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A lipidated peptide derived from the C-terminal tail of the vasopressin 2 receptor shows promise as a new β-arrestin inhibitor.
Pharmacol Res
January 2025
Department of Pharmacology-Physiology, Faculty of Medicine and Health Sciences, Université de Sherbrooke, Sherbrooke, QC, Canada; Institut de Pharmacologie de Sherbrooke, Université de Sherbrooke, Sherbrooke, QC, Canada; RECITAL International Partnership Lab, Université de Caen-Normandie, Caen, France & Université de Sherbrooke, Sherbrooke, QC, Canada. Electronic address:
β-arrestins play pivotal roles in seven transmembrane receptor (7TMR) signalling and trafficking. To study their functional role in regulating specific receptor systems, current research relies mainly on genetic tools, as few pharmacological options are available. To address this issue, we designed and synthesised a novel lipidated phosphomimetic peptide inhibitor targeting β-arrestins, called ARIP, which was developed based on the C-terminal tail (A343-S371) of the vasopressin V2 receptor.
View Article and Find Full Text PDFN-terminal fragment shedding contributes to signaling of the full-length adhesion receptor ADGRL3.
J Biol Chem
January 2025
Department of Psychiatry, Columbia University Vagelos College of Physicians and Surgeons, New York, NY, USA; Department of Molecular Pharmacology and Therapeutics, Columbia University Vagelos College of Physicians and Surgeons, New York, NY, USA; Division of Molecular Therapeutics, New York State Psychiatric Institute, New York, NY, USA. Electronic address:
Most adhesion GPCRs undergo autoproteolytic cleavage during receptor biosynthesis, resulting in non-covalently bound N- and C-terminal fragments (NTF and CTF) that remain associated during receptor trafficking to the plasma membrane. While substantial evidence supports increased G protein signaling when just the CTF is expressed, there is an ongoing debate about whether NTF removal is required to initiate signaling in the context of the wild-type receptor. Here, we use adhesion GPCR latrophilin-3 (ADGRL3) as a model receptor to investigate tethered agonist-mediated activation.
View Article and Find Full Text PDFGeneric residue numbering of the GAIN domain of adhesion GPCRs.
Nat Commun
January 2025
Institute for Medical Physics and Biophysics, Leipzig University, Medical Faculty, Leipzig, Germany.
The GPCR autoproteolysis inducing (GAIN) domain is an ancient protein fold ubiquitous in adhesion G protein-coupled receptors (aGPCR). It contains a tethered agonist necessary and sufficient for receptor activation. The GAIN domain is a hotspot for pathological mutations.
View Article and Find Full Text PDFLeveraging long-acting IL-15 agonists for intratumoral delivery and enhanced antimetastatic activity.
Front Immunol
November 2024
ProLynx Inc., San Francisco, CA, United States.
Article Synopsis
- IL-15 agonists are promising immunotherapy options as they boost the growth of immune cells like natural killer (NK) and CD8 T cells, but they have a short duration in the body requiring frequent doses.
- A new approach using hydrogel microspheres (MS) was developed to extend the half-life of IL-15, which successfully increased its duration to about one week.
- The study found that the MS conjugate of another IL-15 agonist, RLI, had a shorter half-life of 30 hours and was effective in stimulating immune cells, but caused significant injection-site toxicity; thus, it was focused on for intra-tumoral therapy where such effects could be potentially beneficial.
Regulatory mechanisms of steroid hormone receptors on gene transcription through chromatin interaction and enhancer reprogramming.
Cell Oncol (Dordr)
December 2024
Gene Regulation and Diseases Lab, College of Life Science and Technology, College of Biomedicine and Health, Huazhong Agricultural University, Wuhan, 430070, PR China.
Article Synopsis
- The regulation of steroid hormone receptors (SHRs) is essential for understanding how breast cancer progresses, particularly through their impact on gene transcription and chromatin remodeling.
- The review focuses on the roles of androgen receptor (AR), progesterone receptor (PR), and glucocorticoid receptor (GR) in influencing estrogen receptor (ER)-mediated transcription and highlights their dual roles in either promoting or inhibiting gene expression.
- It also discusses four mechanisms of enhancer reprogramming and suggests that combining SHR modulating therapies with current endocrine treatments could enhance the effectiveness of therapies for ER-positive breast cancer.
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