Publications by authors named "Gauri Deshmukh"

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Engineering ERα degraders with pleiotropic ubiquitin ligase ligands maximizes therapeutic efficacy by co-opting distinct effector ligases.
Anna Shemorry, Willem den Besten, Melinda M Mulvihill, Curt J Essenburg, Nicole Blaquiere, Gauri Deshmukh

Cell Chem Biol· May 2025

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Finding a needle in the haystack: ADME and pharmacokinetics/pharmacodynamics characterization and optimization toward orally available bifunctional protein degraders.
Giulia Apprato, Giulia Caron, Gauri Deshmukh, Diego Garcia-Jimenez, Robin Thomas Ulrich Haid

Expert Opin Drug Discov· February 2025

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Potency-Enhanced Peptidomimetic VHL Ligands with Improved Oral Bioavailability.
Hao Wu, Jeremy Murray, Noriko Ishisoko, Alexandra Frommlet, Gauri Deshmukh

J Med Chem· June 2024

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GTP1 metabolic stability assessment: A study of the tau PET tracer [F]GTP1.
Jan Marik, Sharyl Rich, Gauri Deshmukh, Donglu Zhang, Jeff Tinianow

Nucl Med Biol· November 2023

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Identification of GDC-1971 (RLY-1971), a SHP2 Inhibitor Designed for the Treatment of Solid Tumors.
Alexander M Taylor, Bret R Williams, Fabrizio Giordanetto, Elizabeth H Kelley, André Lescarbeau, Gauri Deshmukh

J Med Chem· October 2023

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Optimization of globomycin analogs as novel gram-negative antibiotics.
Keira Garland, Homer Pantua, Marie-Gabrielle Braun, Daniel J Burdick, Georgette M Castanedo, Gauri Deshmukh

Bioorg Med Chem Lett· October 2020

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Evaluating the Pharmacokinetics and Systemic Effects of a Permeability Enhancer Sodium N-[8-(2-hydroxybenzoyl)amino] Caprylate in Rats.
Po-Chang Chiang, Gauri Deshmukh, Jia Liu, Karthik Nagapudi, Jacob Z Chen

J Pharm Sci· August 2020

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RIP1 inhibition blocks inflammatory diseases but not tumor growth or metastases.
Snahel Patel, Joshua D Webster, Eugene Varfolomeev, Youngsu C Kwon, Jason H Cheng, Gauri Deshmukh

Cell Death Differ· January 2020

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Antibody Conjugation of a Chimeric BET Degrader Enables in vivo Activity.
Thomas H Pillow, Pragya Adhikari, Robert A Blake, Jinhua Chen, Geoffrey Del Rosario, Gauri Deshmukh

ChemMedChem· January 2020

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GluN2A NMDA Receptor Enhancement Improves Brain Oscillations, Synchrony, and Cognitive Functions in Dravet Syndrome and Alzheimer's Disease Models.
Jesse E Hanson, Keran Ma, Justin Elstrott, Martin Weber, Sandrine Saillet, Gauri Deshmukh

Cell Rep· January 2020

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Potent and selective inhibitors of receptor-interacting protein kinase 1 that lack an aromatic back pocket group.
Gregory L Hamilton, Huifen Chen, Gauri Deshmukh, Charles Eigenbrot, Rina Fong

Bioorg Med Chem Lett· June 2019

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Lung-restricted inhibition of Janus kinase 1 is effective in rodent models of asthma.
Hart S Dengler, Xiumin Wu, Ivan Peng, Cornelia H Rinderknecht, Youngsu Kwon, Gauri Deshmukh

Sci Transl Med· November 2018

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Use of Subcutaneous and Intraperitoneal Administration Methods to Facilitate Cassette Dosing in Microdialysis Studies in Rats.
Matthew R Durk, Gauri Deshmukh, Nicole Valle, Xiao Ding, Bianca M Liederer

Drug Metab Dispos· July 2018

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Selective Inhibitors of Dual Leucine Zipper Kinase (DLK, MAP3K12) with Activity in a Model of Alzheimer's Disease.
Snahel Patel, William J Meilandt, Rebecca I Erickson, Jinhua Chen, Gauri Deshmukh

J Med Chem· October 2017

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From a novel HTS hit to potent, selective, and orally bioavailable KDM5 inhibitors.
Jun Liang, Sharada Labadie, Birong Zhang, Daniel F Ortwine, Snahel Patel, Gauri Deshmukh

Bioorg Med Chem Lett· July 2017

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GluN2A-Selective Pyridopyrimidinone Series of NMDAR Positive Allosteric Modulators with an Improved Profile.
Elisia Villemure, Matthew Volgraf, Yu Jiang, Guosheng Wu, Cuong Q Ly, Gauri Deshmukh

ACS Med Chem Lett· January 2017

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Design and evaluation of 1,7-naphthyridones as novel KDM5 inhibitors.
Sharada S Labadie, Peter S Dragovich, Richard T Cummings, Gauri Deshmukh, Amy Gustafson

Bioorg Med Chem Lett· September 2016

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Lead optimization of a pyrazolo[1,5-a]pyrimidin-7(4H)-one scaffold to identify potent, selective and orally bioavailable KDM5 inhibitors suitable for in vivo biological studies.
Jun Liang, Birong Zhang, Sharada Labadie, Daniel F Ortwine, Maia Vinogradova, Gauri Deshmukh

Bioorg Med Chem Lett· August 2016

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Fibroblast Activation Protein Cleaves and Inactivates Fibroblast Growth Factor 21.
Diana Ronai Dunshee, Travis W Bainbridge, Noelyn M Kljavin, Jose Zavala-Solorio, Amy C Schroeder, Gauri Deshmukh

J Biol Chem· March 2016

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Discovery of GluN2A-Selective NMDA Receptor Positive Allosteric Modulators (PAMs): Tuning Deactivation Kinetics via Structure-Based Design.
Matthew Volgraf, Benjamin D Sellers, Yu Jiang, Guosheng Wu, Cuong Q Ly, Gauri Deshmukh

J Med Chem· March 2016

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Scaffold-Hopping and Structure-Based Discovery of Potent, Selective, And Brain Penetrant N-(1H-Pyrazol-3-yl)pyridin-2-amine Inhibitors of Dual Leucine Zipper Kinase (DLK, MAP3K12).
Snahel Patel, Seth F Harris, Paul Gibbons, Gauri Deshmukh, Amy Gustafson

J Med Chem· October 2015

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Use of cassette dosing to enhance the throughput of rat brain microdialysis studies.
Gauri Deshmukh, Kefeng Sun, Bianca M Liederer, Xiao Ding, Xingrong Liu

Drug Metab Dispos· July 2015

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Discovery of dual leucine zipper kinase (DLK, MAP3K12) inhibitors with activity in neurodegeneration models.
Snahel Patel, Frederick Cohen, Brian J Dean, Kelly De La Torre, Gauri Deshmukh

J Med Chem· January 2015

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Use of cassette dosing approach to examine the effects of P-glycoprotein on the brain and cerebrospinal fluid concentrations in wild-type and P-glycoprotein knockout rats.
Xingrong Liu, Jonathan Cheong, Xiao Ding, Gauri Deshmukh

Drug Metab Dispos· April 2014

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Design and evaluation of novel 8-oxo-pyridopyrimidine Jak1/2 inhibitors.
Sharada Labadie, Kathy Barrett, Wade S Blair, Christine Chang, Gauri Deshmukh

Bioorg Med Chem Lett· November 2013

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