V. Tsui

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.

Lead optimization of a 4-aminopyridine benzamide scaffold to identify potent, selective, and orally bioavailable TYK2 inhibitors.

Adam R. Johnson, Jun Liang, J. DeVoss, 2013, Journal of medicinal chemistry.

Lead identification of novel and selective TYK2 inhibitors.

Adam R. Johnson, Jun Liang, M. Ultsch, 2013, European journal of medicinal chemistry.

A new regulatory switch in a JAK protein kinase

Charles Eigenbrot, Vickie Tsui, Paul Gibbons, 2011, Proteins.

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 of a potent, selective, and orally available class I phosphatidylinositol 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) kinase inhibitor (GDC-0980) for the treatment of cancer.

BinQing Wei, D. Sutherlin, L. Friedman, 2011, Journal of medicinal chemistry.

Discovery of (thienopyrimidin-2-yl)aminopyrimidines as potent, selective, and orally available pan-PI3-kinase and dual pan-PI3-kinase/mTOR inhibitors for the treatment of cancer.

D. Sutherlin, S. Sideris, L. Friedman, 2010, Journal of medicinal chemistry.

A Unique Approach to Design Potent and Selective Cyclic Adenosine Monophosphate Response Element Binding Protein, Binding Protein (CBP) Inhibitors.

Fei Wang, H. Jayaram, F. A. Romero, 2017, Journal of medicinal chemistry.

Optimization of Pan-Pim Kinase Activity and Oral Bioavailability Leading to Diaminopyrazole (GDC-0339) for the Treatment of Multiple Myeloma.

A. Ebens, C. Noland, J. Lyssikatos, 2019, Journal of Medicinal Chemistry.

Identification of an imidazopyridine scaffold to generate potent and selective TYK2 inhibitors that demonstrate activity in an in vivo psoriasis model.

Adam R. Johnson, Jun Liang, J. DeVoss, 2017, Bioorganic & medicinal chemistry letters.

Antagonism of c-IAP and XIAP proteins is required for efficient induction of cell death by small-molecule IAP antagonists.

S. Hymowitz, W. Fairbrother, K. Deshayes, 2009, ACS chemical biology.

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.

Design and synthesis of a biaryl series as inhibitors for the bromodomains of CBP/P300.

Fei Wang, F. A. Romero, E. Choo, 2018, Bioorganic & 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.

Discovery of 5-Azaindazole (GNE-955) as a Potent Pan-Pim Inhibitor with Optimized Bioavailability.

M. Volgraf, A. Ebens, John G. Moffat, 2017, Journal of medicinal chemistry.

Cis-amide isosteric replacement in thienobenzoxepin inhibitors of PI3-kinase.

E. Bradley, BinQing Wei, J. Lesnick, 2013, Bioorganic & medicinal chemistry letters.

Structure-based design of thienobenzoxepin inhibitors of PI3-kinase.

D. Sutherlin, S. Sideris, Leslie B. Lee, 2011, Bioorganic & medicinal chemistry letters.

Discovery of a potent small-molecule antagonist of inhibitor of apoptosis (IAP) proteins and clinical candidate for the treatment of cancer (GDC-0152).

Zhaoyang Wen, Brigitte Maurer, Vickie Tsui, 2012, Journal of medicinal chemistry.

2-Amino-[1,2,4]triazolo[1,5-a]pyridines as JAK2 inhibitors.

M. Ultsch, C. Eigenbrot, Leslie B. Lee, 2013, Bioorganic & medicinal chemistry letters.

Rational design of phosphoinositide 3-kinase α inhibitors that exhibit selectivity over the phosphoinositide 3-kinase β isoform.

BinQing Wei, D. Sutherlin, J. Lesnick, 2011, Journal of medicinal chemistry.

Structure-based optimization of pyrazolo-pyrimidine and -pyridine inhibitors of PI3-kinase.

D. Sutherlin, L. Friedman, Leslie B. Lee, 2010, Bioorganic & medicinal chemistry letters.

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

F. A. Romero, Alexander M. Taylor, A. Côté, 2016, Journal of medicinal chemistry.

USP7 small-molecule inhibitors interfere with ubiquitin binding

Florian Gnad, Scott E. Martin, Michelle R. Arkin, 2017, Nature.

Genomic analysis of smoothened inhibitor resistance in basal cell carcinoma.

C. Rudin, R. Bourgon, Grégoire Pau, 2015, Cancer cell.

Genomic Analysis of Smoo thened Inhibitor Resistance in Basal Cell Carcinoma Graphical

C. Rudin, R. Bourgon, Grégoire Pau, 2015 .

The Rational Design of Selective Benzoxazepin Inhibitors of the α-Isoform of Phosphoinositide 3-Kinase Culminating in the Identification of (S)-2-((2-(1-Isopropyl-1H-1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)oxy)propanamide (GDC-0326).

S. Steinbacher, Steve Price, E. Gancia, 2016, Journal of medicinal chemistry.

Antagonists of inhibitor of apoptosis proteins based on thiazole amide isosteres.

C. Ly, W. Fairbrother, V. Tsui, 2010, Bioorganic & medicinal chemistry letters.

Orally bioavailable antagonists of inhibitor of apoptosis proteins based on an azabicyclooctane scaffold.

Vickie Tsui, Frederick Cohen, Harvey Wong, 2009, Journal of medicinal chemistry.

Identification of GNE-477, a potent and efficacious dual PI3K/mTOR inhibitor.

D. Sutherlin, S. Sideris, Irina S. Chuckowree, 2010, Bioorganic & medicinal chemistry letters.

Inhibiting the deubiquitinating enzymes (DUBs).

V. Tsui, Chudi O. Ndubaku, 2015, Journal of medicinal chemistry.

Regulatory T Cell Modulation by CBP/EP300 Bromodomain Inhibition*

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

CDK2/cyclinA inhibitors: targeting the cyclinA recruitment site with small molecules derived from peptide leads.

J. Nicholas, D. Sutherlin, V. Tsui, 2006, Bioorganic & medicinal chemistry letters.

Water molecules in protein–ligand interfaces. Evaluation of software tools and SAR comparison

Yong Tang, Eva Nittinger, Paul Gibbons, 2019, Journal of Computer-Aided Molecular Design.

An integrated suite of modeling tools that empower scientists in structure- and property-based drug design

Jeffrey M. Blaney, Philippe Bergeron, Man-Ling Lee, 2015, Journal of Computer-Aided Molecular Design.

Discovery of 3,5-substituted 6-azaindazoles as potent pan-Pim inhibitors.

A. Ebens, J. Lyssikatos, John G. Moffat, 2015, Bioorganic & medicinal chemistry letters.

Discovery of novel pyrazolo[1,5-a]pyrimidines as potent pan-Pim inhibitors by structure- and property-based drug design.

A. Ebens, John G. Moffat, Richard M Pastor, 2013, Bioorganic & medicinal chemistry letters.

Discovery of Small-Molecule Inhibitors of Ubiquitin Specific Protease 7 (USP7) Using Integrated NMR and in Silico Techniques.

I. Wertz, P. Di Lello, L. Kategaya, 2017, Journal of medicinal chemistry.

A new regulatory switch in a JAK protein kinase

Jun Liang, M. Ultsch, M. Lamers, 2011, Proteins.