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Approach for targeting Ras with small molecules that activate SOS-mediated nucleotide exchange

Proceedings of the National Academy of Sciences - PNAS, 2014-03, Vol.111 (9), p.3401-3406

2014

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Fragment Optimization of Reversible Binding to the Switch II Pocket on KRAS Leads to a Potent, In Vivo Active KRASG12C Inhibitor

Journal of medicinal chemistry, 2022-11, Vol.65 (21), p.14614-14629

2022

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Discovery and Structure-Based Optimization of Benzimidazole-Derived Activators of SOS1-Mediated Nucleotide Exchange on RAS

Journal of medicinal chemistry, 2018-10, Vol.61 (19), p.8875-8894

2018

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Arrest of mouse preterm labor until term delivery by combination therapy with atosiban and mundulone, a natural product with tocolytic efficacy

Pharmacological research, 2023-09, Vol.195, p.106876-106876, Article 106876

2023

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Further optimization of the K-Cl cotransporter KCC2 antagonist ML077: Development of a highly selective and more potent in vitro probe

Bioorganic & medicinal chemistry letters, 2012-07, Vol.22 (14), p.4532-4535

2012

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Allosteric antagonism of insect odorant receptor ion channels

PloS one, 2012-01, Vol.7 (1), p.e30304

2012

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High-Content Imaging Platform to Discover Chemical Modulators of Plasma Membrane Rafts

ACS central science, 2022-03, Vol.8 (3), p.370-378

2022

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Discovery of Small Molecules that Bind to K-Ras and Inhibit Sos-Mediated Activation

Angewandte Chemie (International ed.), 2012-06, Vol.51 (25), p.6140-6143

International ed. in English, 2012

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Discovery of WD Repeat-Containing Protein 5 (WDR5)–MYC Inhibitors Using Fragment-Based Methods and Structure-Based Design

Journal of medicinal chemistry, 2020-04, Vol.63 (8), p.4315-4333

2020

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Discovery of Sulfonamide-Derived Agonists of SOS1-Mediated Nucleotide Exchange on RAS Using Fragment-Based Methods

Journal of medicinal chemistry, 2020-08, Vol.63 (15), p.8325-8337

2020

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High-throughput screening identifies small molecules that bind to the RAS:SOS:RAS complex and perturb RAS signaling

Analytical biochemistry, 2018-05, Vol.548 (C), p.44-52

2018

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Small Molecule-Mediated Activation of RAS Elicits Biphasic Modulation of Phospho-ERK Levels that Are Regulated through Negative Feedback on SOS1

Molecular cancer therapeutics, 2018-05, Vol.17 (5), p.1051-1060

2018

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Discovery and Optimization of Potent, Cell-Active Pyrazole-Based Inhibitors of Lactate Dehydrogenase (LDH)

Journal of medicinal chemistry, 2017-11, Vol.60 (22), p.9184-9204

2017

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Synthesis and evaluation of aniline headgroups for alkynyl thienopyrimidine dual EGFR/ErbB-2 kinase inhibitors

Bioorganic & medicinal chemistry letters, 2009-03, Vol.19 (5), p.1332-1336

2009

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A fragment‐based approach to discovery of Receptor for Advanced Glycation End products inhibitors

Proteins, structure, function, and bioinformatics, 2021-11, Vol.89 (11), p.1399-1412

2021

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Dynamic Imaging of LDH Inhibition in Tumors Reveals Rapid In Vivo Metabolic Rewiring and Vulnerability to Combination Therapy

Cell reports (Cambridge), 2020-02, Vol.30 (6), p.1798-1810.e4

2020

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Dual EGFR/ErbB-2 inhibitors from novel pyrrolidinyl-acetylenic thieno[3,2- d]pyrimidines

Bioorganic & medicinal chemistry, 2008-11, Vol.18 (21), p.5738-5740

2008

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Discovery and Optimization of Salicylic Acid-Derived Sulfonamide Inhibitors of the WD Repeat-Containing Protein 5–MYC Protein–Protein Interaction

Journal of medicinal chemistry, 2019-12, Vol.62 (24), p.11232-11259

2019

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Discovery of Aminopiperidine Indoles That Activate the Guanine Nucleotide Exchange Factor SOS1 and Modulate RAS Signaling

Journal of medicinal chemistry, 2018-07, Vol.61 (14), p.6002-6017

2018

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Isoform selective PLD inhibition by novel, chiral 2,8-diazaspiro[4.5]decan-1-one derivatives

