audia; Archana Bommi-Reddy; Jonathan E Wilson
Journal:  ChemMedChem       Date:  2020-04-06       Impact factor: 3.466

5.  Discovery of a selective catalytic p300/CBP inhibitor that targets lineage-specific tumours.

Authors:  Loren M Lasko; Clarissa G Jakob; Rohinton P Edalji; Wei Qiu; Debra Montgomery; Enrico L Digiammarino; T Matt Hansen; Roberto M Risi; Robin Frey; Vlasios Manaves; Bailin Shaw; Mikkel Algire; Paul Hessler; Lloyd T Lam; Tamar Uziel; Emily Faivre; Debra Ferguson; Fritz G Buchanan; Ruth L Martin; Maricel Torrent; Gary G Chiang; Kannan Karukurichi; J William Langston; Brian T Weinert; Chunaram Choudhary; Peter de Vries; John H Van Drie; David McElligott; Ed Kesicki; Ronen Marmorstein; Chaohong Sun; Philip A Cole; Saul H Rosenberg; Michael R Michaelides; Albert Lai; Kenneth D Bromberg
Journal:  Nature       Date:  2017-09-27       Impact factor: 49.962

Review 6.  Exploitation of EP300 and CREBBP Lysine Acetyltransferases by Cancer.

Authors:  Narsis Attar; Siavash K Kurdistani
Journal:  Cold Spring Harb Perspect Med       Date:  2017-03-01       Impact factor: 6.915

Review 7.  Histone acetyltransferases are crucial regulators in NF-κB mediated inflammation.

Authors:  Massimo Ghizzoni; Hidde J Haisma; Harm Maarsingh; Frank J Dekker
Journal:  Drug Discov Today       Date:  2011-04-06       Impact factor: 7.851

Review 8.  KATs in cancer: functions and therapies.

Authors:  A Farria; W Li; S Y R Dent
Journal:  Oncogene       Date:  2015-02-09       Impact factor: 9.867

Review 9.  Lysine acetyltransferases CBP and p300 as therapeutic targets in cognitive and neurodegenerative disorders.

Authors:  Luis M Valor; Jose Viosca; Jose P Lopez-Atalaya; Angel Barco
Journal:  Curr Pharm Des       Date:  2013       Impact factor: 3.116

10.  Discovery of Spiro Oxazolidinediones as Selective, Orally Bioavailable Inhibitors of p300/CBP Histone Acetyltransferases.

Authors:  Michael R Michaelides; Arthur Kluge; Michael Patane; John H Van Drie; Ce Wang; T Matthew Hansen; Roberto M Risi; Robert Mantei; Carmen Hertel; Kannan Karukurichi; Alexandre Nesterov; David McElligott; Peter de Vries; J William Langston; Philip A Cole; Ronen Marmorstein; Hong Liu; Loren Lasko; Kenneth D Bromberg; Albert Lai; Edward A Kesicki
Journal:  ACS Med Chem Lett       Date:  2017-12-13       Impact factor: 4.345
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  7 in total

1.  RBBP4-p300 axis modulates expression of genes essential for cell survival and is a potential target for therapy in glioblastoma.

Authors:  Ann C Mladek; Huihuang Yan; Shulan Tian; Paul A Decker; Danielle M Burgenske; Katrina Bakken; Zeng Hu; Lihong He; Margaret A Connors; Brett L Carlson; Jonathan Wilson; Archana Bommi-Reddy; Andy Conery; Jeanette E Eckel-Passow; Jann N Sarkaria; Gaspar J Kitange
Journal:  Neuro Oncol       Date:  2022-08-01       Impact factor: 13.029

2.  Harnessing Ionic Selectivity in Acetyltransferase Chemoproteomic Probes.

Authors:  Yihang Jing; Jose L Montano; Michaella Levy; Jeffrey E Lopez; Pei-Pei Kung; Paul Richardson; Krzysztof Krajewski; Laurence Florens; Michael P Washburn; Jordan L Meier
Journal:  ACS Chem Biol       Date:  2020-12-29       Impact factor: 5.100

Review 3.  Small molecule targeting of chromatin writers in cancer.

Authors:  Andrew R Conery; Jennifer L Rocnik; Patrick Trojer
Journal:  Nat Chem Biol       Date:  2021-12-24       Impact factor: 15.040

4.  CREBBP/EP300 acetyltransferase inhibition disrupts FOXA1-bound enhancers to inhibit the proliferation of ER+ breast cancer cells.

Authors:  Archana Bommi-Reddy; Sungmi Park-Chouinard; David N Mayhew; Esteban Terzo; Aparna Hingway; Michael J Steinbaugh; Jonathan E Wilson; Robert J Sims; Andrew R Conery
Journal:  PLoS One       Date:  2022-03-30       Impact factor: 3.240

5.  Identification of a BAZ2A-Bromodomain Hit Compound by Fragment Growing.

Authors:  Andrea Dalle Vedove; Giulia Cazzanelli; Laurent Batiste; Jean-Rémy Marchand; Dimitrios Spiliotopoulos; Jessica Corsi; Vito Giuseppe D'Agostino; Amedeo Caflisch; Graziano Lolli
Journal:  ACS Med Chem Lett       Date:  2022-08-03       Impact factor: 4.632

6.  Synthesis and Biological Evaluation of Spirocyclic Chromane Derivatives as a Potential Treatment of Prostate Cancer.

Authors:  Li Feng; Shujia Yu; Hai Wang; Shengwei Yang; Xue Li; Hongjuan Dai; Liwen Zhao; Cheng Jiang; Yazhou Wang
Journal:  Molecules       Date:  2021-05-25       Impact factor: 4.411

7.  Mechanistic insights into p53-regulated cytotoxicity of combined entinostat and irinotecan against colorectal cancer cells.

Authors:  Christian Marx; Jürgen Sonnemann; Mandy Beyer; Oliver D K Maddocks; Sergio Lilla; Irene Hauzenberger; Andrea Piée-Staffa; Kanstantsin Siniuk; Suneetha Nunna; Lisa Marx-Blümel; Martin Westermann; Tobias Wagner; Felix B Meyer; René Thierbach; Christina S Mullins; Said Kdimati; Michael Linnebacher; Francesco Neri; Thorsten Heinzel; Zhao-Qi Wang; Oliver H Krämer
Journal:  Mol Oncol       Date:  2021-07-29       Impact factor: 6.603
  7 in total

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