J David Warren

About

J David Warren, Ph.D., is an experienced researcher in the field of bioorganic and medicinal chemistry, who has placed several compounds into advanced preclinical development. His accomplishments include the development of methodology that allows for the total chemical synthesis of fully glycosylated proteins; the synthesis and application of new photostable fluorophores; the development of novel therapeutics for the treatment of Niemann-Pick type C (NPC) disease; the discovery of nucleoside analogs active against adenosine kinase; the discovery of selective inhibitors of HCN1 for the treatment of neuropathic pain; the discovery of novel PET tracers for imaging the chemokine receptor CXCR4; the identification of a small molecule inhibitor of 3-phosphoglycerate dehydrogenase to target serine biosynthesis in cancer; the discovery and development of inhibitors selective for mycobacterial versus human proteasomes; and the CURE-PRO platform, an innovative new approach to targeted protein degradation. David is an Adjunct Associate Professor of Research in Biochemistry and former Director of the Milstein Chemistry Core Facility at Weill Cornell Medicine in New York City. He received his Ph.D. from Colorado State University, where he was awarded a graduate fellowship from Boehringer Ingelheim, and carried out postdoctoral studies under the tutelage of Dr. Samuel J. Danishefsky at the Memorial Sloan-Kettering Cancer Center as an NIH-supported fellow. He currently sits on the Scientific Advisory Board of Akelos, Inc., and is a scientific advisor for several small biopharmaceutical companies. He holds 10 issued US and international patents and has published over 48 peer-reviewed publications and book chapters.

Work

Weill Cornell Medical College
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Associate Professor

US

Education

Memorial Sloan-Kettering Cancer Center
United States of America

Postdoc

Colorado State University
United States of America

PhD

Fort Lewis College
United States of America

BS

Publications

Healing wounds with a multimodal botanical hydrogel: a clinical outcomes comparison study

Published by

Journal of Wound Care

Summary

journal-article

Linking gene expression to tumor microenvironment using H&E features in stomach adenocarcinoma.

Published by

Journal of Clinical Oncology

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journal-article

Predicting therapeutic response in stomach adenocarcinoma by integrating H&E and RNA-seq using deep learning.

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Journal of Clinical Oncology

Summary

journal-article

Combinatorial Ubiquitination REal-time PROteolysis (CURE-PROs): A Modular Platform for Generating Reversible, Self-Assembling Bifunctional Targeted Degraders

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Journal of Medicinal Chemistry

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journal-article

Real-Time Ratiometric pH Imaging of Macrophage Lysosomes Using the Novel pH-sensitive Probe ApHID

Summary

preprint

An anchor-tether ‘hindered’ HCN1 inhibitor is antihyperalgesic in a rat spared nerve injury neuropathic pain model

Published by

British Journal of Anaesthesia

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journal-article

Probucol is anti-hyperalgesic in a mouse peripheral nerve injury model of neuropathic pain

Published by

Neurobiology of Pain

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journal-article

Substituted alkylphenols as HCN1 antagonists

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patent

THERAPEUTIC COMPOSITION OF CURE-PRO COMPOUNDS FOR TARGETED DEGRADATION OF BET DOMAIN PROTEINS, AND METHODS OF MAKING AND USAGE

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patent

THERAPEUTIC CURE-PRO COMPOUNDS FOR TARGETED DEGRADATION OF BET DOMAIN PROTEINS, AND METHODS OF MAKING AND USING THEM

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patent

THERAPEUTICALLY USEFUL CURE-PRO MOLECULES FOR E3 LIGASE MEDIATED DEGRADATION OF PROTEINS, AND METHODS OF MAKING AND USING THEM

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patent

Tetrathiomolybdate (TM)-associated copper depletion influences collagen remodeling and immune response in the pre-metastatic niche of breast cancer

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npj Breast Cancer

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journal-article

PROTACs: Promising Approaches for Epigenetic Strategies to Overcome Drug Resistance

Published by

Current Cancer Drug Targets

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journal-article

CRL4泛素连接酶抑制剂及其用途

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patent

Inhibitors of CRL4 ubiquitin ligase and uses thereof

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patent

Got milk? A case series of an amatoxin-exposed family, including a breastfeeding mother and infant

