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Selectivity through Targeted Protein Degradation (TPD)

Journal of medicinal chemistry, 2022-06, Vol.65 (12), p.8113-8126

Gopalsamy, Ariamala

2022

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Selectivity through Targeted Protein Degradation (TPD): Miniperspective

Journal of medicinal chemistry, 2022-06, Vol.65 (12), p.8113-8126

Gopalsamy, Ariamala

2022

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Covalent Enzyme Inhibition through Fluorosulfate Modification of a Noncatalytic Serine Residue

ACS chemical biology, 2017-08, Vol.12 (8), p.2015-2020

2017

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Rational Targeting of Active-Site Tyrosine Residues Using Sulfonyl Fluoride Probes

ACS chemical biology, 2015-04, Vol.10 (4), p.1094-1098

2015

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Cellular thermal shift and clickable chemical probe assays for the determination of drug-target engagement in live cells

Organic & biomolecular chemistry, 2016-01, Vol.14 (26), p.6179-6183

2016

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Dual Inhibition of TYK2 and JAK1 for the Treatment of Autoimmune Diseases: Discovery of (( S)-2,2-Difluorocyclopropyl)((1 R,5 S)-3-(2-((1-methyl-1 H-pyrazol-4-yl)amino)pyrimidin-4-yl)-3,8-diazabicyclo[3.2.1]octan-8-yl)methanone (PF-06700841)

Journal of medicinal chemistry, 2018-10, Vol.61 (19), p.8597-8612

2018

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Identification of pyrimidine derivatives as hSMG-1 inhibitors

Bioorganic & medicinal chemistry letters, 2012-11, Vol.22 (21), p.6636-6641

2012

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A small molecule inhibitor of the Wnt antagonist secreted frizzled-related protein-1 stimulates bone formation

Bone (New York, N.Y.), 2009-06, Vol.44 (6), p.1063-1068

2009

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Discovery of Benzisoxazoles as Potent Inhibitors of Chaperone Heat Shock Protein 90

Journal of medicinal chemistry, 2008-02, Vol.51 (3), p.373-375

2008

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Discovery of Dibenzo[c,f][2,7]naphthyridines as Potent and Selective 3-Phosphoinositide-Dependent Kinase-1 Inhibitors

Journal of medicinal chemistry, 2007-11, Vol.50 (23), p.5547-5549

2007

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Identification and SAR of a new series of thieno[3,2- d]pyrimidines as Tpl2 kinase inhibitors

Bioorganic & medicinal chemistry letters, 2011-10, Vol.21 (19), p.5952-5956

2011

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A library approach to rapidly discover photoaffinity probes of the mRNA decapping scavenger enzyme DcpS

Molecular bioSystems, 2015-01, Vol.11 (10), p.2709-2712

2015

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Photocatalyzed Decarboxylative Addition of N‑Substituted Acetic Acids to Aldehydes

Journal of organic chemistry, 2023-02, Vol.88 (3), p.1327-1330

2023

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Identification of iminooxothiazolidines as secreted frizzled related protein-1 inhibitors

Bioorganic & medicinal chemistry letters, 2009-11, Vol.19 (22), p.6337-6339

2009

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Synthetic lethality: targeting SMARCA2 ATPase in SMARCA4-deficient tumors - a review of patent literature from 2019-30 June 2023

Expert opinion on therapeutic patents, 2024-03, Vol.34 (3), p.159-169

2024

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Synthetic lethality: targeting the SMARCA2 bromodomain for degradation in SMARCA4-deficient tumors - a review of patent literature from 2019-June 2023

Expert opinion on therapeutic patents, 2024-04, Vol.34 (4), p.1-229

2024

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Novel Nonnucleoside Inhibitor of Hepatitis C Virus RNA-Dependent RNA Polymerase

Antimicrobial Agents and Chemotherapy, 2004-12, Vol.48 (12), p.4813-4821

2004

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Synthesis of Benzothiazinones from Benzoyl Thiocarbamates: Application to Clinical Candidates for Tuberculosis Treatment

European journal of organic chemistry, 2022-09, Vol.2022 (34), p.n/a

2022

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Photoredox Catalysis: 1,4-Conjugate Addition of N‑Methyl Radicals to Electron-Deficient Olefins via Decarboxylation of N‑Substituted Acetic Acids

