Publications by authors named "Bruce Lefker"

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A Structure-Based Computational Pipeline for Broad-Spectrum Antiviral Discovery.
Maria A Castellanos, Alexander M Payne, Jenke Scheen, Hugo MacDermott-Opeskin, Iván Pulido, Bruce Lefker

bioRxiv· July 2025

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Open-science discovery of DNDI-6510, a compound that addresses genotoxic and metabolic liabilities of the COVID Moonshot SARS-CoV-2 Mpro lead inhibitor.
Ed J Griffen, Daren Fearon, Briana L McGovern, Lizbe Koekemoer, Blake H Balcomb, Bruce A Lefker

bioRxiv· June 2025

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Open science discovery of potent noncovalent SARS-CoV-2 main protease inhibitors.
Melissa L Boby, Daren Fearon, Matteo Ferla, Mihajlo Filep, Lizbé Koekemoer, Bruce A Lefker

Science· November 2023

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Specific quinone reductase 2 inhibitors reduce metabolic burden and reverse Alzheimer's disease phenotype in mice.
Nathaniel L Gould, Gila R Scherer, Silvia Carvalho, Khriesto Shurrush, Haneen Kayyal, Bruce Lefker

J Clin Invest· October 2023

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Toward the assembly and characterization of an encoded library hit confirmation platform: Bead-Assisted Ligand Isolation Mass Spectrometry (BALI-MS).
Anokha S Ratnayake, Mark E Flanagan, Timothy L Foley, Scott L Hultgren, Justin Bellenger, Bruce Lefker

Bioorg Med Chem· July 2021

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Quick Building Blocks (QBB): An Innovative and Efficient Business Model To Speed Medicinal Chemistry Analog Synthesis.
Christopher J Helal, Mark Bundesmann, Susan Hammond, Melissa Holmstrom, Jacquelyn Klug-McLeod, Bruce A Lefker

ACS Med Chem Lett· August 2019

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Covalent Docking Identifies a Potent and Selective MKK7 Inhibitor.
Amit Shraga, Evgenia Olshvang, Natalia Davidzohn, Payam Khoshkenar, Nicolas Germain, Bruce Lefker

Cell Chem Biol· January 2019

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Discovery of PF-06928215 as a high affinity inhibitor of cGAS enabled by a novel fluorescence polarization assay.
Justin Hall, Amy Brault, Fabien Vincent, Shawn Weng, Hong Wang, Bruce Lefker

PLoS One· October 2017

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Practical synthesis of capromorelin, a growth hormone secretagogue, via a crystallization-induced dynamic resolution.
Colin R Rose, Michael P Zawistoski, Bruce A Lefker, F Michael Mangano, Ann S Wright

Bioorg Med Chem· February 2017

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Efficacy and Pharmacology of the NLRP3 Inflammasome Inhibitor CP-456,773 (CRID3) in Murine Models of Dermal and Pulmonary Inflammation.
Michael J Primiano, Bruce A Lefker, Michael R Bowman, Andrea G Bree, Cedric Hubeau

J Immunol· September 2016

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Discovery of a Highly Selective Glycogen Synthase Kinase-3 Inhibitor (PF-04802367) That Modulates Tau Phosphorylation in the Brain: Translation for PET Neuroimaging.
Steven H Liang, Jinshan Michael Chen, Marc D Normandin, Jeanne S Chang, George C Chang, Bruce A Lefker

Angew Chem Int Ed Engl· August 2016

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Binding site elucidation and structure guided design of macrocyclic IL-17A antagonists.
Shenping Liu, Leslie A Dakin, Li Xing, Jane M Withka, Parag V Sahasrabudhe, Bruce A Lefker

Sci Rep· August 2016

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Identification of a novel, non-tetrahydroquinoline variant of the cholesteryl ester transfer protein (CETP) inhibitor torcetrapib, with improved aqueous solubility.
Amit S Kalgutkar, Kosea S Frederick, Heather L Hatch, Catherine M Ambler, David A Perry, Bruce A Lefker

