The islets of Langerhans are central to appropriate glucose homeostasis through their secretion of insulin

involved in the role of GPCRs in lifespan are those that mimic dietary restriction, those related to insulin

October 2022 Recurrent hypoglycemia increases hepatic gluconeogenesis without affecting glycogen metabolism or systemic lipolysis in rat "Introduction: Recurrent hypoglycemia (RH) impairs secretion of counterregulatory hormones. Whether and how RH affects responses within metabolically important peripheral organs to counterregulatory hormones are poorly understood. Objective: To study the effects of RH on metabolic pathways associated with glucose counterregulation within liver, white adipose tissue and skeletal muscle. Methods: Using a widely adopted rodent model of 3-day recurrent hypoglycemia, we first checked expression of counterregulatory hormone G-protein coupled receptors (GPCRs), their inhibitory regulators and downstream enzymes catalyzing glycogen metabolism, gluconeogenesis and lipolysis by qPCR and western blot. Then, we examined epinephrine-induced phosphorylation of PKA substrates to validate adrenergic sensitivity in each organ. Next, we measured hepatic and skeletal glycogen content, degree of breakdown by epinephrine and abundance of phosphorylated glycogen phosphorylase under hypoglycemia and that of phosphorylated glycogen synthase during recovery to evaluate glycogen turnover. Further, we performed pyruvate and lactate tolerance tests to assess gluconeogenesis. Additionally, we measured circulating FFA and glycerol to check lipolysis. The abovementioned studies were repeated in streptozotocin-induced diabetic rat model. Finally, we conducted epinephrine tolerance test to investigate systemic glycemic excursions to counterregulatory hormones. Saline-injected rats served as controls." Read more at the source #DrGPCR #GPCR #IndustryNews

September 2022 Exploiting Dependence of Castration-Resistant Prostate Cancer on the Arginine Vasopressin prostate cancer are treated by androgen deprivation therapy but the disease recurs as incurable castration-resistant receptor (GPCR) arginine vasopressin receptor type1A (AVPR1A) is expressed in CRPC and promotes castration-resistant Furthermore, we found that castration-resistant cells produced AVP, the endogenous ligand for arginine

during bacterial infections and emphasize the contribution of the C3a–C3aR axis in regulating host resistance

links endocytic and secretory pathways via MADD, a Rab11A effector that activates Rab27B Targeting of insulin receptor endocytosis as a treatment to insulin resistance Stepwise phosphorylation of BLT1 defines complex

GPCR-dependent signaling by PM-restricted wild type αq is strongly inhibited by YM, demonstrating that resistance

agonist activation of β2-adrenergic and, potentially, CRF2 receptors appear primarily mediated by altered insulin Clenbuterol injection improved glucose tolerance by increasing insulin secretion in lean mice. UCN2 injection resulted in decreased glucose tolerance associated with lower plasma insulin levels. likely due to the fact that these receptors are also expressed by pancreatic islets where they modulate insulin

Previously, we identified potent positive crosstalk between insulin/IGF-1 receptors and G protein-coupled Here, we show that a combination of insulin and the GPCR agonist neurotensin induced rapid activation

protein (TRPA1) signaling pathways, thereby regulating proliferation, inflammation, adhesion, migration, insulin

GLP-1R, a class B1 GPCR, is integral to metabolic regulation, particularly in glucose homeostasis and insulin For example, in vivo studies in diabetic models have shown that although exendin-P5 induces lower insulin

GPCR Activation and Signaling Trans-palmitoleic acid, a dairy fat biomarker, stimulates insulin secretion Reviews, GPCRs, and more Noncanonical Regulation of cAMP-Dependent Insulin Secretion and Its Implications

Mechanistically, GASP1 inhibited proteasomal degradation of insulin-like growth factor 1 receptor (IGF1R

peptidergic systems GPCR Binders, Drugs, and more A relaxin receptor gene RpGPCR41 is involved in the resistance Anti-G-Protein-Coupled Receptor (GPCR) Antibodies Treated With Therapeutic Plasma Exchange SUCNR1 regulates insulin

receptor GPCRs in Cardiology, Endocrinology, and Taste Gβγ-SNAP25 exocytotic brake removal enhances insulin

Drugs, and more Advances in GPCR-targeted drug development in dermatology Advances in small-molecule insulin

Cardiology, Endocrinology, and Taste The Prostaglandin E2 EP3 Receptor Has Disparate Effects on Islet Insulin

Reviews, GPCRs, and more Short-chain fatty acids: possible regulators of insulin secretion.

If you're already registered, kindly use the provided form to submit your poster abstracts. You don't need to be registered to participate. PRL3-zumab humanized antibody Activation of PI3K/Akt pathway by G protein-coupled receptor 37 promotes resistance

C265 augments β2AR protein kinase A signaling, enables β2AR nitric oxide (NO) signaling, renders mice resistant

Food and Drug Administration's designation of psilocybin as a "Breakthrough Therapy" for treatment-resistant

β-adrenergic-like octopamine receptor (Octβ2R), is the unique target of amitraz, but the honeybee Octβ2R resists

Register today for the GPCR Drug Discovery Conference and save $200 with discount code “ DRGPCR24 ”. required for peripheral metabolism and systemic energy homeostasis Eiken syndrome with parathyroid hormone resistance

tools to study GPCR trafficking in real-time opens new avenues for understanding drug tolerance and resistance

therapies focuses on processes such as angiogenesis, cell signaling, stemness, metastasis, and drug resistance

Consistently, GPR84-/- mice are resistant to the development of colitis induced by DSS.

adenosine signaling and ABC transporters, which extrude drugs outside the cell, such as the multidrug resistance-associated

not only toward PAR-expressing tumors but also for treating EGFR/erbB-expressing tumors in cases of resistance