Class A GPCRs: Structure, function, modeling and structure-based ligand design

X Cong, J Topin, J Golebiowski - Current pharmaceutical …, 2017 - ingentaconnect.com
G protein-coupled receptors (GPCRs), especially the class A, are the most heavily
investigated drug targets in the pharmaceutical industry. Tremendous efforts have been …

[图书][B] Antimicrobial peptides

DA Phoenix, SR Dennison, F Harris - 2012 - books.google.com
In this text, the small team of expert authors presents the field in a comprehensive and
accessible manner that is well suited for students and junior researchers. The result is a …

Activation mechanism of the G protein-coupled sweet receptor heterodimer with sweeteners and allosteric agonists

SK Kim, Y Chen, R Abrol… - Proceedings of the …, 2017 - National Acad Sciences
The sweet taste in humans is mediated by the TAS1R2/TAS1R3 G protein-coupled receptor
(GPCR), which belongs to the class C family that also includes the metabotropic glutamate …

Structure-based discovery and binding site analysis of histamine receptor ligands

R Kiss, GM Keserű - Expert Opinion on Drug Discovery, 2016 - Taylor & Francis
Introduction: The application of structure-based drug discovery in histamine receptor
projects was previously hampered by the lack of experimental structures. The publication of …

How broadly tuned olfactory receptors equally recognize their agonists. Human OR1G1 as a test case

L Charlier, J Topin, C Ronin, SK Kim… - Cellular and molecular …, 2012 - Springer
The molecular features that dominate the binding mode of agonists by a broadly tuned
olfactory receptor are analyzed through a joint approach combining cell biology, calcium …

Structures and agonist binding sites of bitter taste receptor TAS2R5 complexed with Gi protein and validated against experiment

MY Yang, SK Kim, D Kim, SB Liggett… - The journal of …, 2021 - ACS Publications
Bitter taste receptors (TAS2Rs) function in taste perception, but are also expressed in many
extraoral tissues, presenting attractive therapeutic targets. TAS2R5s expressed on human …

Predicted structure of agonist-bound glucagon-like peptide 1 receptor, a class BG protein-coupled receptor

A Kirkpatrick, J Heo, R Abrol… - Proceedings of the …, 2012 - National Acad Sciences
The glucagon-like peptide 1 receptor (GLP1R) is a G protein-coupled receptor (GPCR)
involved in insulin synthesis and regulation; therefore, it is an important drug target for …

[HTML][HTML] Predicted structure and cell signaling of TAS2R14 reveal receptor hyper-flexibility for detecting diverse bitter tastes

A Tokmakova, D Kim, B Guthrie, SK Kim, WA Goddard… - Iscience, 2023 - cell.com
The 25 human bitter taste receptors (TAS2Rs) are expressed on taste and extra-oral cells
representing an integrated chemosensory system. The archetypal TAS2R14 is activated by> …

Predicted structure of fully activated Tas1R3/1R3′ homodimer bound to G protein and natural sugars: Structural insights into G protein activation by a class C sweet …

A Mafi, SK Kim, KC Chou, B Guthrie… - Journal of the …, 2021 - ACS Publications
The Tas1R3 G protein-coupled receptor constitutes the main component of sweet taste
sensory response in humans via forming a heterodimer with Tas1R2 or a homodimer with …

Genetically encoded photo-cross-linkers map the binding site of an allosteric drug on a G protein-coupled receptor

A Grunbeck, T Huber, R Abrol, B Trzaskowski… - ACS chemical …, 2012 - ACS Publications
G protein-coupled receptors (GPCRs) are dynamic membrane proteins that bind
extracellular molecules to transduce signals. Although GPCRs represent the largest class of …