Search Results
494 items found for "Bcl-2"
- Exendin-4 Attenuates Remodeling in the Remote Myocardium of Rats After an Acute Myocardial ...
Remodeling in the Remote Myocardium of Rats After an Acute Myocardial Infarction by Activating β-Arrestin-2, -2, β-arrestin-2, and protein phosphatase-2 (PP2A). Interestingly, Exendin-4 increased mRNA levels of MnSOD, protein levels of β-arrestin-2 and PP2A, and myocardium of rats following acute MI by attenuating β-catenin activation and activating β-arrestin-2, Besides, β-arrestin-2 can stimulate PP2A to dephosphorylation Smad3 (inhibition) and GSK3β (activation
- N-terminal alterations turn the gut hormone GLP-2 into an antagonist with gradual loss of GLP-2 ...
October 2022 N-terminal alterations turn the gut hormone GLP-2 into an antagonist with gradual loss of GLP-2 receptor selectivity towards more GLP-1 receptor interaction "Background and purpose: To fully elucidate the regulatory role of the GLP-2 system in the gut and the bones, potent and selective GLP -2 receptor (GLP-2R) antagonists are needed. or competition binding using 125 I-GLP-2(1-33)[M10Y].
- Anosmin 1 N-terminal domains modulate prokineticin receptor 2 activation by prokineticin 2
August 2022 "The X-linked form of Kallmann syndrome (KS), characterized by hypogonadotropic hypogonadism functions through the activation of the G protein-coupled receptors (GPCRs) prokineticin receptor 1 and 2 (PKR1, 2), and mutations in the PK2 and PKR2 genes are involved in the pathogenesis of KS. of PK2/PKR2 activity by anosmin 1, since this protein is able to enhance the activation of the ERK1/2 (extracellular signal-regulated kinase 1/2) pathway elicited by PK2 through PKR2.
- Function and structure of bradykinin receptor 2 for drug discovery
October 2022 "Type 2 bradykinin receptor (B2R) is an essential G protein-coupled receptor (GPCR) that
- 📰 GPCR Weekly News, May 27 to June 2, 2024
to 25, 2024. Let’s dive into the Classified GPCR News from May 27th to June 2nd, 2024. inverse agonist improves lung functioning in preclinical asthma GPCR Events, Meetings, and Webinars June 2 Mediated Signaling Networks June 25 - 29, 2024 | FENS Forum 2024 October 2024 | Biologics US 2024 October 2 - 4, 2024 | 9th GPCRs in Medicinal Chemistry October 23 - 25, 2024 | 11th Adhesion GPCR Workshop July
- 📰 GPCR Weekly News, October 2 to 8, 2023
Save the dates: November 2 - 4: We're sponsoring the GPCR Retreat and would love to meet you there! - 27, 2023 | 3rd Annual Meeting IRN I-GPCRNet November 2 - 4, 2023 | GPCR Retreat- Registration Closed November 15 - 17, 2023 | MPGPCR Conference November 20 - 23, 2023 | ASCEPT Annual Scientific Meeting February 3 - 7, 2024 | SLAS2024 International Conference and Exhibition March 23 - 24, 2024 | Ligand May 16 - 19, 2024 | ASPET 2024 May 27 - 29, 2024 | SLAS Europe 2024 Conference and Exhibition June 2
- G.CLIPS biotech is 2 years old this month!
July 2022 " G.CLIPS biotech is 2 years old today🎂.
- Developing the Cannabinoid Receptor 2 (CB2) pharmacopoeia: past, present, and future
October 2022 "Cannabinoid Receptor 2 (CB2) is a G protein-coupled receptor (GPCR) with considerable,
- Developing the Cannabinoid Receptor 2 (CB2) pharmacopeia: past, present, and future
August 2022 "Cannabinoid Receptor 2 (CB2) is a G protein-coupled receptor (GPCR) with considerable, though
- Phenylalanine 193 in Extracellular Loop 2 of the β 2-Adrenergic Receptor Coordinates β-Arrestin ...
