Decoding Allosteric Control in Hypoxia-Inducible Factors

Monoterpenoid aryl hydrocarbon receptor allosteric antagonists protect against ultraviolet skin damage in female mice

(2023) Karolína Ondrová et al.   Nature Communications

The protein architecture and allosteric landscape of HNF4α

(2023) Fraydoon Rastinejad   Frontiers in Endocrinology

PROTAC targeted protein degraders: the past is prologue

(2022) Miklós Békés et al.   NATURE REVIEWS DRUG DISCOVERY

Identification of oleoylethanolamide as an endogenous ligand for HIF-3α

(2022) Xiaotong Diao et al.   Nature Communications

Regulation of Erythropoiesis by the Hypoxia-Inducible Factor Pathway: Effects of Genetic and Pharmacological Perturbations

(2022) Gregg L. Semenza   Annual Review of Medicine

The effect of HIF on metabolism and immunity

(2022) Cormac T. Taylor et al.   Nature Reviews Nephrology

AR study of 1,2-benzisothiazole dioxide compounds that agonize HIF-2 stabilization and EPO production

(2022) Wanbin Song et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Tapinarof for the treatment of psoriasis

(2022) Sofia Nogueira et al.   Dermatologic Therapy

Retinoic acid receptor structures: the journey from single domains to full-length complex

(2022) Fraydoon Rastinejad   JOURNAL OF MOLECULAR ENDOCRINOLOGY

Structural basis for the allosteric inhibition of hypoxia-inducible factor (HIF)-2 by belzutifan

(2022) Xintong Ren et al.   MOLECULAR PHARMACOLOGY

The Highly Potent AhR Agonist Picoberin Modulates Hh-Dependent Osteoblast Differentiation

(2022) Jana Flegel et al.   Journal of Medicinal Chemistry

Structures of NPAS4-ARNT and NPAS4-ARNT2 heterodimers reveal new dimerization modalities in the bHLH-PAS transcription factor family

(2022) Xiangnan Sun et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Cryo-EM structure of the agonist-bound Hsp90-XAP2-AHR cytosolic complex

(2022) Jakub Gruszczyk et al.   Nature Communications

Inhibition of hypoxia-inducible factor-2α in renal cell carcinoma with belzutifan: a phase 1 trial and biomarker analysis

(2021) Toni K. Choueiri et al.   NATURE MEDICINE

AHR in the intestinal microenvironment: safeguarding barrier function

(2021) Brigitta Stockinger et al.   Nature Reviews Gastroenterology & Hepatology

The aryl hydrocarbon receptor: A predominant mediator for the toxicity of emerging dioxin-like compounds

(2021) Wanglong Zhang et al.   JOURNAL OF HAZARDOUS MATERIALS

Revolution of Small Molecule Drug Discovery by Affinity Selection-Mass Spectrometry Technology

(2020) Takashi Motoyaji   CHEMICAL & PHARMACEUTICAL BULLETIN

Transitional States in Ligand-Dependent Transformation of the Aryl Hydrocarbon Receptor into Its DNA-Binding Form

(2020) Anatoly A. Soshilov et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Marked and rapid effects of pharmacological HIF-2α antagonism on hypoxic ventilatory control

(2020) Xiaotong Cheng et al.   JOURNAL OF CLINICAL INVESTIGATION

High-Throughput Screening: today’s biochemical and cell-based approaches

(2020) Vincent Blay et al.   DRUG DISCOVERY TODAY

PROTACs: New method to degrade transcription regulating proteins

(2020) Beichen Hu et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Bidirectional modulation of HIF-2 activity through chemical ligands

(2019) Dalei Wu et al.   Nature Chemical Biology

bHLH–PAS Proteins: Their Structure and Intrinsic Disorder

(2019) Marta Kolonko et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

3-[(1S,2S,3R)-2,3-Difluoro-1-hydroxy-7-methylsulfonylindan-4-yl]oxy-5-fluorobenzonitrile (PT2977), a Hypoxia-Inducible Factor 2α (HIF-2α) Inhibitor for the Treatment of Clear Cell Renal Cell Carcinoma

(2019) Rui Xu et al.   JOURNAL OF MEDICINAL CHEMISTRY

Chemical Proteomics and Phenotypic Profiling Identifies the Aryl Hydrocarbon Receptor as a Molecular Target of the Utrophin Modulator Ezutromid

(2019) Isabel V. L. Wilkinson et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

A long hypoxia-inducible factor 3 isoform 2 is a transcription activator that regulates erythropoietin

(2019) Jussi-Pekka Tolonen et al.   CELLULAR AND MOLECULAR LIFE SCIENCES

Oleoylethanolamide: A novel pharmaceutical agent in the management of obesity‐an updated review

(2018) Payahoo Laleh et al.   JOURNAL OF CELLULAR PHYSIOLOGY

Design and Activity of Specific Hypoxia-Inducible Factor-2α (HIF-2α) Inhibitors for the Treatment of Clear Cell Renal Cell Carcinoma: Discovery of Clinical Candidate (S)-3-((2,2-Difluoro-1-hydroxy-7-(methylsulfonyl)-2,3-dihydro-1H-inden-4-yl)oxy)-5-fluorobenzonitrile (PT2385)

(2018) Paul M. Wehn et al.   JOURNAL OF MEDICINAL CHEMISTRY

Tapinarof Is a Natural AhR Agonist that Resolves Skin Inflammation in Mice and Humans