Organic letters, 2020-05, Vol.22 (9), p.3418-3422

2020

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PF-07059013: A Noncovalent Modulator of Hemoglobin for Treatment of Sickle Cell Disease

Journal of medicinal chemistry, 2021-01, Vol.64 (1), p.326-342

2021

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CHAPTER 3 - Anti-Inflammatory Drugs

Pain therapeutics : current and future treatment paradigms, 2014, p.105-130

2014

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Design and optimization of a series of 4-(3-azabicyclo[3.1.0]hexan-3-yl)pyrimidin-2-amines: Dual inhibitors of TYK2 and JAK1

Bioorganic & medicinal chemistry, 2020-05, Vol.28 (10), p.115481-115481, Article 115481

2020

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Binding site elucidation and structure guided design of macrocyclic IL-17A antagonists

Scientific reports, 2016-08, Vol.6 (1), p.30859-30859, Article 30859

2016

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Design and synthesis of oxadiazolidinediones as inhibitors of plasminogen activator inhibitor-1

Bioorganic & medicinal chemistry letters, 2004-07, Vol.14 (13), p.3477-3480

2004

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Selectivity through Targeted Protein Degradation (TPD)

Selectivity through Targeted Protein Degradation (TPD): Miniperspective

Covalent Enzyme Inhibition through Fluorosulfate Modification of a Noncatalytic Serine Residue

Rational Targeting of Active-Site Tyrosine Residues Using Sulfonyl Fluoride Probes

Cellular thermal shift and clickable chemical probe assays for the determination of drug-target engagement in live cells

Dual Inhibition of TYK2 and JAK1 for the Treatment of Autoimmune Diseases: Discovery of (( S)-2,2-Difluorocyclopropyl)((1 R,5 S)-3-(2-((1-methyl-1 H-pyrazol-4-yl)amino)pyrimidin-4-yl)-3,8-diazabicyclo[3.2.1]octan-8-yl)methanone (PF-06700841)

Identification of pyrimidine derivatives as hSMG-1 inhibitors

In vitro and in vivo effects of 2,4 diaminoquinazoline inhibitors of the decapping scavenger enzyme DcpS: Context-specific modulation of SMN transcript levels

A small molecule inhibitor of the Wnt antagonist secreted frizzled-related protein-1 stimulates bone formation

Discovery of Benzisoxazoles as Potent Inhibitors of Chaperone Heat Shock Protein 90

Discovery of Dibenzo[c,f][2,7]naphthyridines as Potent and Selective 3-Phosphoinositide-Dependent Kinase-1 Inhibitors

Identification and SAR of a new series of thieno[3,2- d]pyrimidines as Tpl2 kinase inhibitors

A library approach to rapidly discover photoaffinity probes of the mRNA decapping scavenger enzyme DcpS

Photocatalyzed Decarboxylative Addition of N‑Substituted Acetic Acids to Aldehydes

Identification of iminooxothiazolidines as secreted frizzled related protein-1 inhibitors

Synthetic lethality: targeting SMARCA2 ATPase in SMARCA4-deficient tumors - a review of patent literature from 2019-30 June 2023

Synthetic lethality: targeting the SMARCA2 bromodomain for degradation in SMARCA4-deficient tumors - a review of patent literature from 2019-June 2023

Novel Nonnucleoside Inhibitor of Hepatitis C Virus RNA-Dependent RNA Polymerase

Synthesis of Benzothiazinones from Benzoyl Thiocarbamates: Application to Clinical Candidates for Tuberculosis Treatment

Photoredox Catalysis: 1,4-Conjugate Addition of N‑Methyl Radicals to Electron-Deficient Olefins via Decarboxylation of N‑Substituted Acetic Acids

PF-07059013: A Noncovalent Modulator of Hemoglobin for Treatment of Sickle Cell Disease

CHAPTER 3 - Anti-Inflammatory Drugs

Design and optimization of a series of 4-(3-azabicyclo[3.1.0]hexan-3-yl)pyrimidin-2-amines: Dual inhibitors of TYK2 and JAK1

Binding site elucidation and structure guided design of macrocyclic IL-17A antagonists

Design and synthesis of oxadiazolidinediones as inhibitors of plasminogen activator inhibitor-1

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