Bioorganic & medicinal chemistry letters, 2018-12, Vol.28 (23-24), p.3670-3673

2018

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Pyrazole-Based Lactate Dehydrogenase Inhibitors with Optimized Cell Activity and Pharmacokinetic Properties

Journal of medicinal chemistry, 2020-10, Vol.63 (19), p.10984-11011

2020

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Discovery of Dabrafenib: A Selective Inhibitor of Raf Kinases with Antitumor Activity against B‑Raf-Driven Tumors

ACS medicinal chemistry letters, 2013-03, Vol.4 (3), p.358-362

2013

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Small Molecule Activation of NAPE-PLD Enhances Efferocytosis by Macrophages

ACS chemical biology, 2023-08, Vol.18 (8), p.1891-1904

2023

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Simultaneous Exposure to Intracellular and Extracellular Photosensitizers for the Treatment of Staphylococcus aureus Infections

Antimicrobial agents and chemotherapy, 2021-11, Vol.65 (12), p.e0091921-e0091921

2021

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Dual inhibition of Kif15 by oxindole and quinazolinedione chemical probes

Bioorganic & medicinal chemistry letters, 2019-01, Vol.29 (2), p.148-154

2019

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Approach for targeting Ras with small molecules that activate SOS-mediated nucleotide exchange

Fragment Optimization of Reversible Binding to the Switch II Pocket on KRAS Leads to a Potent, In Vivo Active KRASG12C Inhibitor

Discovery and Structure-Based Optimization of Benzimidazole-Derived Activators of SOS1-Mediated Nucleotide Exchange on RAS

Arrest of mouse preterm labor until term delivery by combination therapy with atosiban and mundulone, a natural product with tocolytic efficacy

Further optimization of the K-Cl cotransporter KCC2 antagonist ML077: Development of a highly selective and more potent in vitro probe

Allosteric antagonism of insect odorant receptor ion channels

High-Content Imaging Platform to Discover Chemical Modulators of Plasma Membrane Rafts

Discovery of Small Molecules that Bind to K-Ras and Inhibit Sos-Mediated Activation

Discovery of WD Repeat-Containing Protein 5 (WDR5)–MYC Inhibitors Using Fragment-Based Methods and Structure-Based Design

Discovery of Sulfonamide-Derived Agonists of SOS1-Mediated Nucleotide Exchange on RAS Using Fragment-Based Methods

High-throughput screening identifies small molecules that bind to the RAS:SOS:RAS complex and perturb RAS signaling

Small Molecule-Mediated Activation of RAS Elicits Biphasic Modulation of Phospho-ERK Levels that Are Regulated through Negative Feedback on SOS1

Discovery and Optimization of Potent, Cell-Active Pyrazole-Based Inhibitors of Lactate Dehydrogenase (LDH)

Synthesis and evaluation of aniline headgroups for alkynyl thienopyrimidine dual EGFR/ErbB-2 kinase inhibitors

A fragment‐based approach to discovery of Receptor for Advanced Glycation End products inhibitors

Dynamic Imaging of LDH Inhibition in Tumors Reveals Rapid In Vivo Metabolic Rewiring and Vulnerability to Combination Therapy

Dual EGFR/ErbB-2 inhibitors from novel pyrrolidinyl-acetylenic thieno[3,2- d]pyrimidines

Discovery and Optimization of Salicylic Acid-Derived Sulfonamide Inhibitors of the WD Repeat-Containing Protein 5–MYC Protein–Protein Interaction

Discovery of Aminopiperidine Indoles That Activate the Guanine Nucleotide Exchange Factor SOS1 and Modulate RAS Signaling

Isoform selective PLD inhibition by novel, chiral 2,8-diazaspiro[4.5]decan-1-one derivatives

Pyrazole-Based Lactate Dehydrogenase Inhibitors with Optimized Cell Activity and Pharmacokinetic Properties

Discovery of Dabrafenib: A Selective Inhibitor of Raf Kinases with Antitumor Activity against B‑Raf-Driven Tumors

Small Molecule Activation of NAPE-PLD Enhances Efferocytosis by Macrophages

Simultaneous Exposure to Intracellular and Extracellular Photosensitizers for the Treatment of Staphylococcus aureus Infections

Dual inhibition of Kif15 by oxindole and quinazolinedione chemical probes

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