Published by

Clinical Toxicology

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journal-article

NOVEL NUCLEOSIDE ANALOGS AND USE THEREOF IN THERAPEUTIC TREATMENT

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patent

INHIBITORS OF CRL4 UBIQUITIN LIGASE AND USES THEREOF

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patent

[18F]Fluoroethyltriazolyl Monocyclam Derivatives as Imaging Probes for the Chemokine Receptor CXCR4

Published by

Molecules

Summary

journal-article

[<sup>18</sup>F]Fluoroethyltriazolyl Monocyclam Derivatives as Imaging Probes for the Chemokine Receptor CXCR4

Published by

Molecules

Summary

journal-article

[<sup>18</sup>F]fluoroethyltriazolyl monocyclam derivatives as imaging probes for the chemokine receptor CXCR4

Published by

Molecules

Summary

journal-article

Alkylphenol inverse agonists of HCN1 gating: H-bond propensity, ring saturation and adduct geometry differentially determine efficacy and potency

Published by

Biochemical Pharmacology

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journal-article

Compositions and their use for removing cholesterol

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patent

Identification of a Mycothiol-Dependent Nitroreductase from Mycobacterium tuberculosis

Published by

ACS Infectious Diseases

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journal-article

[ <sup>18</sup> F]RPS-544: A PET tracer for imaging the chemokine receptor CXCR4

Published by

Nuclear Medicine and Biology

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journal-article

Methods and compositions for altering photophysical properties of fluorophores via proximal quenching

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patent

Dye compositions, methods of preparation, conjugates thereof, and methods of use

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patent

Dual-target binding ligands with modulated pharmacokinetics for endoradiotherapy of prostate cancer

Published by

Journal of Nuclear Medicine

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journal-article

Identification of a nucleoside analog active against adenosine kinase-expressing plasma cell malignancies

Published by

Journal of Clinical Investigation

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journal-article

Influencing the tumor microenvironment: A Phase II study of copper depletion using tetrathiomolybdate in patients with breast cancer at high risk for recurrence and in preclinical models of lung metastases

Published by

Clinical Cancer Research

Summary

journal-article

Erratum: Identification of a small molecule inhibitor of 3-phosphoglycerate dehydrogenase to target serine biosynthesis in cancers (Proceedings of the National Academy of Sciences of the United States of America (2016) 113 (1778-1783) DOI:10.1073/pnas.1521548113)

Published by

Proceedings of the National Academy of Sciences of the United States of America

Summary

journal-article

Identification of a small molecule inhibitor of 3-phosphoglycerate dehydrogenase to target serine biosynthesis in cancers

Published by

Proceedings of the National Academy of Sciences of the United States of America

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journal-article

Methods and compositions for altering photophysical properties of fluorophores via proximal quenching

Summary

patent

Biosynthesis of cell envelope-associated phenolic glycolipids in Mycobacterium marinum

Published by

Journal of Bacteriology

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journal-article

Rapid, semiquantitative assay to discriminate among compounds with activity against replicating or nonreplicating Mycobacterium tuberculosis

Published by

Antimicrobial Agents and Chemotherapy

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journal-article

Targeting mitochondrial cardiolipin and the cytochrome c/cardiolipin complex to promote electron transport and optimize mitochondrial ATP synthesis.

Published by

British journal of pharmacology

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journal-article

Compositions comprising homogeneously glycosylated erythropoietin

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patent

Beta cyclodextrins bind, stabilize, and remove lipofuscin bisretinoids from retinal pigment epithelium

Published by

Proceedings of the National Academy of Sciences of the United States of America

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journal-article

Beta cyclodextrins bind, stabilize, and remove lipofuscin bisretinoids from retinal pigment epithelium

Published by

Proceedings of the National Academy of Sciences of the United States of America

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journal-article

Oxathiazolones selectively inhibit the human immunoproteasome over the constitutive proteasome

Published by

ACS Medicinal Chemistry Letters

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journal-article

Targeting mitochondrial cardiolipin and the cytochrome c/cardiolipin complex to promote electron transport and optimize mitochondrial ATP synthesis

Published by

British Journal of Pharmacology

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journal-article

Pharmacokinetic and in vivo efficacy studies of the mycobactin biosynthesis inhibitor salicyl-AMS in mice

Published by

Antimicrobial Agents and Chemotherapy

Summary

journal-article

Tetrathiomolybdate-associated copper depletion decreases circulating endothelial progenitor cells in women with breast cancer at high risk of relapse

