B. Albrecht

发表

Fragment-Based Discovery of a Selective and Cell-Active Benzodiazepinone CBP/EP300 Bromodomain Inhibitor (CPI-637).

Y. Leblanc, H. Jayaram, R. Sims, 2016, ACS medicinal chemistry letters.

Development of methyl isoxazoleazepines as inhibitors of BET.

R. Cummings, P. Sandy, Y. Leblanc, 2015, Bioorganic & medicinal chemistry letters.

Discovery and optimization of triazolopyridazines as potent and selective inhibitors of the c-Met kinase.

K. Rex, K. Shah, Douglas Hoffman, 2008, Journal of medicinal chemistry.

Discovery and optimization of potent and selective triazolopyridazine series of c-Met inhibitors.

K. Rex, K. Shah, S. Bellon, 2009, Bioorganic & medicinal chemistry letters.

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.

H. Jayaram, F. A. Romero, R. Cummings, 2018, Journal of medicinal chemistry.

Inhibition of bromodomain-containing protein 9 for the prevention of epigenetically-defined drug resistance.

D. Stokoe, P. Sandy, Steffan Vartanian, 2017, Bioorganic & medicinal chemistry letters.

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

Andrew C Good, Vickie Tsui, Jian Wang, 2016, Journal of medicinal chemistry.

Discovery and optimization of a novel series of N-arylamide oxadiazoles as potent, highly selective and orally bioavailable cannabinoid receptor 2 (CB2) agonists.

S. Hitchcock, Xiaoyang Xia, Yuan Cheng, 2008, Journal of Medicinal Chemistry.

A concise, total synthesis of the TMC-95A/B proteasome inhibitors.

Robert M. Williams, B. Albrecht, 2004, Proceedings of the National Academy of Sciences of the United States of America.

Identification of a Benzoisoxazoloazepine Inhibitor (CPI-0610) of the Bromodomain and Extra-Terminal (BET) Family as a Candidate for Human Clinical Trials.

P. Sandy, Y. Leblanc, H. Jayaram, 2016, Journal of medicinal chemistry.

Identification of a novel glutathione conjugate of diclofenac by LTQ-Orbitrap.

B. Albrecht, Y. Teffera, Zhiyang Zhao, 2008, Drug metabolism letters.

A practical synthesis of indoles via a Pd-catalyzed C-N ring formation.

Y. Leblanc, Alexander M. Taylor, A. Côté, 2014, Organic letters.

Antiinflammatory effects of bromodomain and extraterminal domain inhibition in cystic fibrosis lung inflammation.

Wei Chen, S. Wenzel, M. Myerburg, 2016, JCI insight.

Discovery and Optimization of Tetramethylpiperidinyl Benzamides as Inhibitors of EZH2.

P. Trojer, R. Cummings, L. Bergeron, 2014, ACS medicinal chemistry letters.

Synthesis and activity of substituted carbamates as potentiators of the alpha4beta2 nicotinic acetylcholine receptor.

A. Malmberg, K. Clarkin, S. McDonough, 2008, Bioorganic & medicinal chemistry letters.

GNE-064: A Potent, Selective, and Orally Bioavailable Chemical Probe for the Bromodomains of SMARCA2 and SMARCA4 and the Fifth Bromodomain of PBRM1.

A. Good, P. Sandy, Y. Leblanc, 2022, Journal of medicinal chemistry.

GNE-886: A Potent and Selective Inhibitor of the Cat Eye Syndrome Chromosome Region Candidate 2 Bromodomain (CECR2).

P. Sandy, H. Jayaram, R. Sims, 2017, ACS medicinal chemistry letters.

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

Karen E Gascoigne, Fei Wang, S. Kharbanda, 2016, Journal of medicinal chemistry.

Identification of (R)-N-((4-Methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)-1H-indole-3-carboxamide (CPI-1205), a Potent and Selective Inhibitor of Histone Methyltransferase EZH2, Suitable for Phase I Clinical Trials for B-Cell Lymp

Jon R. Wilson, A. Good, P. Trojer, 2016, Journal of medicinal chemistry.

Chemical reactivity of methoxy 4-o-aryl quinolines: identification of glutathione displacement products in vitro and in vivo.

B. Albrecht, J. Harmange, Y. Teffera, 2008, Chemical research in toxicology.

BRD4 is an atypical kinase that phosphorylates Serine2 of the RNA Polymerase II carboxy-terminal domain

B. N. Devaiah, D. Singer, K. Ozato, 2012, Proceedings of the National Academy of Sciences.

Discovery and optimization of substituted piperidines as potent, selective, CNS-penetrant alpha4beta2 nicotinic acetylcholine receptor potentiators.

