H. Bregman

发表

An organometallic protein kinase inhibitor pharmacologically activates p53 and induces apoptosis in human melanoma cells.

K. Flaherty, M. Herlyn, M. Soengas, 2007, Cancer research.

Discovery of novel, induced-pocket binding oxazolidinones as potent, selective, and orally bioavailable tankyrase inhibitors.

Steve Schneider, Xin Huang, John Newcomb, 2013, Journal of medicinal chemistry.

The discovery of aminopyrazines as novel, potent Na(v)1.7 antagonists: hit-to-lead identification and SAR.

H. Bregman, S. McDonough, Liyue Huang, 2012, Bioorganic & Medicinal Chemistry Letters.

The crystal structure of BRAF in complex with an organoruthenium inhibitor reveals a mechanism for inhibition of an active form of BRAF kinase.

Peng Xie, Ronen Marmorstein, Eric Meggers, 2009, Biochemistry.

Exploring Chemical Space with Organometallics: Ruthenium Complexes as Protein Kinase Inhibitors

G. E. Atilla‐Gokcumen, Douglas S. Williams, H. Bregman, 2007 .

Structure-Based Design of Potent and Selective CK1γ Inhibitors.

H. Bregman, J. Newcomb, Xin Huang, 2012, ACS medicinal chemistry letters.

Application of a Parallel Synthetic Strategy in the Discovery of Biaryl Acyl Sulfonamides as Efficient and Selective NaV1.7 Inhibitors.

Dong Liu, R. Fremeau, H. Bregman, 2016, Journal of medicinal chemistry.

Identification of a potent, state-dependent inhibitor of Nav1.7 with oral efficacy in the formalin model of persistent pain.

Xiao Mei Zheng, A. Malmberg, H. Bregman, 2011, Journal of medicinal chemistry.

Crystal Structure of the PIM2 Kinase in Complex with an Organoruthenium Inhibitor

S. Knapp, F. von Delft, J. Debreczeni, 2009, PloS one.

Specificity of induction of cancer protective enzymes by analogues of tert-butyl-4-hydroxyanisole (BHA).

H. Bregman, P. Talalay, H. Prochaska, 1985, Biochemical pharmacology.

Discovery and hit-to-lead optimization of pyrrolopyrimidines as potent, state-dependent Na(v)1.7 antagonists.

H. Bregman, S. McDonough, A. Zou, 2012, Bioorganic & medicinal chemistry letters.

Discovery and optimization of aminopyrimidinones as potent and state-dependent Nav1.7 antagonists.

A. Malmberg, H. Bregman, S. McDonough, 2012, Bioorganic & medicinal chemistry letters.

The discovery of benzoxazine sulfonamide inhibitors of NaV1.7: Tools that bridge efficacy and target engagement.

R. Fremeau, H. Bregman, M. Chu-Moyer, 2017, Bioorganic & medicinal chemistry letters.

Development of novel dual binders as potent, selective, and orally bioavailable tankyrase inhibitors.

H. Bregman, J. Newcomb, P. Andrews, 2013, Journal of medicinal chemistry.

Discovery of a class of novel tankyrase inhibitors that bind to both the nicotinamide pocket and the induced pocket.

H. Bregman, Xin Huang, Cindy A. Wilson, 2013, Journal of medicinal chemistry.

Exploring Chemical Space with Organometallics: Ruthenium Complexes as Protein Kinase Inhibitors

Seann P. Mulcahy, G. E. Atilla‐Gokcumen, Douglas S. Williams, 2007 .

Structure-based design of 2-aminopyridine oxazolidinones as potent and selective tankyrase inhibitors.

Steve Schneider, Xin Huang, Angel Guzman-Perez, 2013, ACS medicinal chemistry letters.

Sulfonamides as Selective NaV1.7 Inhibitors: Optimizing Potency and Pharmacokinetics While Mitigating Metabolic Liabilities.

R. Fremeau, H. Bregman, M. Chu-Moyer, 2017, Journal of Medicinal Chemistry.

A modular synthesis of the lamellarins: total synthesis of lamellarin G trimethyl ether.

H. Bregman, S. Handy, Yanan Zhang, 2004, The Journal of organic chemistry.

Purinylpyridinylamino-based DFG-in/αC-helix-out B-Raf inhibitors: Applying mutant versus wild-type B-Raf selectivity indices for compound profiling.

D. Whittington, H. Bregman, Matthew R. Lee, 2016, Bioorganic & medicinal chemistry.

An organometallic inhibitor for glycogen synthase kinase 3.

