Skip to main content
U.S. Department of Energy
Office of Scientific and Technical Information

Discovery of Dual TAF1-ATR Inhibitors and Ligand-Induced Structural Changes of the TAF1 Tandem Bromo

Journal Article · · J. Med. Chem.

Research Organization:
Advanced Photon Source (APS), Argonne National Laboratory (ANL), Argonne, IL (US)
Sponsoring Organization:
DOE - Office Of Science; INDUSTRY
OSTI ID:
1871740
Journal Information:
J. Med. Chem., Journal Name: J. Med. Chem. Journal Issue: (5) Vol. 65
Country of Publication:
United States
Language:
ENGLISH

References (64)

Towards a mechanistic understanding of core promoter recognition from cryo-EM studies of human TFIID journal December 2017
Discovery of AZD3147: A Potent, Selective Dual Inhibitor of mTORC1 and mTORC2 journal February 2015
Structural Basis of Inhibitor Selectivity in the BRD7/9 Subfamily of Bromodomains journal February 2020
Design of thienopyranone-based BET inhibitors that bind multiple synthetic lethality targets journal July 2020
Differential BET Bromodomain Inhibition by Dihydropteridinone and Pyrimidodiazepinone Kinase Inhibitors journal October 2021
The Commonly Used PI3-Kinase Probe LY294002 Is an Inhibitor of BET Bromodomains journal December 2013
X-ray solution scattering (SAXS) combined with crystallography and computation: defining accurate macromolecular structures, conformations and assemblies in solution journal August 2007
Histone Recognition and Large-Scale Structural Analysis of the Human Bromodomain Family journal March 2012
Structure of the histone chaperone CIA/ASF1–double bromodomain complex linking histone modifications and site-specific histone eviction journal April 2010
Functional substitution for TAFII250 by a retroposed homolog that is expressed in human spermatogenesis journal September 2002
Features and development of Coot journal March 2010
Benzoisoquinolinediones as Potent and Selective Inhibitors of BRPF2 and TAF1/TAF1L Bromodomains journal May 2017
The mutational landscape of endometrial cancer journal February 2015
Mapping the chemical chromatin reactivation landscape identifies BRD4-TAF1 cross-talk journal May 2016
Integration, scaling, space-group assignment and post-refinement journal January 2010
Defect in the p53-Mdm2 Autoregulatory Loop Resulting from Inactivation of TAF II 250 in Cell Cycle Mutant tsBN462 Cells journal August 2000
Structural Insights into the Eukaryotic Transcription Initiation Machinery journal May 2017
BET Bromodomain Proteins Function as Master Transcription Elongation Factors Independent of CDK9 Recruitment journal July 2017
Dual Inhibition of TAF1 and BET Bromodomains from the BI-2536 Kinase Inhibitor Scaffold journal September 2019
A triple action CDK4/6-PI3K-BET inhibitor with augmented cancer cell cytotoxicity journal July 2020
Phosphorylation of p53 by TAF1 Inactivates p53-Dependent Transcription in the DNA Damage Response journal January 2014
Phase II study of ceralasertib (AZD6738) in combination with durvalumab in patients with advanced/metastatic melanoma who have failed prior anti-PD-1 therapy journal February 2022
Transcriptional Addiction in Cancer journal February 2017
GNE-371, a Potent and Selective Chemical Probe for the Second Bromodomains of Human Transcription-Initiation-Factor TFIID Subunit 1 and Transcription-Initiation-Factor TFIID Subunit 1-like journal October 2018
TAF1 plays a critical role in AML1-ETO driven leukemogenesis journal October 2019
Structural and functional insight into TAF1–TAF7, a subcomplex of transcription factor II D journal June 2014
Dual-activity PI3K–BRD4 inhibitor for the orthogonal inhibition of MYC to block tumor growth and metastasis journal January 2017
Design of a Chemical Probe for the Bromodomain and Plant Homeodomain Finger-Containing (BRPF) Family of Proteins journal August 2017
The Novel ATR Inhibitor BAY 1895344 Is Efficacious as Monotherapy and Combined with DNA Damage–Inducing or Repair–Compromising Therapies in Preclinical Cancer Models journal October 2019
Asymmetric Synthesis of Chiral Sulfoximines through the S‐Alkylation of Sulfinamides journal December 2019
CRYSOL – a Program to Evaluate X-ray Solution Scattering of Biological Macromolecules from Atomic Coordinates journal December 1995
