Results 251 to 260 of about 317,690 (321)

Progress on the development of Class A GPCR‐biased ligands

British Journal of Pharmacology, EarlyView.
Class A G protein‐coupled receptors (GPCRs) continue to garner interest for their essential roles in cell signalling and their importance as drug targets. Although numerous drugs in the clinic target these receptors, over 60% GPCRs remain unexploited. Moreover, the adverse effects triggered by the available unbiased GPCR modulators, limit their use and
Paula Morales, Magdalena M. Scharf, Marcel Bermudez, Attila Egyed, Rafael Franco, Olivia K. Hansen, Nadine Jagerovic, Jan Jakubík, György M. Keserű, Dóra Judit Kiss, Pawel Kozielewicz, Olav Larsen, Maria Majellaro, Ana Mallo‐Abreu, Gemma Navarro, Rubén Prieto‐Díaz, Mette M. Rosenkilde, Eddy Sotelo, Holger Stark, Tobias Werner, Laura M. Wingler   +20 more
wiley   +1 more source

Phosphatidylinositol 3-Kinase Inhibition and Allogeneic Stem Cell Transplantation Can Overcome Chemotherapy Resistance in Refractory Burkitt Lymphoma. [PDF]

J Hematol
Wirk B, Jayakumar R, Lim J.
europepmc   +1 more source

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

British Journal of Pharmacology, EarlyView.
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

Structural pathway for PI3-kinase regulation by VPS15 in autophagy. [PDF]

Science
Cook ASI, Chen M, Nguyen TN, Cabezudo AC, Khuu G, Rao S, Garcia SN, Yang M, Iavarone AT, Ren X, Lazarou M, Hummer G, Hurley JH.   +12 more
europepmc   +1 more source

High‐throughput screen identifies MAS9 as a novel inhibitor of the C‐type lectin receptor‐2 (CLEC‐2)–podoplanin interaction

British Journal of Pharmacology, EarlyView.
Abstract Background and Purpose The C‐type lectin‐like receptor‐2 (CLEC‐2) is a platelet receptor for the endogenous ligand podoplanin. This interaction contributes to several (patho)physiological processes, such as lymphangiogenesis, preservation of blood and lymphatic vessel integrity organ development, and tumour metastasis.
Marcin A. Sowa, Yan Wu, Jan van Groningen, Ying Di, Helma van den Hurk, Johannes A. Eble, Jonathan M. Gibbins, Ángel García, Alice Y. Pollitt   +8 more
wiley   +1 more source

The Effect and Treatment of PIK3CA Mutations in Breast Cancer: Current Understanding and Future Directions. [PDF]

Medicina (Kaunas)
Cho YB, Park KS.
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, EarlyView.
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

Targeted Therapies for Slow-Flow Vascular Malformations. [PDF]

Australas J Dermatol
Li GX, Sebaratnam DF, Pham JP.
europepmc   +1 more source

Pharmacokinetics and pharmacodynamics of intranasal insulin in a rat brain

British Journal of Pharmacology, EarlyView.
Abstract Background and Purpose Understanding of the insulin‐mediated effects on signalling and metabolism is important not only for fundamental knowledge of insulin's action in the brain but also for elucidating the mechanism of therapeutic potential in neurodegenerative disorders with underlying brain metabolic dysfunction.
Jelena Osmanovic Barilar, Leonarda Vlahov, Ana Babic Perhoc, Jan Homolak, Davor Virag, Eugenio Barone, Melita Salkovic‐Petrisic, Ana Knezović   +7 more
wiley   +1 more source

Susceptibility of Brca1(L63X/+) rat to ovarian reserve dissipation by chemotherapeutic agents to breast cancer

Cancer Science, Volume 116, Issue 4, Page 1139-1152, April 2025.
We analyzed the effects of olaparib in the presence and absence of cyclophosphamide in a recently established rat BRCA1‐mutant model and found for the first time that mutant ovaries are more susceptible to oxidative stress, potentially depleting primordial follicles via activation of granulosa cells and inducing oocyte death due to accumulated DNA ...
Satoshi Kaseki, Reina Sonehara, Yashiro Motooka, Hideaki Tanaka, Tomoko Nakamura, Satoko Osuka, Shinya Akatsuka, Hiroaki Kajiyama, Tomoji Mashimo, Tatsuhiko Imaoka, Shinya Toyokuni   +10 more
wiley   +1 more source