Xenobiotica· July 2014

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From partial to full agonism: identification of a novel 2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole as a full agonist of the human GPR119 receptor.
Kentaro Futatsugi, Vincent Mascitti, Cristiano R W Guimarães, Nao Morishita, Cuiman Cai, Bruce A Lefker

Bioorg Med Chem Lett· January 2013

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Design and evaluation of a 2-(2,3,6-trifluorophenyl)acetamide derivative as an agonist of the GPR119 receptor.
Vincent Mascitti, Benjamin D Stevens, Chulho Choi, Kim F McClure, Cristiano R W Guimarães, Bruce A Lefker

Bioorg Med Chem Lett· March 2011

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Activation of the G-protein-coupled receptor 119: a conformation-based hypothesis for understanding agonist response.
Kim F McClure, Etzer Darout, Cristiano R W Guimarães, Michael P DeNinno, Vincent Mascitti, Bruce A Lefker

J Med Chem· March 2011

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Orally active and brain permeable proline amides as highly selective 5HT2c agonists for the treatment of obesity.
Kevin K-C Liu, Bruce A Lefker, Mark A Dombroski, Phoebe Chiang, Peter Cornelius

Bioorg Med Chem Lett· April 2010

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Discovery of CP-533536: an EP2 receptor selective prostaglandin E2 (PGE2) agonist that induces local bone formation.
Kimberly O Cameron, Bruce A Lefker, Hua Z Ke, Mei Li, Michael P Zawistoski

Bioorg Med Chem Lett· April 2009

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Diphenyl ethers as androgen receptor antagonists for the topical suppression of sebum production.
Lorna H Mitchell, Lain-Yen Hu, Maria Nguyen, Stephen Fakhoury, Yvonne Smith, Bruce Lefker

Bioorg Med Chem Lett· April 2009

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Rational design and synthesis of 4-((1R,2R)-2-hydroxycyclohexyl)-2(trifluoromethyl)benzonitrile (PF-998425), a novel, nonsteroidal androgen receptor antagonist devoid of phototoxicity for dermatological indications.
Jie Jack Li, Donna M Iula, Maria N Nguyen, Lain-Yen Hu, Danielle Dettling, Bruce A Lefker

J Med Chem· November 2008

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(1R,2S)-4-(2-cyano-cyclohexyl-oxy)-2-trifluoromethyl-benzonitrile, a potent androgen receptor antagonist for stimulating hair growth and reducing sebum production.
Lain-Yen Hu, Daniel Du, Jennifer Hoffman, Yvonne Smith, Victor Fedij, Bruce Lefker

Bioorg Med Chem Lett· November 2007

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Preparation of 4-aryl-2-trifluoromethylbenzonitrile derivatives as androgen receptor antagonists for topical suppression of sebum production.
Jennifer A Van Camp, Lain-Yen Hu, Catherine Kostlan, Bruce Lefker, Jie Li

Bioorg Med Chem Lett· October 2007

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Discovery of highly selective EP4 receptor agonists that stimulate new bone formation and restore bone mass in ovariectomized rats.
Kimberly O Cameron, Bruce A Lefker, Margaret Y Chu-Moyer, David T Crawford, Paul DaSilva Jardine

Bioorg Med Chem Lett· April 2006

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A nonprostanoid EP4 receptor selective prostaglandin E2 agonist restores bone mass and strength in aged, ovariectomized rats.
Hua Zhu Ke, D Todd Crawford, Hong Qi, Hollis A Simmons, Thomas A Owen, Bruce A Lefker

J Bone Miner Res· April 2006

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Estrogen receptor beta selective ligands: discovery and SAR of novel heterocyclic ligands.
Richard Chesworth, Matthew D Wessel, Lisa Heyden, F Michael Mangano, Michael Zawistoski, Bruce Lefker

Bioorg Med Chem Lett· December 2005

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