Ligand binding at the protein–lipid interface: strategic considerations for drug design
J Payandeh, M Volgraf - Nature Reviews Drug Discovery, 2021 - nature.com
Many drug targets are embedded within the phospholipid bilayer of cellular membranes,
including G protein-coupled receptors, ion channels, transporters and membrane-bound …
including G protein-coupled receptors, ion channels, transporters and membrane-bound …
Roles of polyunsaturated fatty acids, from mediators to membranes
T Harayama, T Shimizu - Journal of lipid research, 2020 - ASBMB
PUFAs, such as AA and DHA, are recognized as important biomolecules, but understanding
their precise roles and modes of action remains challenging. PUFAs are precursors for a …
their precise roles and modes of action remains challenging. PUFAs are precursors for a …
Structural basis for activation of CB1 by an endocannabinoid analog
K Krishna Kumar, MJ Robertson, E Thadhani… - Nature …, 2023 - nature.com
Endocannabinoids (eCBs) are endogenous ligands of the cannabinoid receptor 1 (CB1), a
G protein-coupled receptor that regulates a number of therapeutically relevant physiological …
G protein-coupled receptor that regulates a number of therapeutically relevant physiological …
Structure of formylpeptide receptor 2-Gi complex reveals insights into ligand recognition and signaling
Formylpeptide receptors (FPRs) as G protein-coupled receptors (GPCRs) can recognize
formylpeptides derived from pathogens or host cells to function in host defense and cell …
formylpeptides derived from pathogens or host cells to function in host defense and cell …
Structural insights into sphingosine-1-phosphate receptor activation
L Yu, L He, B Gan, R Ti, Q Xiao… - Proceedings of the …, 2022 - National Acad Sciences
As a critical sphingolipid metabolite, sphingosine-1-phosphate (S1P) plays an essential role
in immune and vascular systems. There are five S1P receptors, designated as S1PR1 to …
in immune and vascular systems. There are five S1P receptors, designated as S1PR1 to …
Structural basis of ligand binding modes at the human formyl peptide receptor 2
T Chen, M Xiong, X Zong, Y Ge, H Zhang… - Nature …, 2020 - nature.com
The human formyl peptide receptor 2 (FPR2) plays a crucial role in host defense and
inflammation, and has been considered as a drug target for chronic inflammatory diseases …
inflammation, and has been considered as a drug target for chronic inflammatory diseases …
Classification model for the second extracellular loop of class A GPCRs
A Nicoli, A Dunkel, T Giorgino, C de Graaf… - Journal of Chemical …, 2022 - ACS Publications
The extracellular loop 2 (ECL2) is the longest and the most diverse loop among class AG
protein-coupled receptors (GPCRs). It connects the transmembrane (TM) helices 4 and 5 …
protein-coupled receptors (GPCRs). It connects the transmembrane (TM) helices 4 and 5 …
G protein–coupled receptors in asthma therapy: pharmacology and drug action
Asthma is a heterogeneous inflammatory disease of the airways that is associated with
airway hyperresponsiveness and airflow limitation. Although asthma was once simply …
airway hyperresponsiveness and airflow limitation. Although asthma was once simply …
Pro-phagocytic function and structural basis of GPR84 signaling
GPR84 is a unique orphan G protein-coupled receptor (GPCR) that can be activated by
endogenous medium-chain fatty acids (MCFAs). The signaling of GPR84 is largely pro …
endogenous medium-chain fatty acids (MCFAs). The signaling of GPR84 is largely pro …
Molecular recognition and activation of the prostacyclin receptor by anti-pulmonary arterial hypertension drugs
The prostacyclin (PGI2) receptor (IP) is a Gs-coupled receptor associated with blood
pressure regulation, allergy, and inflammatory response. It is a main therapeutic target for …
pressure regulation, allergy, and inflammatory response. It is a main therapeutic target for …