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A current structural perspective on PXR and CAR in drug metabolism

Expert opinion on drug metabolism & toxicology, 2018-06, Vol.14 (6), p.635-647

2018

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Role of CAR and PXR in xenobiotic sensing and metabolism

Expert opinion on drug metabolism & toxicology, 2012-07, Vol.8 (7), p.803-817

2012

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SPA70 is a potent antagonist of human pregnane X receptor

Nature communications, 2017-09, Vol.8 (1), p.741-14, Article 741

2017

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Building a Chemical Toolbox for Human Pregnane X Receptor Research: Discovery of Agonists, Inverse Agonists, and Antagonists Among Analogs Based on the Unique Chemical Scaffold of SPA70

Journal of medicinal chemistry, 2021-02, Vol.64 (3), p.1733-1761

2021

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Drug discovery technologies to identify and characterize modulators of the pregnane X receptor and the constitutive androstane receptor

Drug discovery today, 2019-03, Vol.24 (3), p.906-915

2019

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A bromodomain-independent mechanism of gene regulation by the BET inhibitor JQ1: direct activation of nuclear receptor PXR

Nucleic acids research, 2024-02, Vol.52 (4), p.1661

2024

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Chemical manipulation of an activation/inhibition switch in the nuclear receptor PXR

Nature communications, 2024-05, Vol.15 (1), p.4054-14, Article 4054

2024

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Clobetasol Propionate Is a Heme-Mediated Selective Inhibitor of Human Cytochrome P450 3A5

Journal of medicinal chemistry, 2020-02, Vol.63 (3), p.1415-1433

2020

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Blocking an N-terminal acetylation-dependent protein interaction inhibits an E3 ligase

Nature chemical biology, 2017-08, Vol.13 (8), p.850

2017

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Piperine activates human pregnane X receptor to induce the expression of cytochrome P450 3A4 and multidrug resistance protein 1

Toxicology and applied pharmacology, 2013-10, Vol.272 (1), p.96-107

2013

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CINPA1 binds directly to constitutive androstane receptor and inhibits its activity

Biochemical pharmacology, 2018-06, Vol.152, p.211-223

2018

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Exploiting a water network to achieve enthalpy-driven, bromodomain-selective BET inhibitors

Bioorganic & medicinal chemistry, 2018-01, Vol.26 (1), p.25-36

2018

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Strategies for developing pregnane X receptor antagonists: Implications from metabolism to cancer

Medicinal research reviews, 2020-05, Vol.40 (3), p.1061-1083

2020

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FE(II) Is the Native Cofactor for Escherichia coli Methionine Aminopeptidase

The Journal of biological chemistry, 2008-10, Vol.283 (40), p.26879-26885

2008

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Design and Optimization of 1H‑1,2,3-Triazole-4-carboxamides as Novel, Potent, and Selective Inverse Agonists and Antagonists of PXR

Journal of medicinal chemistry, 2022-12, Vol.65 (24), p.16829-16859

2022

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Design and Optimization of 1 H -1,2,3-Triazole-4-carboxamides as Novel, Potent, and Selective Inverse Agonists and Antagonists of PXR

Journal of medicinal chemistry, 2022-12, Vol.65 (24), p.16829-16859

2022

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A current structural perspective on PXR and CAR in drug metabolism

Expert opinion on drug metabolism & toxicology, 2018-06, Vol.14 (6), p.635-647

2018

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Small-molecule modulators of PXR and CAR

Biochimica et biophysica acta, 2016-09, Vol.1859 (9), p.1141-1154

2016

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CITCO Directly Binds to and Activates Human Pregnane X Receptor

Molecular pharmacology, 2020-03, Vol.97 (3), p.180-190

2020

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Special Topics in Drug Discovery

2016

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E3 ligase autoinhibition by C-degron mimicry maintains C-degron substrate fidelity

Molecular cell, 2023-03, Vol.83 (5), p.770-786.e9

2023

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One Protein, Two Enzymes Revisited: A Structural Entropy Switch Interconverts the Two Isoforms of Acireductone Dioxygenase

Journal of molecular biology, 2006-11, Vol.363 (4), p.823-834

2006

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Novel Pyrrolopyrimidine-Based α-Helix Mimetics: Cell-Permeable Inhibitors of Protein−Protein Interactions

Journal of the American Chemical Society, 2011-02, Vol.133 (4), p.676-679

2011

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Molecular basis of crosstalk in nuclear receptors: heterodimerization between PXR and CAR and the implication in gene regulation

Nucleic acids research, 2022-04, Vol.50 (6), p.3254

2022

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Probes of the Catalytic Site of Cysteine Dioxygenase

The Journal of biological chemistry, 2006-06, Vol.281 (23), p.15774-15779

2006

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A current structural perspective on PXR and CAR in drug metabolism

Role of CAR and PXR in xenobiotic sensing and metabolism

SPA70 is a potent antagonist of human pregnane X receptor

Building a Chemical Toolbox for Human Pregnane X Receptor Research: Discovery of Agonists, Inverse Agonists, and Antagonists Among Analogs Based on the Unique Chemical Scaffold of SPA70

Drug discovery technologies to identify and characterize modulators of the pregnane X receptor and the constitutive androstane receptor

A bromodomain-independent mechanism of gene regulation by the BET inhibitor JQ1: direct activation of nuclear receptor PXR

Chemical manipulation of an activation/inhibition switch in the nuclear receptor PXR

Clobetasol Propionate Is a Heme-Mediated Selective Inhibitor of Human Cytochrome P450 3A5

Blocking an N-terminal acetylation-dependent protein interaction inhibits an E3 ligase

Piperine activates human pregnane X receptor to induce the expression of cytochrome P450 3A4 and multidrug resistance protein 1

CINPA1 binds directly to constitutive androstane receptor and inhibits its activity

Exploiting a water network to achieve enthalpy-driven, bromodomain-selective BET inhibitors

Strategies for developing pregnane X receptor antagonists: Implications from metabolism to cancer

FE(II) Is the Native Cofactor for Escherichia coli Methionine Aminopeptidase

Design and Optimization of 1H‑1,2,3-Triazole-4-carboxamides as Novel, Potent, and Selective Inverse Agonists and Antagonists of PXR

Design and Optimization of 1 H -1,2,3-Triazole-4-carboxamides as Novel, Potent, and Selective Inverse Agonists and Antagonists of PXR

A current structural perspective on PXR and CAR in drug metabolism

Small-molecule modulators of PXR and CAR

CITCO Directly Binds to and Activates Human Pregnane X Receptor

Special Topics in Drug Discovery

E3 ligase autoinhibition by C-degron mimicry maintains C-degron substrate fidelity

One Protein, Two Enzymes Revisited: A Structural Entropy Switch Interconverts the Two Isoforms of Acireductone Dioxygenase

Novel Pyrrolopyrimidine-Based α-Helix Mimetics: Cell-Permeable Inhibitors of Protein−Protein Interactions

Molecular basis of crosstalk in nuclear receptors: heterodimerization between PXR and CAR and the implication in gene regulation

Probes of the Catalytic Site of Cysteine Dioxygenase

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