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Ligand-Based Competition Binding by Real-Time 19 F NMR in Human Cells

Journal of medicinal chemistry, 2024-01, Vol.67 (2), p.1115-1126

2024

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Molecular Determinants of the Anticonvulsant Felbamate Binding Site in the N-Methyl-d-Aspartate Receptor

Journal of medicinal chemistry, 2008-03, Vol.51 (6), p.1534-1545

2008

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Engineering of a Biologically Active Insulin Dimer

Journal of medicinal chemistry, 2021-12, Vol.64 (23), p.17448-17454

2021

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Synthesis and biochemical evaluation of δ(2)-isoxazoline derivatives as DNA methyltransferase 1 inhibitors

Journal of medicinal chemistry, 2011-11, Vol.54 (21), p.7663-7677

2011

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Structure-Based Drug Design and Optimization of Mannoside Bacterial FimH Antagonists

Journal of medicinal chemistry, 2010-06, Vol.53 (12), p.4779-4792

2010

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Structural Insight into the Interactions between Death-Associated Protein Kinase 1 and Natural Flavonoids

Journal of medicinal chemistry, 2015-09, Vol.58 (18), p.7400-7408

2015

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Development of Selective Phosphatidylinositol 5‑Phosphate 4‑Kinase γ Inhibitors with a Non-ATP-competitive, Allosteric Binding Mode

Journal of medicinal chemistry, 2022-02, Vol.65 (4), p.3359-3370

2022

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Discovery of a Highly Potent, Cell-Permeable Macrocyclic Peptidomimetic (MM-589) Targeting the WD Repeat Domain 5 Protein (WDR5)–Mixed Lineage Leukemia (MLL) Protein–Protein Interaction

Journal of medicinal chemistry, 2017-06, Vol.60 (12), p.4818-4839

2017

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Small Molecule Antagonists of the Interaction between the Histone Deacetylase 6 Zinc-Finger Domain and Ubiquitin

Journal of medicinal chemistry, 2017-11, Vol.60 (21), p.9090-9096

2017

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Development and Characterization of a Fluorescent Tracer for the Free Fatty Acid Receptor 2 (FFA2/GPR43)

Journal of medicinal chemistry, 2017-07, Vol.60 (13), p.5638-5645

2017

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Discovery of a Potent Small-Molecule Antagonist of Inhibitor of Apoptosis (IAP) Proteins and Clinical Candidate for the Treatment of Cancer (GDC-0152)

Journal of medicinal chemistry, 2012-05, Vol.55 (9), p.4101-4113

2012

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7‑Hydroxycoumarins Are Affinity-Based Fluorescent Probes for Competitive Binding Studies of Macrophage Migration Inhibitory Factor

Journal of medicinal chemistry, 2020-10, Vol.63 (20), p.11920-11933

2020

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5′-Silylated 3′-1,2,3-triazolyl Thymidine Analogues as Inhibitors of West Nile Virus and Dengue Virus

Journal of medicinal chemistry, 2015-05, Vol.58 (9), p.4016-4028

2015

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Proposed Allosteric Inhibitors Bind to the ATP Site of CK2α

Journal of medicinal chemistry, 2020-11, Vol.63 (21), p.12786-12798

2020

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Design and Evaluation of Peptide Dual-Agonists of GLP‑1 and NPY2 Receptors for Glucoregulation and Weight Loss with Mitigated Nausea and Emesis

Journal of medicinal chemistry, 2021-01, Vol.64 (2), p.1127-1138

2021

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Discovery of (S)‑1-(1-(Imidazo[1,2‑a]pyridin-6-yl)ethyl)-6-(1-methyl‑1H‑pyrazol-4-yl)‑1H‑[1,2,3]triazolo[4,5‑b]pyrazine (Volitinib) as a Highly Potent and Selective Mesenchymal–Epithelial Transition Factor (c-Met) Inhibitor in Clinical Development for Treatment of Cancer

Journal of medicinal chemistry, 2014-09, Vol.57 (18), p.7577-7589

2014

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Discovery, Synthesis, and Molecular Pharmacology of Selective Positive Allosteric Modulators of the δ‑Opioid Receptor

Journal of medicinal chemistry, 2015-05, Vol.58 (10), p.4220-4229

2015

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FimH Antagonists for the Oral Treatment of Urinary Tract Infections: From Design and Synthesis to in Vitro and in Vivo Evaluation

Journal of medicinal chemistry, 2010-12, Vol.53 (24), p.8627-8641

2010

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Astemizole Arrests the Proliferation of Cancer Cells by Disrupting the EZH2-EED Interaction of Polycomb Repressive Complex 2

