kinases (GRKs) and subsequent recruitment of β-arrestins, resulting in receptor internalization into endosomes has been extended by discovering that some internalized GPCRs continue to signal via G proteins from endosomes the parathyroid hormone (PTH) type 1 receptor (PTHR), which engages on sustained cAMP signaling from endosomes This mini-review discusses recent insights into the mechanisms of PTHR endosomal signaling and its physiological

protein complex in neurotransmitter release has been well characterized, the mechanisms that modulate the delivery molecular players, including SNARE proteins; here, SNARE proteins play a role in the fusion of recycling endosomes

GPCRs, G proteins, and arrestins on endosomal membranes3,4. Furthermore, targeting GPCRs in specific cellular compartments requires precise delivery mechanisms to This may involve the development of specialized delivery vehicles, such as nanoparticles or liposomes expressed in cellular compartments require innovative approaches to overcome barriers related to stability, delivery Towards a molecular understanding of endosomal trafficking by Retromer and Retriever.

the cellular biology of G protein-coupled receptors (GPCRs) about a novel biosensor shed light on the endosomal , published in Nature Chemical Biology, highlights the role of the chaperone protein DNAJC13 in the endosomal-lysosomal During this process, APEX2 can label proteins in the vicinity, allowing the capture of a snapshot of the endosomal Finally, this analysis provided insights into the molecular composition of the endosomal environment

The signaling profile of CXCR3 changes as it traffics from the plasma membrane to endosomes in a ligand-specific Endosomal signaling is critical for biased activation of G proteins, β-arrestins, and extracellular-signal-regulated

HEK293 and Huh-7-Lunet cells after activation by glucagon within 5 min and transit via EEA1-marked endosomes Together, these results implicate the endosomal signaling paradigm in metabolic regulation by glucagon

arrestin have been classified as "class A" GPCRs whereas "class B" GPCRs co-internalize with arrestin into endosomes

Bianca Plouffe and their colleagues' research on 'β-arrestin-dependent and -independent endosomal GPCR GPCR Activation and Signaling β-Arrestin-dependent and -independent endosomal G protein activation by

for their study on the Role of the V2R-βarrestin-Gβγ complex in promoting G protein translocation to endosomes Rhodnius Prolixus (Stål ) Role of the V2R-βarrestin-Gβγ complex in promoting G protein translocation to endosomes

relevant to schizophrenia' Carole Daly and their team research on 'β-arrestin-dependent and -independent endosomal Angiotensin Receptors Promote Collagen Secretion in Myofibroblasts β-arrestin-dependent and -independent endosomal

Using fast recycling, slow recycling, and late endosomal recycling markers, CCR2 was also shown to be rapidly sorted into fast-recycling Rab4-positive endosomes in a more sustained manner compared to the atypical scavenging receptor ACKR3, and Rab7-positive late endosomes.

Cheng, JoAnn Trejo, et al. for their research on Ubiquitin-driven GPCR Inflammatory Signaling at the Endosome structural determinants thereof Ubiquitin-driven G Protein-Coupled Receptor Inflammatory Signaling at the Endosome

We further showed the intracellular trafficking and targeting process of F-Hst1, in which early endosome

in vivo Cryo-EM advances in GPCR structure determination Visualization of endogenous G proteins on endosomes

Therapeutic antagonism of the neurokinin 1 receptor in endosomes provides sustained pain relief.

Research G protein-coupled receptor (GPCR) pharmacogenomics Visualization of endogenous G proteins on endosomes

GPCR Activation and Signaling Endosome positioning coordinates spatially selective GPCR signaling.

Integrative Biophysical Approach Redox-modulated SNX25 as a novel regulator of GPCR-G protein signaling from endosomes

signaling at the constitutively active orphan G protein-coupled receptor GPR52 β-Arrestin-independent endosomal

State-dependent dynamics of extramembrane domains in the β2 -adrenergic receptor β-Arrestin-independent endosomal

Endosomal signaling via cAMP in parathyroid hormone (PTH) type 1 receptor biology β-arrestin1 is an E3

Classified GPCR News from April 15th to 21st, 2024 GPCR Activation and Signaling Beneath the surface: endosomal

GPCR Activation and Signaling Therapeutic antagonism of the neurokinin 1 receptor in endosomes provides

increases β-arrestin signaling at the constitutively active orphan G protein-coupled receptor GPR52 Endosome

lysophosphatidic acid (LPA) and smoothened (Smo) receptors to initiate new drug-screening strategies and targeted delivery

Odorants, the natural ligands, could potentially be used as ligands and particular forms of odorant delivery drive receptor inactivation or activation of the receptor to destroy tumor cells or be used in drug delivery

GPCRs in Oncology and Immunology GPR143 controls ESCRT-dependent exosome biogenesis and promotes cancer

indications where potent receptor activation is required, they are also highly effective vehicles for payload delivery Orion has demonstrated that this target cell-specific delivery cannot be achieved using the native ligand Figure 4: Payload delivery using Orion’s superagonist analogs on target cells expressing CCR5. molecules for indications where subtle tuning of receptor signaling is required, or as vehicles for payload delivery