A. Malmberg, K. Clarkin, S. McDonough, 2008, Bioorganic & Medicinal Chemistry Letters.

Discovery, Design, and Optimization of Isoxazole Azepine BET Inhibitors.

P. Sandy, Y. Leblanc, H. Jayaram, 2013, ACS medicinal chemistry letters.

S(+)-4-(1-Phenylethylamino)quinazolines as inhibitors of human immunoglobulin E synthesis: potency is dictated by stereochemistry and atomic point charges at N-1.

P. Ettmayer, A. Bérces, B. Albrecht, 2001, Journal of medicinal chemistry.

A concise formal total synthesis of TMC-95A/B proteasome inhibitors.

Robert M. Williams, B. Albrecht, 2003, Organic letters.

Asymmetric synthesis of (+)-hypusine.

R. Williams, B. Albrecht, D. Demong, 2001, Organic letters.

Discovery of Benzotriazolo[4,3-d][1,4]diazepines as Orally Active Inhibitors of BET Bromodomains.

P. Sandy, Y. Leblanc, H. Jayaram, 2016, ACS medicinal chemistry letters.

Pharmacological effects of nonselective and subtype-selective nicotinic acetylcholine receptor agonists in animal models of persistent pain

A. Malmberg, K. Clarkin, T. Juan, 2010, PAIN®.

An Indexed Combinatorial Library: The Synthesis and Testing of Insect Repellents

B. Albrecht, K. Gelato, W. Miles, 2001 .

Identification of potent, selective KDM5 inhibitors.

P. Trojer, P. Sandy, Y. Leblanc, 2016, Bioorganic & medicinal chemistry letters.

An inhibitor of KDM5 demethylases reduces survival of drug-tolerant cancer cells.

P. Trojer, E. Jackson, D. Arnott, 2016, Nature chemical biology.

EZH2 inhibitor efficacy in non-Hodgkin's lymphoma does not require suppression of H3K27 monomethylation.

P. Trojer, Shilpi Arora, R. Cummings, 2014, Chemistry & biology.

Synthesis, structural analysis, and SAR studies of triazine derivatives as potent, selective Tie-2 inhibitors.

P. Gallant, M. Morrison, P. Rose, 2007, Bioorganic & medicinal chemistry letters.

Identification of EZH2 and EZH1 small molecule inhibitors with selective impact on diffuse large B cell lymphoma cell growth.

E. Chan, P. Trojer, P. Sandy, 2013, Chemistry & biology.

Regulatory T Cell Modulation by CBP/EP300 Bromodomain Inhibition*

G. Hatzivassiliou, P. Sandy, H. Jayaram, 2016, The Journal of Biological Chemistry.

Entry into the bi-aryl moiety of the TMC-95 proteasome inhibitors via the Stille protocol

Robert M. Williams, B. Albrecht, 2001 .

Evolution of a highly selective and potent 2-(pyridin-2-yl)-1,3,5-triazine Tie-2 kinase inhibitor.

Richard Kendall, P. Gallant, M. Morrison, 2007, Journal of medicinal chemistry.

GNE-781, A Highly Advanced Potent and Selective Bromodomain Inhibitor of Cyclic Adenosine Monophosphate Response Element Binding Protein, Binding Protein (CBP).

Karen E Gascoigne, Y. Ran, G. Hatzivassiliou, 2017, Journal of medicinal chemistry.

A Potent and Orally Efficacious, Hydroxyethylamine-Based Inhibitor of β-Secretase.

Yuan Cheng, Yi Luo, Wenge Zhong, 2012, ACS medicinal chemistry letters.

Discovery, design, and synthesis of indole-based EZH2 inhibitors.

A. Good, P. Trojer, R. Cummings, 2015, Bioorganic & medicinal chemistry letters.

Design and Synthesis of Styrenylcyclopropylamine LSD1 Inhibitors.

A. Good, P. Trojer, R. Cummings, 2020, ACS medicinal chemistry letters.

Discovery of potent and selective 8-fluorotriazolopyridine c-Met inhibitors.

K. Rex, D. Whittington, S. Bellon, 2015, Journal of medicinal chemistry.

Discovery and optimization of a potent and selective triazolopyridinone series of c-Met inhibitors.

K. Rex, D. Whittington, S. Bellon, 2012, Bioorganic & Medicinal Chemistry Letters.

Alkynylpyrimidine amide derivatives as potent, selective, and orally active inhibitors of Tie-2 kinase.

David Powers, Paul Hughes, Richard Kendall, 2007, Journal of medicinal chemistry.