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...
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Inês Pinheiro
- Aug 21
- 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...
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Inês Pinheiro
- Jun 28
- 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...
1551
Inês Pinheiro
- May 16
- 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...
1930
Monserrat Avila-Zozaya
- Apr 21
- 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...
580
Inês Pinheiro
- Apr 11
- 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...
750
Inês Pinheiro
- Feb 23
- 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...
1040
Inês Pinheiro
- Jan 13
- 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...
1520
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...
2060
GPCR News
- Oct 31, 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...
140
GPCR News
- Oct 31, 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...
370
GPCR News
- Oct 31, 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...
170
GPCR News
- Oct 31, 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...
250
GPCR News
- Oct 31, 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...
260
GPCR News
- Oct 31, 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...
150
GPCR News
- Oct 31, 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...
570
GPCR News
- Sep 30, 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...
60
GPCR News
- Sep 30, 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...
70
GPCR News
- Sep 30, 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...
20
GPCR News
- Sep 30, 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...
40