Results 41 to 50 of about 4,050 (178)

Developing the Dopamine D3 Receptor (D3R) Antagonist, (R)‐VK4‐116, as a Non‐Opioid Medication for the Treatment of Opioid Use Disorder

Medicinal Research Reviews, EarlyView.
ABSTRACT Opioid use disorder (OUD) remains a major global health challenge, and currently approved treatments (methadone, buprenorphine, and naltrexone) are all opioid receptor‐targeting drugs with limitations in access, adherence, stigma, and use in polysubstance use disorders. Because the dopamine D3 receptor (D3R) is enriched in limbic brain regions
Chia‐Kuei Wu, Yu‐Chih Lin, Junfeng Huang, Bangwei Ding, Pramod Terse, Rahul Nandre, Haksong Jin, Molly Congdon, Kun Shen, Philip Sanderson, Gregory Tawa, Stephanie Mounaud, Marta De Santis, Donald Lo, Elizabeth A. Ottinger, Amy Hauck Newman   +15 more
wiley   +1 more source

Sodium Ions Affect GPR17 Conformational States and Functionality

Proteins: Structure, Function, and Bioinformatics, EarlyView.
ABSTRACT Sodium is an allosteric modulator of several class‐A GPCR regulating active versus inactive conformation state and may be a critical issue for the optimization of crystallization procedures. Herein, the role of Na+ in the regulation of GPR17 conformational states was studied through MD simulations of GPR17 wild‐type and mutated on two ...
Luca Palazzolo, Simona Daniele, Davide Bianchi, Lara Russo, Stefano Capaldi, Maria Letizia Trincavelli, Ivano Eberini   +6 more
wiley   +1 more source

Granzyme K: A new frontier in systemic lupus erythematosus

Rheumatology &Autoimmunity, EarlyView.
The role of Granzyme K in the pathogenesis of systemic lupus erythematosus and its clinical translational significance. Abstract Systemic lupus erythematosus (SLE) is a complex autoimmune disorder driven by dysregulated adaptive and innate immunity and aberrant complement activity.
Zhongyu Chen, Yunjing Pu, Peihui Yang, Qinghuan Zhu, Haojun Long, Danqi Deng   +5 more
wiley   +1 more source

Beta‐arrestin 1 and beta‐arrestin 2 differentially direct the phosphorylation‐dependent and ‐independent internalization and desensitization of delta‐opioid receptor

The FASEB Journal, 2006
δ‐opioid receptor (DOR) and its phosphorylation‐deficient mutant S363A (DORS363A) underwent internalization and desensitization during the long‐term activation by [D‐Pen 2 ,D‐Pen 5 ]enkephalin (DPDPE).
Yu Qiu, Odile Maestri‐El Kouhen, Horace H. Loh, Ping‐Yee Law   +3 more
openaire   +1 more source

Spatiotemporal Expression of ARRDC5 in Mammalian Spermatogenesis

Andrology, EarlyView.
ABSTRACT Background Spermiogenesis is the final phase of sperm development during which haploid round spermatids transform into specialized spermatozoa and occurs across distinct stages of sperm production in the seminiferous epithelium. Abnormalities in this process lead to malformations and an inability of sperm to fertilize eggs.
LeeLa D. Robinson, Jon M. Oatley
wiley   +1 more source

Compartmentalisation in cAMP signalling: A phase separation perspective

British Journal of Pharmacology, EarlyView.
Cells rely on precise spatiotemporal control of signalling pathways to ensure functional specificity. The compartmentalisation of cyclic AMP (cAMP) and protein kinase A (PKA) signalling enables distinct cellular responses within a crowded cytoplasmic space.
Milda Folkmanaite, Manuela Zaccolo
wiley   +1 more source

Mechanism of beta-arrestin 1 mediated Src activation via Src SH3 domain revealed by cryo-electron microscopy

Nature Communications
Beta-arrestins (βarrs) are key regulators and transducers of G-protein coupled receptor signaling; however, little is known of how βarrs communicate with their downstream effectors. Here, we delineate structural mechanisms underlying βarr-mediated signal
Natalia Pakharukova, Brittany N. Thomas, Harsh Bansia, Linus Li, Dana K. Bassford, Rinat R. Abzalimov, Jihee Kim, Alem W. Kahsai, Biswaranjan Pani, Kunhong Xiao, Roni Ochakovski, Shibo Liu, Xingdong Zhang, Seungkirl Ahn, Amedee des Georges, Robert J. Lefkowitz   +15 more
doaj   +1 more source

The potential for biased signalling in the P2Y receptor family of GPCRs

British Journal of Pharmacology, EarlyView.
The purinergic receptor family is primarily activated by nucleotides, and contains members of both the G protein coupled‐receptor (GPCR) superfamily (P1 and P2Y) and ligand‐gated ion channels (P2X). The P2Y receptors are widely expressed in the human body, and given the ubiquitous nature of nucleotides, purinergic signalling is involved with a plethora
Claudia M. Sisk, Simon Pitchford, Graham Ladds   +2 more
wiley   +1 more source

PDE4D and PDE3B orchestrate distinct cAMP microdomains in 3T3‐L1 adipocytes

British Journal of Pharmacology, EarlyView.
Basal conditions: •Ins/PDE3B lowers cytoplasmic cAMP (cyt‐cAMP) without affecting plasma membrane cAMP (pm‐cAMP). •Insulin decreases lipid droplet cAMP (LD‐cAMP) independent of PDE3B. •FGF1/PDE4D modestly reduces both cyt‐ and pm‐cAMP, while PDE4D alone can modulate LD‐cAMP. ISO stimulation: •Ins/PDE3B has minimal impact on cyt‐cAMP.
Johannes Krier, David Spähn, David Arturo Juarez Lopez, Judith L. Nono, Judith Seigner, Lisa Jacob, Siegfried Ussar, Robert Lukowski, Andreas L. Birkenfeld, Gencer Sancar   +9 more
wiley   +1 more source

Cannabigerol reverses mechanical allodynia through α2A‐adrenergic modulation of thalamocortical signaling in chemotherapy‐induced neuropathy

British Journal of Pharmacology, EarlyView.
Abstract Background and Purpose Chemotherapy‐induced peripheral neuropathy (CIPN) is a prevalent and treatment‐resistant side effect of platinum‐based chemotherapy, characterised by mechanical allodynia. Cannabigerol (CBG), a non‐psychoactive cannabinoid, has shown antinociceptive potential, but its site and mechanism of action remain unclear.
Quinn W. Wade, Nathan Morris, Diana E. Sepulveda, Alonso Cortez‐Resendiz, Christopher Brandl, Jennifer E. Lausch, Mariya Starostina, Nicholas M. Graziane   +7 more
wiley   +1 more source