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Benzoisoquinolinediones as Potent and Selective Inhibitors of BRPF2 and TAF1/TAF1L Bromodomains

forfatter

Léa Bouché

Amaury E Fernández-Montalván

Kilian Huber

Cynthia Tallant

udgivet i: Journal of Medicinal Chemistry

dato for udgivelse: 2017-05-01

sprog: engelsk

Cites articles 70

Date

Titel

Forfattere

2017-01-09

Design of a Biased Potent Small Molecule Inhibitor of the Bromodomain and PHD Finger-Containing (BRPF) Proteins Suitable for Cellular and in Vivo Studies

Pavel Savitsky, David Michael Andrews, Susanne Müller, Paul E Brennan, Tim C P Somervaille, Cynthia Tallant
2016-09-28

Discovery of a Potent and Selective in Vivo Probe (GNE-272) for the Bromodomains of CBP/EP300

F. Anthony Romero, Andrew R Conery, James R Kiefer, Andrea Cochran, Ivana Yen
2016-09-27

Development of Selective CBP/P300 Benzoxazepine Bromodomain Inhibitors

Paul E Brennan, Stefan Knapp, Cynthia Tallant
2016-10-13

Discovery and Optimization of a Selective Ligand for the Switch/Sucrose Nonfermenting-Related Bromodomains of Polybromo Protein-1 by the Use of Virtual Screening and Hydration Analysis

Panagis Filippakopoulos, Vassilios Myrianthopoulos, David Heidenreich, Efstathios Kastritis, Jessica A Downs, Stefan Knapp, Emmanuel Mikros, Alexios-Leandros Skaltsounis, Cynthia Tallant, Catherine Rogers
2016-09-01

Discovery of a Potent, Selective, and Cell-Active Dual Inhibitor of Protein Arginine Methyltransferase 4 and Protein Arginine Methyltransferase 6.

David Smil, Cheryl Arrowsmith, Dalia Barsyte-Lovejoy, Magdalena M. Szewczyk, Jing Liu
2016-05-09

GSK6853, a Chemical Probe for Inhibition of the BRPF1 Bromodomain

Isabelle Becher, David J Fallon, Chun-Wa Chung
2016-06-10

Clinical progress and pharmacology of small molecule bromodomain inhibitors

Nicholas C.O. Tomkinson
2016-05-31

Diving into the Water: Inducible Binding Conformations for BRD4, TAF1(2), BRD9, and CECR2 Bromodomains

James R Kiefer, F. Anthony Romero, Andrea Cochran
2016-05-09

Mapping the chemical chromatin reactivation landscape identifies BRD4-TAF1 cross-talk

Giulio Superti-Furga, Christoph Bock, Stefan Kubicek, Johannes Zuber, Susanne Müller, Stefan Knapp, Cynthia Tallant, Kilian Huber, Freya Klepsch, Charles-Hugues Claude Jean Lardeau
2016-05-26

Discovery and Characterization of a Highly Potent and Selective Aminopyrazoline-Based in Vivo Probe (BAY-598) for the Protein Lysine Methyltransferase SMYD2

Antonius Ter Laak, Amaury E Fernández-Montalván, Peter J. Brown, Cheryl Arrowsmith, Carlo Stresemann, Magdalena M. Szewczyk
2016-03-31

Structure of promoter-bound TFIID and model of human pre-initiation complex assembly

Eva Nogales, Pablo Chacón
2016-05-26

Structure-Based Design of an in Vivo Active Selective BRD9 Inhibitor

Susanne Müller, Stefan Knapp, Cynthia Tallant
2016-02-15

Evidence of TAF1 dysfunction in peripheral models of X-linked dystonia-parkinsonism

Aloysius Domingo, Roland Dominic Jamora, Uwe Walter, Ron Shamir, Ana Westenberger, Katja Lohmann, Christine Klein
2016-01-22

Targeting epigenetic regulators for cancer therapy: modulation of bromodomain proteins, methyltransferases, demethylases, and microRNAs
2016-02-25

Discovery of I-BRD9, a Selective Cell Active Chemical Probe for Bromodomain Containing Protein 9 Inhibition

Gerard Drewes, Tony Kouzarides, Anne-Marie Michon, Paola Grandi, David Drewry, Antje Dittmann, Isabelle Becher, Andrew Bannister, Rab K Prinjha, Ka Hing Che
2016-05-30

The BRPF2/BRD1-MOZ complex is involved in retinoic acid-induced differentiation of embryonic stem cells.
2015-12-18

Bromodomains: Structure, function and pharmacology of inhibition
2015-12-16

The Chromatin Regulator BRPF3 Preferentially Activates the HBO1 Acetyltransferase but Is Dispensable for Mouse Development and Survival

Linya You, Dengshun Miao, Cindy Degerny
2015-12-03

TAF1 Variants Are Associated with Dysmorphic Features, Intellectual Disability, and Neurological Manifestations

Laurence Faivre, Tjitske Kleefstra, Carmen Orellana, Silvestre Oltra, Maria Tzetis, Francisco Martinez, Carlos E Prada, David A. Mittelman, Gareth Highnam, Sandra Monfort, Alfonso Caro-Llopis, Kay Metcalfe, A. Micheil Innes, Jillian S Parboosingh
2015-11-24

A Potent, Selective, and Cell-Active Inhibitor of Human Type I Protein Arginine Methyltransferases

Peter J. Brown, Cheryl Arrowsmith, Dalia Barsyte-Lovejoy, Jing Liu, Magdalena M. Szewczyk
2015-11-17

OPLS3: A Force Field Providing Broad Coverage of Drug-like Small Molecules and Proteins

William L. Jorgensen
2015-12-01

Disrupting Acetyl-Lysine Recognition: Progress in the Development of Bromodomain Inhibitors

F. Anthony Romero
2015-09-23

Open access chemical probes for epigenetic targets

Peter J. Brown, Susanne Müller
2015-07-01

The promise and peril of chemical probes

Cheryl Arrowsmith, Jonathan B Baell, Paul E Brennan, Peter J. Brown, Aled Edwards, Kilian Huber, Stefan Knapp, John P. Overington, Michael A Walters, Robert N Young, Nathanael Gray, Adrian J Carter, Jayme L Dahlin, Susanne Müller, Stuart Schreiber, Leticia Toledo-Sherman, Timothy M Willson
2015-01-01

Targeting BET bromodomains for cancer treatment

Amaury E Fernández-Montalván
2015-06-10

Structure-Guided Design of IACS-9571, a Selective High-Affinity Dual TRIM24-BRPF1 Bromodomain Inhibitor

Jannik N Andersen, Michelle Craig Barton, Carlo Toniatti, Giulio F Draetta
2015-05-25

NanoBRET--A Novel BRET Platform for the Analysis of Protein-Protein Interactions
2015-05-14

Discovery of a Chemical Tool Inhibitor Targeting the Bromodomains of TRIM24 and BRPF.

Pavel Savitsky, Susanne Müller, Stefan Knapp, Paul E Brennan, Cynthia Tallant
2015-05-11

Discovery of cancer drug targets by CRISPR-Cas9 screening of protein domains

Justin B Kinney
2015-03-15

The chromatin regulator Brpf1 regulates embryo development and cell proliferation

Linya You
2014-12-16

Best of both worlds: combining pharma data and state of the art modeling technology to improve in Silico pKa prediction

Andreas H Göller, Robert D. Clark
2014-09-10

1,3-Dimethyl Benzimidazolones Are Potent, Selective Inhibitors of the BRPF1 Bromodomain

Anne-Marie Michon, Paola Grandi, Chun-Wa Chung

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