Rational design of agonists for bitter taste receptor TAS2R14: from modeling to bench and back

Diverse GPCRs exhibit conserved water networks for stabilization and activation

(2019) A. J. Venkatakrishnan et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Ultra-large library docking for discovering new chemotypes

(2019) Jiankun Lyu et al.   NATURE

Beyond the Flavour: The Potential Druggability of Chemosensory G Protein-Coupled Receptors

(2019) Antonella Di Pizio et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Reengineering the ligand sensitivity of the broadly tuned human bitter taste receptor TAS2R14

(2018) Stefanie Nowak et al.   BIOCHIMICA ET BIOPHYSICA ACTA-GENERAL SUBJECTS

Natural product modulators of human sensations and mood: molecular mechanisms and therapeutic potential

(2018) Tomáš Pluskal et al.   CHEMICAL SOCIETY REVIEWS

Chemosensory bitter taste receptors (T2Rs) are activated by multiple antibiotics

(2018) Appalaraju Jaggupilli et al.   FASEB JOURNAL

Structure and dynamics of GPCR signaling complexes

(2018) Daniel Hilger et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Bitter and sweet tasting molecules: It's complicated

(2018) Antonella Di Pizio et al.   NEUROSCIENCE LETTERS

Structure and dynamics of GPCR signaling complexes

(2018) Daniel Hilger et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Overcoming chemoresistance in pancreatic cancer cells: role of the bitter taste receptor T2R10

(2018) Louisa Stern et al.   Journal of Cancer

Bitterless guaifenesin prodrugs-design, synthesis, characterization, in vitro kinetics, and bitterness studies

(2018) Amin Thawabteh et al.   Chemical Biology & Drug Design

Therapeutic potential of ectopic olfactory and taste receptors

(2018) Sung-Joon Lee et al.   NATURE REVIEWS DRUG DISCOVERY

BitterDB: taste ligands and receptors database in 2019

(2018) Ayana Dagan-Wiener et al.   NUCLEIC ACIDS RESEARCH

Structure-guided development of selective M3 muscarinic acetylcholine receptor antagonists

(2018) Hongtao Liu et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Taste receptor polymorphisms and male infertility

(2017) M Gentiluomo et al.   HUMAN REPRODUCTION

Flavones modulate respiratory epithelial innate immunity: Anti-inflammatory effects and activation of the T2R14 receptor

(2017) Benjamin M. Hariri et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Structure-Based Design and Discovery of New M2 Receptor Agonists

(2017) Inbar Fish et al.   JOURNAL OF MEDICINAL CHEMISTRY

Radiolabeled Dibenzodiazepinone-Type Antagonists Give Evidence of Dualsteric Binding at the M2 Muscarinic Acetylcholine Receptor

(2017) Andrea Pegoli et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of new GPCR ligands to illuminate new biology

(2017) Bryan L Roth et al.   Nature Chemical Biology

Trends in GPCR drug discovery: new agents, targets and indications

(2017) Alexander S. Hauser et al.   NATURE REVIEWS DRUG DISCOVERY

Applying Structure-Based Drug Design Approaches to Allosteric Modulators of GPCRs

(2017) Miles Congreve et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Identification of the Beer Component Hordenine as Food-Derived Dopamine D2 Receptor Agonist by Virtual Screening a 3D Compound Database

(2017) Thomas Sommer et al.   Scientific Reports

Ligand binding modes from low resolution GPCR models and mutagenesis: chicken bitter taste receptor as a test-case

(2017) Antonella Di Pizio et al.   Scientific Reports

Probing the Binding Pocket of the Broadly Tuned Human Bitter Taste Receptor TAS2R14 by Chemical Modification of Cognate Agonists

(2016) Rafik Karaman et al.   Chemical Biology & Drug Design

Bitter taste receptors: Novel insights into the biochemistry and pharmacology

(2016) Appalaraju Jaggupilli et al.   INTERNATIONAL JOURNAL OF BIOCHEMISTRY & CELL BIOLOGY

Structure Property Relationships of Carboxylic Acid Isosteres

(2016) Pierrik Lassalas et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structure-based discovery of opioid analgesics with reduced side effects

(2016) Aashish Manglik et al.   NATURE

Structure-guided development of heterodimer-selective GPCR ligands

(2016) Harald Hübner et al.   Nature Communications

New paradigms in GPCR drug discovery

(2015) Kenneth A. Jacobson   BIOCHEMICAL PHARMACOLOGY

Promiscuity and selectivity of bitter molecules and their receptors

(2015) Antonella Di Pizio et al.   BIOORGANIC & MEDICINAL CHEMISTRY

TAS2R bitter taste receptors regulate thyroid function

(2015) Adam A. Clark et al.   FASEB JOURNAL

Evidence for a Transient Additional Ligand Binding Site in the TAS2R46 Bitter Taste Receptor

(2015) Massimo Sandal et al.   Journal of Chemical Theory and Computation

Class I odorant receptors, TAS1R and TAS2R taste receptors, are markers for subpopulations of circulating leukocytes

(2015) Agne Malki et al.   JOURNAL OF LEUKOCYTE BIOLOGY

Protein structure prediction provides comparable performance to crystallographic structures in docking-based virtual screening

(2015) Hongying Du et al.   METHODS

The importance of ligands for G protein-coupled receptor stability

(2015) Xianjun Zhang et al.   TRENDS IN BIOCHEMICAL SCIENCES

Taste receptors in innate immunity

(2014) Robert J. Lee et al.   CELLULAR AND MOLECULAR LIFE SCIENCES

Conformational restriction: an effective tactic in 'follow-on'-based drug discovery

(2014) Zengjun Fang et al.   Future Medicinal Chemistry

Computational Studies of Smell and Taste Receptors

(2014) Antonella Di Pizio et al.   ISRAEL JOURNAL OF CHEMISTRY

The bitter pill: clinical drugs that activate the human bitter taste receptor TAS2R14

(2013) Anat Levit et al.   FASEB JOURNAL

The Human Bitter Taste Receptor TAS2R10 Is Tailored to Accommodate Numerous Diverse Ligands

(2013) S. Born et al.   JOURNAL OF NEUROSCIENCE

Flufenamic acid as an ion channel modulator

(2013) Romain Guinamard et al.   PHARMACOLOGY & THERAPEUTICS

Development of Potent and Selective Inhibitors of Aldo–Keto Reductase 1C3 (Type 5 17β-Hydroxysteroid Dehydrogenase) Based on N-Phenyl-Aminobenzoates and Their Structure–Activity Relationships

(2012) Adegoke O. Adeniji et al.   JOURNAL OF MEDICINAL CHEMISTRY

Neuroscience: Hardwired for taste

(2012) Bijal P. Trivedi   NATURE

Insights into the Binding of Phenyltiocarbamide (PTC) Agonist to Its Target Human TAS2R38 Bitter Receptor

(2010) Xevi Biarnés et al.   PLoS One

Structural requirements of bitter taste receptor activation

(2010) A. Brockhoff et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Novel Flufenamic Acid Analogues as Inhibitors of Androgen Receptor Mediated Transcription

(2009) Clémentine Féau et al.   ACS Chemical Biology