Results 61 to 70 of about 44,347 (208)

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

P2X receptors: epithelial ion channels and regulators of salt and water transport. [PDF]

, 2008
When the results from electrophysiological studies of renal epithelial cells are combined with data from in vivo tubule microperfusion experiments and immunohistochemical surveys of the nephron, the accumulated evidence suggests that ATP-gated ion ...
Brian F. King, Bucheimer RE, Dai LJ, Dubyak GR, Egan TM, Inscho EW, King BF, Lazarowski ER, Lazarowski ER, Lehrmann H, Leipziger J, Li L, McCoy DE, North RA, Pelegrin P, Piper AS, Ralevic V, Schwiebert EM, Scott S.P. Wildman, Shirley DG, Taylor AL, Unwin RJ, Vekaria R, Wildman SS, Wildman SS, Wildman SS, Wildman SS, Wildman SS, Wolff SC, Zhang Y   +29 more
core   +1 more source

Nimodipine reduces microglial activation in vitro as evidenced by morphological phenotype, phagocytic activity and high‐throughput RNA sequencing

British Journal of Pharmacology, EarlyView.
Background and Purpose Nimodipine, an L‐type voltage‐gated calcium channel blocker, is an approved cerebral vasorelaxant. We hypothesized that nimodipine attenuates the pro‐inflammatory shift in microglial phenotypes. Here, we analysed the effects of nimodipine on morphological and functional microglial phenotypes as well as their transcriptomic ...
István Pesti, Valentin Varga, Erda Qorri, Rita Frank, Diana Kata, Krisztián Vinga, Péter Archibald Szarvas, Ákos Menyhárt, Károly Gulya, Ferenc Bari, Eszter Farkas   +10 more
wiley   +1 more source

ER localized bestrophin1 activates Ca2+ dependent ion channels TMEM16A and SK4 [PDF]

, 2009
Bestrophins form Ca2+ activated Cl- channels and regulate intercellular Ca2+ signaling1. We demonstrate that bestrophin 1 is localized in the endoplasmic reticulum (ER), where it physically interacts with stromal interacting molecule 1 (Stim1), the ER ...
Fadi AlDehni, Jiraporn Ousingsawat, Joana Almaç, Karl Kunzelmann, Rainer Schreiber, Ralph Witzgall, René   +6 more
core   +2 more sources

Lipid regulation of adenylyl cyclase Rv1625c from Mycobacterium tuberculosis by its membrane‐domain receptor

The FEBS Journal, EarlyView.
The adenylyl cyclase (AC) Rv1625c from M. tuberculosis is a monomeric progenitor of the nine pseudoheterodimeric mammalian AC isoforms. The hexahelical membrane anchor of Rv1625c serves as an inhibitory receptor for fatty acids, particularly oleic acid. One ligand binds into each monomer of the active Rv1625c dimer.
Anita Charlotte Friderun Schultz, Marius Landau, Andrei N. Lupas, Joachim Erdmann Schultz   +3 more
wiley   +1 more source

Macrophage centripetal migration drives spontaneous healing process after spinal cord injury. [PDF]

, 2019
Traumatic spinal cord injury (SCI) brings numerous inflammatory cells, including macrophages, from the circulating blood to lesions, but pathophysiological impact resulting from spatiotemporal dynamics of macrophages is unknown.
Edgerton, V Reggie, Hara, Masamitsu, Harimaya, Katsumi, Inoue, Kazuhide, Iwamoto, Yukihide, Kijima, Ken, Kobayakawa, Kazu, Kubota, Kensuke, Masuda, Takahiro, Matsumoto, Yoshihiro, Nakashima, Yasuharu, Ohkawa, Yasuyuki, Okada, Seiji, Ozato, Keiko, Saito, Takeyuki, Tamaru, Tetsuya, Tamura, Tomohiko, Tsuda, Makoto, Yokota, Kazuya, Yoshizaki, Shingo   +19 more
core   +1 more source

Mind the GAPS: Glia associated with psychological stress

Journal of Neuroendocrinology, EarlyView.
Abstract Glial cells are an integral component of the nervous system, performing crucial functions that extend beyond structural support, including modulation of the immune system, tissue repair, and maintaining tissue homeostasis. Recent studies have highlighted the importance of glial cells as key mediators of stress responses across different organs.
Niklas Blank, Molly Weiner, Shaan Patel, Sarah Köhler, Christoph A. Thaiss   +4 more
wiley   +1 more source

Isolation and characterization of Pisum sativum apyrases, PsNTP9 and PsNTP9-DM, cloned and expressed in Escherichia coli [PDF]

, 2019
Adenosine triphosphate (ATP) is widely known as a fuel source for many biochemical processes, and to a lesser degree also as a signaling molecule in plants and animals.
Wallen, Michael Andrew, Jr
core   +1 more source

The human colon: Evidence for degenerative changes during aging and the physiological consequences

Neurogastroenterology &Motility, EarlyView.
Reduced nociceptor innervation can explain diminished abdominal pain among the elderly. Degenerative changes occur within the colon wall, especially ascending colon. Mechanisms may include senescence‐like activity and inflammaging. Constipation is more likely to occur during age‐related challenges affecting functions of the bowel that now have reduced ...
Nicholas Baidoo, Gareth J. Sanger
wiley   +1 more source

Emerging key roles for P2X receptors in the kidney [PDF]

, 2013
P2X ionotropic non-selective cation channels are expressed throughout the kidney and are activated in a paracrine or autocrine manner following the binding of extracellular ATP and related extracellular nucleotides. Whilst there is a wealth of literature
Birch, R. E., Peppiatt-Wildman, Claire M., Schwiebert, E. M., Wildman, Scott S.P.   +3 more
core   +2 more sources