Phenylalanine 193 in Extracellular Loop 2 of the β 2-Adrenergic Receptor Coordinates β -Arrestin Interaction The β 2-adrenergic receptor ( β 2AR) is a prototypical and extensively studied GPCR that can provide This single point mutation in extracellular loop 2 of the β 2AR is sufficient to intrinsically bias the the extracellular loops of the receptor and the extracellular pocket formed by transmembrane domains 2, Our studies reveal that F193 in extracellular loop 2 in the β2-adrenergic receptor mediates interactions
- Unlock the Future of GPCR Science: Breakthroughs and Courses Await | Sep 2 - Sep 8, 2024
Discovery Targeting G Protein-Coupled Receptors for New Therapeutic Options 📍 Boston, MA 📅 October 2 3, 2024 | 22nd Discovery on Target October 2024 | Biologics US 2024 October 2 - 4, 2024 | 9th GPCRs for GPCRs October 23 - 25, 2024 | 11th Adhesion GPCR Workshop November 5 - 7, 2024 | 16th Annual PEGS Europe NEW November 26 - 28, 2024 | GPCRs-Targeted Drug Discovery Summit Europe July 12 - 17, 2026 mechanism of some class B1 GPCR family members Structural basis of Frizzled 4 in recognition of Dishevelled 2
- 📰 GPCR Weekly News, June 26 to July 2, 2023
Let's take a quick look at the weekly Classified GPCR News from June 26th to July 2nd, 2023. , and more Noncanonical Regulation of cAMP-Dependent Insulin Secretion and Its Implications in Type 2 Structure-based pharmacophore modeling 2. (July 2 - 7, 2023). 3rd Annual Meeting IRN I-GPCRNet (October 25 - 27, 2023) GPCR Retreat (November 2 - 4, 2023) Registration
- 📰 GPCR Weekly News - January 2 to 8, 2023
GPCRs in Oncology and Immunology Vasoactive intestinal peptide receptor 2 signaling promotes breast cancer March 2023. GPCR Events, Meetings, and Webinars 2nd GPCR-Targeted Drug Discovery Summit | February 21-23, Boston. June 11-16, 2023. 19th World Congress of Basic & Clinical Pharmacology 2023. July 2 - 7. Metabolism and Pharmacokinetics PhD Opportunity - Investigation Of The Role Of The Formyl Peptide Receptor 2
- Nuclear localization of histamine receptor 2 in primary human lymphatic endothelial cells
August 2022 "Histamine exerts its physiological functions through its four receptor subtypes. In this work, we report the subcellular localization of histamine receptor 2 (H2R), a G protein-coupled
- Although the cannabinoid type-2 receptor (CB2) is highly expressed in the immune system, emerging...
September 2022 Cannabinoid type-2 receptors: An emerging target for regulating schizophrenia-relevant brain circuits "Although the cannabinoid type-2 receptor (CB2) is highly expressed in the immune system
- β-arrestin1 and 2 exhibit distinct phosphorylation-dependent conformations when coupling to the...
October 2022 β-arrestin1 and 2 exhibit distinct phosphorylation-dependent conformations when coupling However, whether β-arrestin1 and 2 respond differently for binding to the same GPCR is still unknown. advanced NanoLuc/FlAsH-based biosensors reveals distinct conformational signatures of β-arrestin1 and 2
- Lysine 101 in the CRAC Motif in Transmembrane Helix 2 Confers Cholesterol-Induced Thermal...
September 2022 Lysine 101 in the CRAC Motif in Transmembrane Helix 2 Confers Cholesterol-Induced Thermal residue in a cholesterol recognition/interaction amino acid consensus (CRAC) motif in transmembrane helix 2
- Structure of the human galanin receptor 2 bound to galanin and Gq reveals the basis of ligand...
