How GPCRs Engage GPCR Kinases in the First Step of Homologous Desensitization [PDF]
J.J.G. Tesmer +5 more
openalex +1 more source
Balancing Promise and Peril: Hemophilia Gene Therapy Insights
ABSTRACT Hemophilia is an inherited disorder characterized by impaired blood clotting caused by mutations in the genes responsible for producing coagulation factor (F) VIII (hemophilia A, HA) or FIX (hemophilia B, HB). Current treatment primarily relies on replacement therapy, involving frequent and costly infusions of FVIII or FIX concentrates.
Saicharan Akula +4 more
wiley +1 more source
Evaluation of leptin treatment on maintenance of body weight loss in diet‐induced obese mice
Abstract Aims To evaluate the therapeutic potential of leptin treatment for weight loss maintenance preclinically, through a systematic evaluation of leptin efficacy (a) following a period of weight loss stability (as in published clinical studies), and (b) across a range of circulating leptin concentrations achieved through a variety of different ...
Danna M. Breen +9 more
wiley +1 more source
Homologous desensitization of the human guanylate cyclase C receptor
Guanylate Cyclase C (GCC) serves as a receptor for the endogenous ligands, guanylin and uroguanylin, as well as the family of bacterial heat‐stable enterotoxins (ST), which are one of the major causes of diarrhoea the world over. We had earlier provided evidence that GCC, present in the human colonic T84 cell line, is desensitized on prolonged exposure
Bakre, Manjiri M +2 more
openaire +3 more sources
Targeting Histamine H4 Receptor in the Rostral Ventromedial Medulla to Relieve Hypertension
H4R and its downstream TRPV1 channel mediate the excitatory effect of TMN histaminergic afferent inputs on GABAergic sympathoinhibitory neurons in RVMM. Intranasal delivery of selective H4R agonist VUF 8430 suppresses renal sympathetic outflow and elicits sustained depressor and bradycardia responses in SHRs and CUMS‐induced hypertensive rats ...
Ying Shi +18 more
wiley +1 more source
Differential interaction of glimepiride and glibenclamide with the β-cell sulfonylurea receptor I. Binding characteristics [PDF]
Glimepiride is a novel sulfonylurea drug for treatment of non-insulin-dependent diabetes mellitus with higher blood sugar lowering efficacy in diabetic patients than glibenclamide raising the question whether this characteristics is in line with ...
Aguilar-Bryan +35 more
core +1 more source
The functional architecture of the acetylcholine nicotinic receptor explored by affinity labelling and site-directed mutagenesis [PDF]
The scientific community will remember Peter Läuger as an exceptional man combining a generous personality and a sharp and skilful mind. He was able to attract by his views the interest of a large spectrum of biologists concerned by the mechanism of ion ...
Bertrand, Daniel +3 more
core
Prostaglandin metabolite induces inhibition of TRPA1 and channel-dependent nociception [PDF]
BACKGROUND: The Transient Receptor Potential (TRP) ion channel TRPA1 is a key player in pain pathways. Irritant chemicals activate ion channel TRPA1 via covalent modification of N-terminal cysteines.
Barabas, Marie E +11 more
core +2 more sources
The full repertoire of Drosophila gustatory receptors for detecting an aversive compound. [PDF]
The ability to detect toxic compounds in foods is essential for animal survival. However, the minimal subunit composition of gustatory receptors required for sensing aversive chemicals in Drosophila is unknown.
Jeong, Yong Taek +6 more
core +2 more sources
GRK6 regulates the hemostatic response to injury through its rate-limiting effects on GPCR signaling in platelets. [PDF]
G protein-coupled receptors (GPCRs) mediate the majority of platelet activation in response to agonists. However, questions remain regarding the mechanisms that provide negative feedback toward activated GPCRs to limit platelet activation and thrombus ...
Benovic, Jeffrey +13 more
core +1 more source

