Results 291 to 300 of about 113,722 (335)

Astroglial CB1 Reveal Sex‐Specific Synaptic Effects of Amphetamine

Glia, Volume 73, Issue 8, Page 1673-1691, August 2025.
Main Points Astroglial CB1 mediate long‐term depression in the NAc through purine release. Amphetamine occludes LTD in male mice by inducing the saturation of A1 receptors. Astroglial CB1 mediate behavioral amphetamine effects in males, but not in females.
Yamuna Mariani, Tommaso Dalla‐Tor, Tommaso Garavaldi, Francisca Julio‐Kalajzić, Doriane Gisquet, Paula Gomez‐Sotres, Astrid Cannich, Giuditta Gambino, Filippo Drago, Roman Serrat, Imane Hurel, Francis Chaouloff, Sandrine Pouvreau, Luigi Bellocchio, Giovanni Marsicano, Ana Covelo   +15 more
wiley   +1 more source

DeorphaNN: Virtual screening of GPCR peptide agonists using AlphaFold-predicted active-state complexes and deep learning embeddings

Ferguson L, Ouellet S, Vandewyer E, Wang C, Wunna Z, Lim TK, Schafer WR, Beets I.   +7 more
europepmc   +1 more source

Large scale investigation of GPCR molecular dynamics data uncovers allosteric sites and lateral gateways. [PDF]

Nat Commun
Aranda-García D, Stepniewski TM, Torrens-Fontanals M, García-Recio A, Lopez-Balastegui M, Medel-Lacruz B, Morales-Pastor A, Peralta-García A, Dieguez-Eceolaza M, Sotillo-Nuñez D, Ding T, Drabek M, Jacquemard C, Jakowiecki J, Jespers W, Jiménez-Rosés M, Jun-Yu-Lim V, Nicoli A, Orzel U, Shahraki A, Tiemann JKS, Ledesma-Martin V, Nerín-Fonz F, Suárez-Dou S, Canal O, Pándy-Szekeres G, Mao J, Gloriam DE, Kellenberger E, Latek D, Guixà-González R, Gutiérrez-de-Terán H, Tikhonova IG, Hildebrand PW, Filizola M, Babu MM, Di Pizio A, Filipek S, Kolb P, Cordomi A, Giorgino T, Marti-Solano M, Selent J.   +42 more
europepmc   +1 more source

Efficacy of IDOR‐1117‐2520, a novel, orally available CCR6 antagonist in preclinical models of skin dermatitis

British Journal of Pharmacology, Volume 182, Issue 15, Page 3452-3475, August 2025.
Background and Purpose The chemokine receptor CCR6 guides pathogenic T17 cells, implicated in autoimmune diseases including psoriasis, to sites of inflammation via the chemokine CCL20. Therefor, pharmacological inhibition of CCR6+ immune cell migration provides a novel therapeutic approach.
Paulina Kulig, Pijus Brazauskas, Madeleine Suffiotti, Emilie Raoult, Ulrike Babilonski, Bérengère Renault, Ursula Grieder, Enrico Vezzali, Peter Blattmann, Marianne M. Martinic, Mark J. Murphy   +10 more
wiley   +1 more source

P-Rex1 Limits the Agonist-Induced Internalisation of GPCRs Independently of its Rac-GEF Activity

Baker MJ, Hampson E, Islam P, Pelaez Moral R, Maunders EA, Hornigold K, Tsonou E, Hornigold DC, Hubbard RE, Massey AJ, Welch HCE.   +10 more
europepmc   +1 more source

Dimerisation of the VIP receptor VIPR2 is essential to its binding VIP and Gαi proteins, and to its functions in breast cancer cells

British Journal of Pharmacology, Volume 182, Issue 15, Page 3612-3627, August 2025.
Abstract Background and Purpose Several G protein‐coupled receptors (GPCRs) are known to homodimerise. Dimeric GPCRs may have different properties from their monomers, but the molecular basis and functional significance of GPCR dimerisation remain largely unknown.
Satoshi Asano, Kairi Ozasa, Teru Uehara, Rei Yokoyama, Takanobu Nakazawa, Souichi Yanamoto, Yukio Ago   +6 more
wiley   +1 more source

The Hunt for the Putative Epoxyeicosatrienoic Acid Receptor. [PDF]

ACS Chem Biol
Arnold WR, Jain S, Sinha V, Das A.
europepmc   +1 more source

Advancing antihypertensive drug development

British Journal of Pharmacology, Volume 182, Issue 15, Page 3389-3410, August 2025.
Hypertension affects more than a billion individuals worldwide and remains a major cause of cardiovascular morbidity and mortality. Despite advances in therapies, optimal blood pressure control remains elusive for many patients because of treatment resistance, adverse effects, and adherence challenges.
Fay Pu, Yanrong Liu, Fozia Zahir Ahmed, Xin Wang, Darren Green, Hongyuan Zhang   +5 more
wiley   +1 more source

Single-molecule localization microscopy as a tool to quantify di/oligomerization of receptor tyrosine kinases and G protein-coupled receptors. [PDF]

Mol Pharmacol
Sharrocks KL, Swaih AM, Hanyaloglu AC.
europepmc   +1 more source

Absence of Functional Autoantibodies Targeting Angiotensin II Receptor Type 1 and Endothelin‐1 Type A Receptor in Circulation and Purified IgG From Patients With Systemic Sclerosis

Arthritis &Rheumatology, Volume 77, Issue 7, Page 901-913, July 2025.
Objective Systemic sclerosis (SSc) is a rare but severe autoimmune disease characterized by immune dysregulation, fibrosis, and vasculopathy. Although previous studies have highlighted the presence of functional autoantibodies targeting the angiotensin II receptor type 1 (AT1) and endothelin‐1 type A receptor (ETAR), leading to autoantibody‐mediated ...
Wieke M. van Oostveen, Eva M. Hoekstra, E. W. Nivine Levarht, Ilana B. Kotliar, Thomas P. Sakmar, René E. M. Toes, Jeska K. de Vries‐Bouwstra, Laura H. Heitman, Cynthia M. Fehres   +8 more
wiley   +1 more source