Targeting Intracellular Allosteric Sites in GPCRs
Exploring the intracellular allosteric site GPCRs represent one of the largest and most vital families of cell surface receptors, playing...
top of page
Ecosystem
Beta Site
Blog: Blog2
GPCR News
Search
Inês Pinheiro
- Aug 21, 2023
- 5 min
Decoding β-Arrestins: from Structure to function
Fine-tuning GPCR signaling: conformational dynamics and intracellular responses GPCR signaling is a complex process modulated by protein...
1600
Inês Pinheiro
- Jun 28, 2023
- 7 min
Structural landscape of the Chemokine Receptor system
Chemokine receptors (CKRs) belong to a subfamily of G-protein-coupled receptors (GPCRs) and play a crucial role in inflammation and...
1621
Inês Pinheiro
- May 16, 2023
- 5 min
Artificial intelligence – faster, smarter, cheaper GPCR drug discovery
Artificial intelligence - Machine learning vs Deep Learning GPCRs have long been recognized as important drug targets, and numerous drugs...
2140
Monserrat Avila-Zozaya
- Apr 21, 2023
- 3 min
VAMP2: a crucial player in the delivery of MOR to the synapse
Transporting Protein-coupled receptors (GPCRs) to the synapse, where they are involved in neurotransmission, is a complex process...
610
Inês Pinheiro
- Apr 11, 2023
- 4 min
Feeder or trigger – CCR2 as a scavenger and regulator of cell migration
Canonical chemokine receptors – scavenging “decoys” Chemokine receptors coordinate cell migration upon interaction with their cognate...
780
Inês Pinheiro
- Feb 23, 2023
- 4 min
Glyco-sulfo hotspots in the chemokine receptor system
Glycosylation and sulfation – N-terminal PTMs on chemokine receptors The interaction of chemokine receptors with their cognate chemokine...
1070
Inês Pinheiro
- Jan 13, 2023
- 4 min
Odorant receptors – a bit of smell for drug discovery
Odorant receptors function and expression landscape Odorant receptors (ORs) belong to the G protein-coupled receptor (GPCR) family and...
1580
Inês Pinheiro
- Dec 6, 2022
- 3 min
Transmembrane domains of GPCR dimers – a novel hot spot for drug discovery
Transmembrane domains of GPCR dimers – a novel hot spot for drug discovery G-protein-coupled receptors (GPCRs) can form biologically...
2080
GPCR News
- Nov 1, 2022
- 1 min
Emerging approaches for decoding neuropeptide transmission
November 2022 "Neuropeptides produce robust effects on behavior across species, and recent research has benefited from advances in...
160
GPCR News
- Nov 1, 2022
- 1 min
Location bias contributes to functionally selective responses of biased CXCR3 agonists
November 2022 "Some G protein-coupled receptor (GPCR) ligands act as "biased agonists" that preferentially activate specific signaling...
400
GPCR News
- Nov 1, 2022
- 1 min
Deciphering the signaling mechanisms of β-arrestin1 and β-arrestin2 in regulation of cancer cell...
November 2022 Deciphering the signaling mechanisms of β-arrestin1 and β-arrestin2 in regulation of cancer cell cycle and metastasis...
190
GPCR News
- Nov 1, 2022
- 1 min
Structure-Based Discovery of Negative Allosteric Modulators of the Metabotropic Glutamate Receptor 5
November 2022 "Recently determined structures of class C G protein-coupled receptors (GPCRs) revealed the location of allosteric binding...
280
GPCR News
- Nov 1, 2022
- 1 min
Structural insights into adhesion GPCR ADGRL3 activation and Gq, Gs, Gi, and G12 coupling
November 2022 "Adhesion G-protein-coupled receptors (aGPCRs) play key roles in a diversity of physiologies. A hallmark of aGPCR...
270
GPCR News
- Nov 1, 2022
- 1 min
Conservation of Allosteric Ligand Binding Sites in G-Protein Coupled Receptors
November 2022 "Despite the growing number of G protein-coupled receptor (GPCR) structures, only 39 structures have been cocrystallized...
190
GPCR News
- Nov 1, 2022
- 1 min
Dimerization of β2-adrenergic receptor is responsible for the constitutive activity subjected to inv
November 2022 "Dimerization of beta 2-adrenergic receptor (β2-AR) has been observed across various physiologies. However, the function of...
610
GPCR News
- Oct 1, 2022
- 1 min
High hedgehog signaling is transduced by a multikinase-dependent switch controlling the...
October 2022 High hedgehog signaling is transduced by a multikinase-dependent switch controlling the apico-basal distribution of the GPCR...
100
GPCR News
- Oct 1, 2022
- 1 min
Structure of the vasopressin hormone-V2 receptor-β-arrestin1 ternary complex
October 2022 "Arrestins interact with G protein-coupled receptors (GPCRs) to stop G protein activation and to initiate key signaling...
90
GPCR News
- Oct 1, 2022
- 1 min
Dual loss of regulator of G protein signaling 2 and 5 exacerbates ventricular myocyte arrhythmias...
October 2022 Dual loss of regulator of G protein signaling 2 and 5 exacerbates ventricular myocyte arrhythmias and disrupts the...
30
GPCR News
- Oct 1, 2022
- 1 min
Mechanistic basis of GPCR activation explored by ensemble refinement of crystallographic structures
October 2022 "G protein-coupled receptors (GPCRs) are important drug targets characterized by a canonical seven transmembrane (TM) helix...
60
Become a Member
Individuals
Organizations