Published by

Annals of Oncology

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journal-article

Tetrathiomolybdate-associated copper depletion decreases circulating endothelial progenitor cells in women with breast cancer at high risk of relapse

Published by

Annals of Oncology

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journal-article

The mitochondrial-targeted compound SS-31 re-energizes ischemic mitochondria by interacting with cardiolipin

Published by

Journal of the American Society of Nephrology

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journal-article

The Mitochondrial-Targeted Compound SS-31 Re-Energizes Ischemic Mitochondria by Interacting with Cardiolipin

Published by

Journal of the American Society of Nephrology

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journal-article

Whole Cell Screen for Inhibitors of pH Homeostasis in Mycobacterium tuberculosis

Published by

PLoS ONE

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journal-article

Whole Cell Screen for Inhibitors of pH Homeostasis in Mycobacterium tuberculosis

Published by

Plos One

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journal-article

Cyanine fluorophore derivatives with enhanced photostability

Published by

Nature Methods

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journal-article

Cyanine fluorophore derivatives with enhanced photostability

Published by

Nature Methods

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journal-article

Enhanced photostability of cyanine fluorophores across the visible spectrum

Published by

Nature Methods

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journal-article

Enhanced photostability of cyanine fluorophores across the visible spectrum

Published by

Nature Methods

Summary

journal-article

Nonsteroidal anti-inflammatory drug sensitizes Mycobacterium tuberculosis to endogenous and exogenous antimicrobials

Published by

Proceedings of the National Academy of Sciences of the United States of America

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journal-article

Nonsteroidal anti-inflammatory drug sensitizes Mycobacterium tuberculosis to endogenous and exogenous antimicrobials

Published by

Proceedings of the National Academy of Sciences of the United States of America

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journal-article

On the mechanisms of cyanine fluorophore photostabilization

Published by

Journal of Physical Chemistry Letters

Summary

journal-article

On the mechanisms of cyanine fluorophore photostabilization

Published by

Journal of Physical Chemistry Letters

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journal-article

Photoproducts of Tryptophan, Their Synthesis and Uses Thereof

Summary

patent

Discovery and biological characterization of 1-(1H-indol-3-yl)-9H-pyrido[3,4-b]-indole as an aryl hydrocarbon receptor activator generated by photoactivation of tryptophan by sunlight

Published by

Chemico-Biological Interactions

Summary

journal-article

Discovery and biological characterization of 1-(1H-indol-3-yl)-9H-pyrido[3, 4-b]indole as an aryl hydrocarbon receptor activator generated by photoactivation of tryptophan by sunlight

Published by

Chemico-Biological Interactions

Summary

journal-article

On the chemical mechanism of succinic semialdehyde dehydrogenase (GabD1) from Mycobacterium tuberculosis

Published by

Archives of Biochemistry and Biophysics

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journal-article

On the chemical mechanism of succinic semialdehyde dehydrogenase (GabD1) from Mycobacterium tuberculosis

Published by

Archives of Biochemistry and Biophysics

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journal-article

Opsin Is a Phospholipid Flippase

Published by

Current Biology

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journal-article

Opsin is a phospholipid flippase

Published by

Current Biology

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journal-article

Endocytosis of beta-cyclodextrins is responsible for cholesterol reduction in Niemann-Pick type C mutant cells

Published by

Proceedings of the National Academy of Sciences of the United States of America

Summary

journal-article

Endocytosis of beta-cyclodextrins is responsible for cholesterol reduction in Niemann-Pick type C mutant cells

Published by

Proceedings of the National Academy of Sciences of the United States of America

Summary

journal-article

Triazaspirodimethoxybenzoyls as Selective Inhibitors of Mycobacterial Lipoamide Dehydrogenase

Published by

Biochemistry

Summary

journal-article

Triazaspirodimethoxybenzoyls as selective inhibitors of mycobacterial lipoamide dehydrogenase

Published by

Biochemistry

Summary

journal-article

Method for preparing polyfunctionalized peptides and/or proteins via native chemical ligation

Summary

patent

Cooperation between a coenzyme A-independent stand-alone initiation module and an iterative type I polyketide synthase during synthesis of mycobacterial phenolic glycolipids

