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494 items found for "Bcl-2"
- Unlocking Cell's Secrets: Spontaneous β-Arrestin-Membrane Preassociation Drives Receptor-Activation
activation, then regulate trigger receptor internalization via interaction with the adaptor protein 2 J., & Calebiro, D. (2023). Cell, 186(10), 2238–2255.e20. https://doi.org/10.1016/j.cell.2023.04.018 Janetzko, J., Kise, R., Barsi-Rhyne Neurosci. 2, 727–733. https://doi.org/10.1038/35094577. Pharmacology & therapeutics, 89(2), 139–147. https://doi.org/10.1016/s0163-7258(00)00107-8
- 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
- Decoding β-Arrestins: from Structure to function
for receptor internalization. β-Arrestins facilitate this process by interacting with adapter protein 2 (AP-2) and clathrin. F et al. 2021, Chen, H. et al. 2022). This includes proteins like AP-2 and clathrin, vital for internalization, as well as MAPK cascade kinases In addition, the question of whether β-arrestin1 and 2 serve overlapping or distinct functions remains
- Molecular insights into regulation of constitutive activity by RNA editing 5HT2C serotonin receptor
September 2022 "RNA editing is a process by which post-transcriptional changes of mRNA nucleotides alter The 5HT2C serotonin receptor, which undergoes 32 distinct RNA-editing events leading to 24 protein isoforms We also provide a comprehensive analysis of agonist activation and constitutive activity across all 24 Collectively, these findings reveal a unique hydrogen-bonding network located on intracellular loop 2
- PLC-IP3-ORAI pathway participates in the activation of the MRGPRB2 receptor in mouse peritoneal...
September 2022 PLC-IP3-ORAI pathway participates in the activation of the MRGPRB2 receptor in mouse peritoneal and voltage-dependent current caused by MRGPRB2 activation were blocked by U73122 (PLC blocker) or 2-
- Unlocking the Future of Medicine: Advancements in GPCR Research
📰 GPCR Weekly News, July 15 to 21, 2024 Hey everyone! The required elements of a comprehensive and effective GPCR Discovery. 2. to 25, 2024 . in drug discovery October 2024 | Biologics US 2024 October 2 - 4, 2024 | 9th GPCRs in Medicinal Chemistry October 23 - 25, 2024 | 11th Adhesion GPCR Workshop July 12 - 17, 2026 | 20th World Congress of Basic
- Artificial intelligence – faster, smarter, cheaper GPCR drug discovery
established AI framework which involves three stages: 1) feature extraction or pattern identification; 2) structural data (from X-ray crystallography, cryoEM or molecular dynamics simulation experiments). 2. ; Kuang, Feng, Hu, Wang, He & Kong, 2016). 5. this field: 1) the quality and availability of data can be a challenge in AI-driven drug discovery; 2) accessibility of databases to a wider audience will encourage the development of new ideas and methods. 2.
- Molecular mechanism of allosteric modulation for the cannabinoid receptor CB1
September 2022 "Given the promising clinical value of allosteric modulators of G protein-coupled-receptors These structures show that ZCZ011 binds to an extrahelical site in the transmembrane 2 (TM2)-TM3-TM4
- Allosteric Effect of Nanobody Binding on Ligand-Specific Active States of the β2 Adrenergic Receptor
Besides, ligand-specific subtle differences in the conformations assumed by intracellular loop 2 and extracellular loop 2 are captured from the trajectories of various ligand-bound receptors in the presence
- Regulation of pulmonary surfactant by the adhesion GPCR GPR116/ADGRF5 requires a tethered agonist...
October 2022 Regulation of pulmonary surfactant by the adhesion GPCR GPR116/ADGRF5 requires a tethered conserved amino acids for GPR116 activation in the tethered agonist sequence and in extracellular loops 2/
- Fluorescent Ligands Targeting Intracellular Allosteric Binding Site of the Chemokine Receptor CCR2
August 2022 "Fluorescently labeled ligands are versatile molecular tools to study G protein-coupled receptors fluorescent ligands targeting the intracellular allosteric binding site (IABS) of the CC chemokine receptor 2
- California gold rush for Sosei Heptares
November 2021 "Cambridge’s Japanese-owned life sciences company Sosei Heptares has clinched a lucrative Neurocrine Biosciences anticipates initiating a Phase 2 study with the selective M4 agonist HTL-0016878 in schizophrenia in 2022 and Phase 1 studies for a dual M1/M4 and selective M1 agonist in 2023."
- Ligands can differentially and temporally modulate GPCR interaction with 14-3-3 isoforms
September 2022 "GPCR signaling and function depend on their associated proteins and subcellular locations decreasing agonist-induced GPCR/14-3-3 signal intensity could also be paralleled with GPCR/β-arrestin-2
- GPCR kinase phosphorylation of distal C-tail sites specifies βarrestin1-mediated signaling by...
September 2022 "G protein-coupled receptor (GPCR) kinases (GRKs) and arrestins mediate GPCR desensitization to βarr1 and focal adhesion kinase phosphorylation but not extracellular signal-regulated kinase 1/2
- The Bile Acid Membrane Receptor TGR5 in Cancer: Friend or Foe?
