Results 141 to 150 of about 63,776 (234)

Ligand bias and inverse agonism on 5‐HT2A receptor‐mediated modulation of G protein activity in post‐mortem human brain

British Journal of Pharmacology, Volume 182, Issue 14, Page 3320-3335, July 2025.
Abstract Background and Purpose Whereas biased agonism on the 5‐HT2A receptor has been ascribed to hallucinogenic properties of psychedelics, no information about biased inverse agonism on this receptor is available. In schizophrenia, increased 5‐HT2A receptor constitutive activity has been suggested, highlighting the therapeutic relevance of inverse ...
Itziar Muneta‐Arrate, Patricia Miranda‐Azpiazu, Igor Horrillo, Rebeca Diez‐Alarcia, J. Javier Meana   +4 more
wiley   +1 more source

G Protein Selectivity in Dopamine Receptors is Determined before GDP Release. [PDF]

Biochemistry
Tawfeeq C, Hilibrand AS, Smith JS, Portillo J, Kruse AC, Abrol R.   +5 more
europepmc   +1 more source

ERNEST COST action overview on the (patho)physiology of GPCRs and orphan GPCRs in the nervous system

British Journal of Pharmacology, Volume 182, Issue 14, Page 3178-3210, July 2025.
G protein‐coupled receptors (GPCRs) are a large family of cell surface receptors that play a critical role in nervous system function by transmitting signals between cells and their environment. They are involved in many, if not all, nervous system processes, and their dysfunction has been linked to various neurological disorders representing important
Necla Birgül Iyison, Clauda Abboud, Dayana Abboud, Abdulrasheed O. Abdulrahman, Ana‐Nicoleta Bondar, Julie Dam, Zafiroula Georgoussi, Jesús Giraldo, Anemari Horvat, Christos Karoussiotis, Alba Paz‐Castro, Miriam Scarpa, Hannes Schihada, Nicole Scholz, Bilge Güvenc Tuna, Nina Vardjan   +15 more
wiley   +1 more source

Structural insights into ligand recognition and G protein preferences across histamine receptors. [PDF]

Commun Biol
Matsuzaki Y, Sano FK, Oshima HS, Akasaka H, Kobayashi K, Tanaka T, Itoh Y, Shihoya W, Kise Y, Kusakizako T, Inoue A, Nureki O.   +11 more
europepmc   +1 more source

The path to the G protein‐coupled receptor structural landscape: Major milestones and future directions

British Journal of Pharmacology, Volume 182, Issue 14, Page 3225-3248, July 2025.
G protein‐coupled receptors (GPCRs) play a crucial role in cell function by transducing signals from the extracellular environment to the inside of the cell. They mediate the effects of various stimuli, including hormones, neurotransmitters, ions, photons, food tastants and odorants, and are renowned drug targets.
Małgorzata M. Kogut‐Günthel, Zeenat Zara, Alessandro Nicoli, Alexandra Steuer, Marta Lopez‐Balastegui, Jana Selent, Sanjai Karanth, Melanie Koehler, Antonella Ciancetta, Layara Akemi Abiko, Franz Hagn, Antonella Di Pizio   +11 more
wiley   +1 more source

Polymeric Gluten Proteins as Climate-Resilient Markers of Quality: Can LC-MS/MS Provide Valuable Information about Spring Wheat Grown in Diverse Climates? [PDF]

J Agric Food Chem
Lama S, Muneer F, America AHP, Kuktaite R.   +3 more
europepmc   +1 more source

Dual Targeting of Pim and PI3 Kinases in Mature T‐Cell Lymphoma

European Journal of Haematology, Volume 115, Issue 1, Page 82-95, July 2025.
ABSTRACT Provirus Integration site for Moloney leukemia virus (Pim) family members are well‐known oncogenes, with an expression that is restricted to few cell types including hematopoietic cells in adult organisms, making it a promising target for lymphoma treatment.
M. Lohrberg, M. Heber, L. Ries, K. Markus, N. Ksionsko, N. Schmidt, G. Nothnick, L. Thielking, M. O'Neill, S. Martínéz‐González, C. Blanco‐Aparicio, J. Pastor, D. Cunningham, R. Koch   +13 more
wiley   +1 more source

Silkworm Enzyme Hydrolysates Improve Memory in MCI Models via CREB-BDNF Signaling and Enhanced Brain Mitochondrial Function. [PDF]

Nutrients
Kim YH, Phuong N, Hoang NMA, Kim HJ, Baik MY, Koh YH.   +5 more
europepmc   +1 more source

Targeted protein degradation of PDE4 shortforms by a novel proteolysis targeting chimera

The FEBS Journal, Volume 292, Issue 13, Page 3360-3377, July 2025.
Here, we report KTX207, a previously undescribed cereblon‐based PDE4 PROTAC that can specifically target PDE4D shortform for degradation. We showed that KTX207 could improve selectivity, potency and enable a long‐lasting effect when used at a sub‐nanomolar concentration.
Yuan Yan Sin, Aoife Giblin, Aleksandra Judina, Punchita Rujirachaivej, Laura G. Corral, Eliza Glennon, Zhi Xian Tai, Tian Feng, Eduardo Torres, Alina Zorn, Julia Gorelik, Elka Kyurkchieva, Pa Thai Yenchitsomanus, Cathy Swindlehurst, Kyle Chan, David Stirling, George S. Baillie   +16 more
wiley   +1 more source

Stimulatory and inhibitory G-protein signaling relays drive cAMP accumulation for timely metamorphosis in the chordate <i>Ciona</i>. [PDF]

Elife
Hozumi A, Totsuka NM, Onodera A, Wang Y, Hamada M, Shiraishi A, Satake H, Horie T, Hotta K, Sasakura Y.   +9 more
europepmc   +1 more source