September 2022 Structure of the human galanin receptor 2 bound to galanin and Gq reveals the basis of
- Expression pattern and clinical significance of beta 2-adrenergic receptor in oral squamous cell...
September 2022 Expression pattern and clinical significance of beta 2-adrenergic receptor in oral squamous cell carcinoma: an emerging prognostic indicator and future therapeutic target " Purpose: Beta 2-Adrenergic
- Addex Therapeutics Completes Patient Enrollment For Dipraglurant Blepharospasm Phase 2 Clinical ...
April 2022 Addex Therapeutics Completes Patient Enrollment For Dipraglurant Blepharospasm Phase 2 Clinical Study " Geneva, Switzerland, April 13, 2022 - Addex Therapeutics Ltd (SIX: ADXN, Nasdaq: ADXN), a clinical-stage discovery and development, announced today that patient enrollment has been completed in its Phase 2a
- 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 Previously, the absence of regulator of G protein signaling (RGS) 2 and 5, separately, was shown to cause
- Karuna Therapeutics Announces Positive Results from Phase 3 EMERGENT-2 Trial of KarXT in...
August 2022 Karuna Therapeutics Announces Positive Results from Phase 3 EMERGENT-2 Trial of KarXT in Schizophrenia "BOSTON--(BUSINESS WIRE)--Aug. 8, 2022-- Karuna Therapeutics , Inc. psychiatric and neurological conditions, today announced positive topline results from its Phase 3 EMERGENT-2 point reduction in the Positive and Negative Syndrome Scale (PANSS) total score compared to placebo (-21.2 statistically significant reduction of symptoms, as assessed by PANSS total score, starting at Week 2
- Lysophosphatidic Acid and Several Neurotransmitters Converge on Rho-Kinase 2 Signaling to Manage...
Lysophosphatidic Acid and Several Neurotransmitters Converge on Rho-Kinase 2 Signaling to Manage Motoneuron We hypothesized that isoform 2 of rho-kinase (ROCK2), acting as downstream GPCRs, mediates adjustment
- Lipid Modulation of a Class B GPCR: Elucidating the Modulatory Role of PI(4,5)P 2 Lipids
September 2022 "Phosphatidylinositol 4,5-bisphosphate (PI(4,5)P2) lipids have been shown to stabilize
- Cell Surface Calcium-Sensing Receptor Heterodimers: Mutant Gene Dosage Affects Ca 2+ Sensing but...
September 2022 Cell Surface Calcium-Sensing Receptor Heterodimers: Mutant Gene Dosage Affects Ca 2+ Sensing Transfected HEK-293 cells were assessed for Ca2+o -stimulated Ca2+i mobilization using mutations in either the VFT domains and/or HH bundle intraloop-2 or intraloop-3. We consider how receptor asymmetry may support the underlying mechanisms. © 2022 The Authors.
- Discovery of 3(2-aminoethyl)-thiazolidine-2,4-diones as a novel chemotype of sigma-1 receptor ligand
August 2022 "Abstract Sigma receptor is a transmembrane non-GPCR protein expressed mainly in the endoplasmic It is classified into two types: Sigma-1 (S1R) and Sigma-2 (S2R) based on their biological functions. study, we report the discovery of a novel lead compound for S1R binding, based on the thiazolidine-2,4
- G protein-coupled receptor kinase 2 is essential to enable vasoconstrictor-mediated arterial ...
G protein-coupled receptor kinase 2 is essential to enable vasoconstrictor-mediated arterial smooth muscle In VSMC, G protein-coupled receptor kinase 2 (GRK2) is known to regulate numerous vasoconstrictor GPCRs
- G protein-coupled receptor kinase type 2 and β-arrestin2: Key players in immune cell functions...
August 2022 G protein-coupled receptor kinase type 2 and β-arrestin2: Key players in immune cell functions and inflammation "G protein-coupled receptor kinase type 2 (GRK2) and β-arrestin2 are representative