(2017) Susan H. Smith et al.   JOURNAL OF INVESTIGATIVE DERMATOLOGY

Activation of intestinal hypoxia-inducible factor 2α during obesity contributes to hepatic steatosis

(2017) Cen Xie et al.   NATURE MEDICINE

Structural hierarchy controlling dimerization and target DNA recognition in the AHR transcriptional complex

(2017) Seung-Hyeon Seok et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

The quaternary architecture of RARβ–RXRα heterodimer facilitates domain–domain signal transmission

(2017) Vikas Chandra et al.   Nature Communications

Visualizing the Architectures and Interactions of Nuclear Receptors

(2016) Sepideh Khorasanizadeh et al.   ENDOCRINOLOGY

NPAS1-ARNT and NPAS3-ARNT crystal structures implicate the bHLH-PAS family as multi-ligand binding transcription factors

(2016) Dalei Wu et al.   eLife

Selective Small Molecule Induced Degradation of the BET Bromodomain Protein BRD4

(2015) Michael Zengerle et al.   ACS Chemical Biology

Surface Plasmon Resonance (SPR) Biosensors in Pharmaceutical Analysis

(2015) Andreea Olaru et al.   CRITICAL REVIEWS IN ANALYTICAL CHEMISTRY

HIF3α: the little we know

(2015) Linda Ravenna et al.   FEBS Journal

Structural integration in hypoxia-inducible factors

(2015) Dalei Wu et al.   NATURE

Tissue-based map of the human proteome

(2015) M. Uhlen et al.   SCIENCE

Nuclear receptor full-length architectures: confronting myth and illusion with high resolution

(2015) Fraydoon Rastinejad et al.   TRENDS IN BIOCHEMICAL SCIENCES

Unsaturated fatty acids as high-affinity ligands of the C-terminal Per-ARNT-Sim domain from the Hypoxia-inducible factor 3α

(2015) Angela M. Fala et al.   Scientific Reports

Vascular Endothelial Growth Factor Signaling in Hypoxia and Inflammation

(2014) S. Ramakrishnan et al.   Journal of Neuroimmune Pharmacology

AhR sensing of bacterial pigments regulates antibacterial defence

(2014) Pedro Moura-Alves et al.   NATURE

Genome-wide survey and expression analysis of the bHLH-PAS genes in the amphioxus Branchiostoma floridae reveal both conserved and diverged expression patterns between cephalochordates and vertebrates

(2014) Kun-Lung Li et al.   EvoDevo

Retinoic Acid Actions through Mammalian Nuclear Receptors

(2013) Pengxiang Huang et al.   CHEMICAL REVIEWS

Loss-of-function mutations in SIM1 contribute to obesity and Prader-Willi–like features

(2013) Amélie Bonnefond et al.   JOURNAL OF CLINICAL INVESTIGATION

Development of Inhibitors of the PAS-B Domain of the HIF-2α Transcription Factor

(2013) Jamie L. Rogers et al.   JOURNAL OF MEDICINAL CHEMISTRY

Understanding nuclear receptor form and function using structural biology

(2013) Fraydoon Rastinejad et al.   JOURNAL OF MOLECULAR ENDOCRINOLOGY

Structure and Dimerization Properties of the Aryl Hydrocarbon Receptor PAS-A Domain

(2013) D. Wu et al.   MOLECULAR AND CELLULAR BIOLOGY

Multidomain integration in the structure of the HNF-4α nuclear receptor complex

(2013) Vikas Chandra et al.   NATURE

Allosteric inhibition of hypoxia inducible factor-2 with small molecules

(2013) Thomas H Scheuermann et al.   Nature Chemical Biology

Regulating the ARNT/TACC3 Axis: Multiple Approaches to Manipulating Protein/Protein Interactions with Small Molecules

(2012) Yirui Guo et al.   ACS Chemical Biology

Identification of Cys255 in HIF-1α as a novel site for development of covalent inhibitors of HIF-1α/ARNT PasB domain protein-protein interaction

(2012) Rosa Cardoso et al.   PROTEIN SCIENCE

Crystal Structure of the Heterodimeric CLOCK:BMAL1 Transcriptional Activator Complex

(2012) N. Huang et al.   SCIENCE

Roles of the human hypoxia-inducible factor (HIF)-3α variants in the hypoxia response

(2011) Minna Heikkilä et al.   CELLULAR AND MOLECULAR LIFE SCIENCES

Npas4 Regulates a Transcriptional Program in CA3 Required for Contextual Memory Formation

(2011) K. Ramamoorthi et al.   SCIENCE

Structural Overview of the Nuclear Receptor Superfamily: Insights into Physiology and Therapeutics

(2010) Pengxiang Huang et al.   Annual Review of Physiology

Mammalian Per-Arnt-Sim Proteins in Environmental Adaptation

(2010) Brian E. McIntosh et al.   Annual Review of Physiology

Principles of Ligand Binding within a Completely Buried Cavity in HIF2α PAS-B

(2009) Jason Key et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Artificial ligand binding within the HIF2  PAS-B domain of the HIF2 transcription factor

(2009) T. H. Scheuermann et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Structure and Signaling Mechanism of Per-ARNT-Sim Domains

(2009) Andreas Möglich et al.   STRUCTURE

Interacting haplotypes at the NPAS3 locus alter risk of schizophrenia and bipolar disorder

(2008) B S Pickard et al.   MOLECULAR PSYCHIATRY