Journal of medicinal chemistry, 2014-11, Vol.57 (22), p.9512-9521

2014

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Drug Design Targeting T‑Cell Factor-Driven Epithelial–Mesenchymal Transition as a Therapeutic Strategy for Colorectal Cancer

Journal of medicinal chemistry, 2019-11, Vol.62 (22), p.10182-10203

2019

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Diamidine Compounds for Selective Inhibition of Protein Arginine Methyltransferase 1

Journal of medicinal chemistry, 2014-03, Vol.57 (6), p.2611-2622

2014

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Discovery and Preclinical Pharmacology of a Selective ATP-Competitive Akt Inhibitor (GDC-0068) for the Treatment of Human Tumors

Journal of medicinal chemistry, 2012-09, Vol.55 (18), p.8110-8127

2012

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Selective Inhibitors of the JMJD2 Histone Demethylases: Combined Nondenaturing Mass Spectrometric Screening and Crystallographic Approaches

Journal of medicinal chemistry, 2010-02, Vol.53 (4), p.1810-1818

2010

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Ligand-Based Competition Binding by Real-Time 19 F NMR in Human Cells

Molecular Determinants of the Anticonvulsant Felbamate Binding Site in the N-Methyl-d-Aspartate Receptor

Engineering of a Biologically Active Insulin Dimer

Synthesis and biochemical evaluation of δ(2)-isoxazoline derivatives as DNA methyltransferase 1 inhibitors

Structure-Based Drug Design and Optimization of Mannoside Bacterial FimH Antagonists

Structural Insight into the Interactions between Death-Associated Protein Kinase 1 and Natural Flavonoids

Discovery and SAR of 5-(3-Chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic Acid (CX-4945), the First Clinical Stage Inhibitor of Protein Kinase CK2 for the Treatment of Cancer

Development of Selective Phosphatidylinositol 5‑Phosphate 4‑Kinase γ Inhibitors with a Non-ATP-competitive, Allosteric Binding Mode

Discovery of a Highly Potent, Cell-Permeable Macrocyclic Peptidomimetic (MM-589) Targeting the WD Repeat Domain 5 Protein (WDR5)–Mixed Lineage Leukemia (MLL) Protein–Protein Interaction

Small Molecule Antagonists of the Interaction between the Histone Deacetylase 6 Zinc-Finger Domain and Ubiquitin

Development and Characterization of a Fluorescent Tracer for the Free Fatty Acid Receptor 2 (FFA2/GPR43)

Discovery of a Potent Small-Molecule Antagonist of Inhibitor of Apoptosis (IAP) Proteins and Clinical Candidate for the Treatment of Cancer (GDC-0152)

7‑Hydroxycoumarins Are Affinity-Based Fluorescent Probes for Competitive Binding Studies of Macrophage Migration Inhibitory Factor

5′-Silylated 3′-1,2,3-triazolyl Thymidine Analogues as Inhibitors of West Nile Virus and Dengue Virus

Proposed Allosteric Inhibitors Bind to the ATP Site of CK2α

Design and Evaluation of Peptide Dual-Agonists of GLP‑1 and NPY2 Receptors for Glucoregulation and Weight Loss with Mitigated Nausea and Emesis

Discovery of (S)‑1-(1-(Imidazo[1,2‑a]pyridin-6-yl)ethyl)-6-(1-methyl‑1H‑pyrazol-4-yl)‑1H‑[1,2,3]triazolo[4,5‑b]pyrazine (Volitinib) as a Highly Potent and Selective Mesenchymal–Epithelial Transition Factor (c-Met) Inhibitor in Clinical Development for Treatment of Cancer

Discovery, Synthesis, and Molecular Pharmacology of Selective Positive Allosteric Modulators of the δ‑Opioid Receptor

FimH Antagonists for the Oral Treatment of Urinary Tract Infections: From Design and Synthesis to in Vitro and in Vivo Evaluation

Astemizole Arrests the Proliferation of Cancer Cells by Disrupting the EZH2-EED Interaction of Polycomb Repressive Complex 2

Drug Design Targeting T‑Cell Factor-Driven Epithelial–Mesenchymal Transition as a Therapeutic Strategy for Colorectal Cancer

Diamidine Compounds for Selective Inhibition of Protein Arginine Methyltransferase 1

Discovery and Preclinical Pharmacology of a Selective ATP-Competitive Akt Inhibitor (GDC-0068) for the Treatment of Human Tumors

Selective Inhibitors of the JMJD2 Histone Demethylases: Combined Nondenaturing Mass Spectrometric Screening and Crystallographic Approaches

4,5-Diarylisoxazole Hsp90 Chaperone Inhibitors: Potential Therapeutic Agents for the Treatment of Cancer

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