September 2022 "The G-protein-coupled bile acid receptor, Gpbar1 or TGR5, is characterized as a membrane protein kinase B (AKT), nuclear factor kappa-B (NF-κB), extracellular regulated protein kinases (ERK1/2)
- GB83, an Agonist of PAR2 with a Unique Mechanism of Action Distinct from Trypsin and PAR2-AP
October 2022 "Protease-activated receptor 2 (PAR2) is a G-protein-coupled receptor (GPCR) activated by
- Comparative study of neuropeptide signaling systems in Hemiptera
October 2022 "Numerous physiological processes in insects are tightly regulated by neuropeptides and Hormone-Related Peptides (GnRHs) system of Sternorrhyncha was differentiated from those of the other 2
- Neurocrine Biosciences Announces Positive Phase 3 Data for KINECT-HD Study Evaluating Valbenazine...
December 2021 Neurocrine Biosciences Announces Positive Phase 3 Data for KINECT-HD Study Evaluating Food and Drug Administration in 2022 SAN DIEGO, Dec. 7, 2021 /PRNewswire/ -- Neurocrine Biosciences ( evaluating the efficacy, safety and tolerability of valbenazine, a selective vesicular monoamine transporter 2
- Pharmacological Properties and Function of PxOctβ3 Octopamine Receptor in Plutella xylostella (L.)
September 2022 "The diamondback moth (Plutella xylostella) is one of the most destructive lepidopteran This ORF was also cloned and expressed in HEK-293 cells. Furthermore, the agonists naphazoline, clonidine, 2-phenethylamine, and amitraz activated the PxOctβ3
- New Resources in GPCRdb
GPCR on the 24th of June! This time, the GPCRdb team ( Dr. David Gloriam , Dr. will present and demonstrate the newest resources of the GPCRdb: 1) the new G protein resources and 2)
- Confo Therapeutics Doses First Subjects In Phase 1 Clinical Trial Of CFTX-1554 For The Treatment ...
March 2022 Confo Therapeutics Doses First Subjects In Phase 1 Clinical Trial Of CFTX-1554 For The Treatment Pain " — Confo’s first drug candidate moves into clinical development — Ghent, Belgium – March 10, 2022 first-in-human trial of their clinical candidate CFTX-1554, a novel inhibitor of the angiotensin II type 2
- Glyco-sulfo hotspots in the chemokine receptor system
, Kufavera I et al. 2017). ) by tyrosine sulfotransferase 1 or 2 (TPST1/2). The atypical chemokine receptor 2 (ACKR2), US28 and sphingosine-1-phosphate receptor 1 (S1PR1) also carry ; Casarosa P et al. 2005; Gao J et al. 2003; Fieger CB et al. 2005). ; Dyer DP et al. 2016).
- Pharmacophore-guided Virtual Screening to Identify New β 3 -adrenergic Receptor Agonists
August 2022 "Abstract The β3 -adrenergic receptor (β3 -AR) is found in several tissues such as adipose Two β3 -AR agonists are used clinically: mirabegron 1 and vibegron 2, which are indicated for overactive
- Gαs and Gαq/11 protein coupling bias of two AVPR2 mutants (R68W and V162A) that cause nephrogenic di
August 2022 Gαs and Gαq/11 protein coupling bias of two AVPR2 mutants (R68W and V162A) that cause nephrogenic diabetes insipidus "Loss-of-function mutations of the arginine vasopressin receptor 2 gene (AVPR2) cause
- C5aR2 receptor: The genomic twin of the flamboyant C5aR1
September 2022 "The complement fragment C5a is one of the most potent proinflammatory glycoproteins complexed to C-terminal peptide of C5a (meta-active) and the C5a (active), embedded to a model palmitoyl-2-
- Addex's strategic partner The Janssen Pharmaceutical Companies of Johnson & Johnson, Inc. has...
November 2021 Addex's strategic partner The Janssen Pharmaceutical Companies of Johnson & Johnson, Inc completed Phase 1 studies in Japan with JNJ-40411813 (ADX71149) " Geneva, Switzerland, November 15, 2021 ADX71149 is a selective metabotropic glutamate type 2 (mGlu2) receptor positive allosteric modulator
- Exploiting Dependence of Castration-Resistant Prostate Cancer on the Arginine Vasopressin ...
September 2022 Exploiting Dependence of Castration-Resistant Prostate Cancer on the Arginine Vasopressin AVPR1A is part of a family of GPCR's including arginine vasopressin receptor type 2 (AVPR2).
- Roles of Focal Adhesion Kinase PTK2 and Integrin αIIbβ3 Signaling in Collagen- and GPVI-Dependent...
September 2022 Roles of Focal Adhesion Kinase PTK2 and Integrin αIIbβ3 Signaling in Collagen- and GPVI-Dependent focused on disclosing the integrin-dependent roles of focal adhesion kinase (protein tyrosine kinase 2,