Published by

Journal of the American Chemical Society

Summary

journal-article

Inhibitors selective for mycobacterial versus human proteasomes

Published by

Nature

Summary

journal-article

Inhibitors selective for mycobacterial versus human proteasomes

Published by

Nature

Summary

journal-article

Synthesis and evaluation of inhibitors selective for mycobacterial vs. human proteasomes

Published by

Abstracts of Papers of the American Chemical Society

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journal-article

Synthetic carbohydrate-based anticancer vaccines: The Memorial Sloan-Kettering experience

Published by

Expert Review of Vaccines

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journal-article

Synthetic carbohydrate-based anticancer vaccines: the Memorial Sloan-Kettering experience

Published by

Expert Review of Vaccines

Summary

journal-article

Synthetic carbohydrate-based antitumor vaccines

Published by

ACS Symposium Series

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book

Fully synthetic carbohydrate HIV antigens designed on the logic of the 2G12 antibody

Published by

Journal of the American Chemical Society

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journal-article

Fully synthetic carbohydrate HIV antigens designed on the logic of the 2G12 antibody

Published by

Journal of the American Chemical Society

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journal-article

Synthetic glycopeptide-based vaccines

Published by

Glycopeptides and Glycoproteins: Synthesis, Structure, and Application

Summary

journal-article

A highly convergent synthesis of an N-linked glycopeptide presenting the H-type 2 human blood group determinant

Published by

Tetrahedron

Summary

journal-article

A highly convergent synthesis of an N-linked glycopeptide presenting the H-type 2 human blood group determinant

Published by

Tetrahedron

Summary

journal-article

A route to cyclic peptides and glycopeptides by native chemical ligation using in situ derived thioesters

Published by

Tetrahedron Letters

Summary

journal-article

A route to cyclic peptides and glycopeptides by native chemical ligation using in situ derived thioesters

Published by

Tetrahedron Letters

Summary

journal-article

Building complex glycopeptides: Development of a cysteine-free native chemical ligation protocol

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Angewandte Chemie - International Edition

Summary

journal-article

Building complex glycopeptides: Development of a cysteine-free native chemical ligation protocol

Published by

Angewandte Chemie-International Edition

Summary

journal-article

Reiterative cysteine-based coupling leading to complex, homogeneous glycopeptides

Published by

Tetrahedron Letters

Summary

journal-article

Reiterative cysteine-based coupling leading to complex, homogeneous glycopeptides

Published by

Tetrahedron Letters

Summary

journal-article

Studies related to the relative thermodynamic stability of C-terminal peptidyl esters of O-hydroxy thiophenol: Emergence of a doable strategy for non-cysteine ligation applicable to the chemical synthesis of glycopeptides

Published by

Journal of the American Chemical Society

Summary

journal-article

Studies related to the relative thermodynamic stability of C-terminal peptidyl esters of O-hydroxy thiophenol: Emergence of a doable strategy for non-cysteine ligation applicable to the chemical synthesis of glycopeptides

Published by

Journal of the American Chemical Society

Summary

journal-article

Synthesis of the fucosylated biantennary N-glycan of erythropoietin

Published by

Tetrahedron Letters

Summary

journal-article

Synthesis of the fucosylated biantennary N-glycan of erythropoietin

Published by

Tetrahedron Letters

Summary

journal-article

Synthetic carbohydrate-based antitumor vaccines: Challenges and opportunities

Published by

Expert Review of Vaccines

Summary

journal-article

Synthetic carbohydrate-based antitumor vaccines: challenges and opportunities

Published by

Expert Review of Vaccines

Summary

journal-article

Toward fully synthetic glycoproteins by ultimately convergent routes: A solution to a long-standing problem

Published by

Journal of the American Chemical Society

Summary

journal-article

Toward fully synthetic glycoproteins by ultimately convergent routes: A solution to a long-standing problem

Published by

Journal of the American Chemical Society

Summary

journal-article

Synthesis of indoles by palladium-catalyzed reductive N-heteroannulation of 2-nitrostyrenes: Methyl indole-4-carboxylate [(1H-Indole-4-carboxylic acid, methyl ester)]

Published by

Organic Syntheses

Summary

book

Chiral ketone-catalyzed asymmetric epoxidation of 2,2-disubstituted vinylsilanes

Published by

Journal of Organic Chemistry

Summary

journal-article