Promiscuous targeting of bromodomains by bromosporine identifies BET proteins as master regulators of primary transcription response in leukemia journal October 2016
Determination of the regularization parameter in indirect-transform methods using perceptual criteria journal August 1992
Activation of a DNA Damage Checkpoint Response in a TAF1-Defective Cell Line journal June 2004
Multiple direct interactions of TBP with the MYC oncoprotein journal November 2019
DIALS : implementation and evaluation of a new integration package journal February 2018
Dual kinase-bromodomain inhibitors for rationally designed polypharmacology journal March 2014
Modeling of loops in protein structures journal January 2000
Accurate assessment of mass, models and resolution by small-angle scattering journal April 2013
Transcription factor TAFII250 promotes Mdm2-dependent turnover of p53 journal January 2007
SAXSMoW 2.0: Online calculator of the molecular weight of proteins in dilute solution from experimental SAXS data measured on a relative scale journal December 2018
BI 2536, a Potent and Selective Inhibitor of Polo-like Kinase 1, Inhibits Tumor Growth In Vivo journal February 2007
An Acetylation Switch in p53 Mediates Holo-TFIID Recruitment journal November 2007
UCSF Chimera?A visualization system for exploratory research and analysis journal January 2004
ATSAS 2.8 : a comprehensive data analysis suite for small-angle scattering from macromolecular solutions journal June 2017
BioXTAS RAW : improvements to a free open-source program for small-angle X-ray scattering data reduction and analysis journal September 2017
Discovery and Characterization of AZD6738, a Potent Inhibitor of Ataxia Telangiectasia Mutated and Rad3 Related (ATR) Kinase with Application as an Anticancer Agent journal October 2018
Diving into the Water: Inducible Binding Conformations for BRD4, TAF1(2), BRD9, and CECR2 Bromodomains journal May 2016
phenix.model_vs_data : a high-level tool for the calculation of crystallographic model and data statistics journal May 2010
Quantitative Characterization of Bivalent Probes for a Dual Bromodomain Protein, Transcription Initiation Factor TFIID Subunit 1 journal March 2018
Crystal structure of a TAF1-TAF7 complex in human transcription factor IID reveals a promoter binding module journal November 2014
Rapid measurement of binding constants and heats of binding using a new titration calorimeter journal May 1989
Inhibition of Thr-55 phosphorylation restores p53 nuclear localization and sensitizes cancer cells to DNA damage journal November 2008
How good are my data and what is the resolution? journal June 2013
Ab initio electron density determination directly from solution scattering data journal January 2018
Acetyl-lysine Binding Site of Bromodomain-Containing Protein 4 (BRD4) Interacts with Diverse Kinase Inhibitors journal March 2014
Drugging ATR: progress in the development of specific inhibitors for the treatment of cancer journal June 2015
Concise and modular synthesis of regioisomeric haptens for the production of high-affinity and stereoselective antibodies to the strobilurin azoxystrobin journal January 2011
Restoring Low Resolution Structure of Biological Macromolecules from Solution Scattering Using Simulated Annealing journal June 1999
A TFIID-SAGA Perturbation that Targets MYB and Suppresses Acute Myeloid Leukemia journal January 2018
Rationally Designed PI3Kα Mutants to Mimic ATR and Their Use to Understand Binding Specificity of ATR Inhibitors journal June 2017
Structure and Function of a Human TAF II 250 Double Bromodomain Module journal May 2000
Stereospecific α-(hetero)arylation of sulfoximines and sulfonimidamides journal January 2022
Evolving SAXS versatility: solution X-ray scattering for macromolecular architecture, functional landscapes, and integrative structural biology journal October 2019

Similar Records

Discovery of Dual TAF1-ATR Inhibitors and Ligand-Induced Structural Changes of the TAF1 Tandem Bromo
Journal Article · 2022 · J. Med. Chem. · OSTI ID:1856385

Dual Inhibition of TAF1 and BET Bromodomains from the BI-2536 Kinase Inhibitor Scaffold
Journal Article · 2019 · ACS Medicinal Chemistry Letters · OSTI ID:1576009

Discovery of a BTK/MNK dual inhibitor for lymphoma and leukemia
Journal Article · 2016 · Leukemia · OSTI ID:1234758

Related Subjects