Douglas S. Williams, H. Bregman, E. Meggers, 2004, Journal of the American Chemical Society.

Switching on a signaling pathway with an organoruthenium complex.

Douglas S. Williams, H. Bregman, E. Meggers, 2005, Angewandte Chemie.

Electrophilic properties of itaconate and derivatives regulate the IκBζ–ATF3 inflammatory axis

Maxim N. Artyomov, E. Klechevsky, S. Akira, 2018, Nature.

An unusual dehalogenation in the Suzuki coupling of 4-bromopyrrole-2-carboxylates

H. Bregman, S. Handy, Jennifer S Lewis, 2003 .

Crystal structures of human glycine receptor α3 bound to a novel class of analgesic potentiators

J. Luther, H. Bregman, Xin Huang, 2016, Nature Structural &Molecular Biology.

Organometallic Compounds with Biological Activity: A Very Selective and Highly Potent Cellular Inhibitor for Glycogen Synthase Kinase 3

G. E. Atilla‐Gokcumen, Douglas S. Williams, H. Bregman, 2006, Chembiochem : a European journal of chemical biology.

Effectiveness of COVID-19 mRNA Vaccination in Preventing COVID-19–Associated Hospitalization Among Adults with Previous SARS-CoV-2 Infection — United States, June 2021–February 2022

H. Bregman, L. Feldstein, I. Plumb, 2022, MMWR. Morbidity and mortality weekly report.

Applications of parallel synthetic lead hopping and pharmacophore-based virtual screening in the discovery of efficient glycine receptor potentiators.

H. Bregman, L. Berry, Liyue Huang, 2017, European journal of medicinal chemistry.

A modular synthesis of the lamellarins: total synthesis of lamellarin G trimethyl ether.

H. Bregman, S. Handy, Yanan Zhang, 2004, The Journal of organic chemistry.

Ruthenium half-sandwich complexes bound to protein kinase Pim-1.

S. Knapp, J. Debreczeni, A. Bullock, 2006, Angewandte Chemie.

Inhibition of Inactive States of Tetrodotoxin-Sensitive Sodium Channels Reduces Spontaneous Firing of C-Fiber Nociceptors and Produces Analgesia in Formalin and Complete Freund’s Adjuvant Models of Pain

Zhe Zhang, A. Malmberg, D. Simone, 2015, PloS one.

Rapid access to unexplored chemical space by ligand scanning around a ruthenium center: discovery of potent and selective protein kinase inhibitors.

Eric Meggers, H. Bregman, E. Meggers, 2006, Journal of the American Chemical Society.

2-Phenylamino-6-cyano-1H-benzimidazole-based isoform selective casein kinase 1 gamma (CK1γ) inhibitors.

H. Bregman, J. Newcomb, Xin Huang, 2012, Bioorganic & medicinal chemistry letters.

The Discovery and Hit-to-Lead Optimization of Tricyclic Sulfonamides as Potent and Efficacious Potentiators of Glycine Receptors.

H. Bregman, Xin Huang, Liyue Huang, 2017, Journal of medicinal chemistry.

Ruthenium half-sandwich complexes as protein kinase inhibitors: derivatization of the pyridocarbazole pharmacophore ligand.

R. Webster, Douglas S. Williams, H. Bregman, 2007, Organic & biomolecular chemistry.

From imide to lactam metallo-pyridocarbazoles: distinct scaffolds for the design of selective protein kinase inhibitors.

S. Diamond, H. Bregman, E. Meggers, 2009, Journal of Organic Chemistry.

Ruthenium half-sandwich complexes as protein kinase inhibitors: an N-succinimidyl ester for rapid derivatizations of the cyclopentadienyl moiety.

H. Bregman, E. Meggers, 2006, Organic letters.

Sulfonamides as Selective NaV1.7 Inhibitors: Optimizing Potency and Pharmacokinetics to Enable in Vivo Target Engagement.

R. Fremeau, H. Bregman, M. Chu-Moyer, 2016, ACS medicinal chemistry letters.

The discovery of aminopyrazines as novel, potent Na(v)1.7 antagonists: hit-to-lead identification and SAR.

H. Bregman, S. McDonough, Liyue Huang, 2012, Bioorganic & medicinal chemistry letters.

From imide to lactam metallo-pyridocarbazoles: distinct scaffolds for the design of selective protein kinase inhibitors.

S. Diamond, H. Bregman, E. Meggers, 2009, The Journal of organic chemistry.