Results 41 to 50 of about 205,233 (331)

Agonist-directed desensitization of the β2-adrenergic receptor. [PDF]

PLoS ONE, 2011
The β(2)-adrenergic receptor (β(2)AR) agonists with reduced tachyphylaxis may offer new therapeutic agents with improved tolerance profile. However, receptor desensitization assays are often inferred at the single signaling molecule level, thus ligand ...
Vasiliy Goral, Yan Jin, Haiyan Sun, Ann M Ferrie, Qi Wu, Ye Fang   +5 more
doaj   +1 more source

Aminomethanesulfonic acid illuminates the boundary between full and partial agonists of the pentameric glycine receptor

eLife, 2022
To clarify the determinants of agonist efficacy in pentameric ligand-gated ion channels, we examined a new compound, aminomethanesulfonic acid (AMS), a molecule intermediate in structure between glycine and taurine.
Josip Ivica, Hongtao Zhu, Remigijus Lape, Eric Gouaux, Lucia G Sivilotti   +4 more
doaj   +1 more source

Evaluation of partial ?-adrenoceptor agonist activity [PDF]

British Journal of Clinical Pharmacology, 1997
A partial β‐adrenoceptor (β‐AR) agonist will exhibit opposite agonist and antagonist activity depending on the prevailing degree of adrenergic tone or the presence of a β‐AR agonist with higher intrinsic activity. In vivo partial β‐AR agonist activity will be evident at rest with low endogenous adrenergic tone, as for example with chronotropicity (β1 ...
B J, Lipworth, A, Grove
openaire   +2 more sources

Hematopoietic (stem) cells—The elixir of life?

FEBS Letters, EarlyView.
The aging of HSCs (hematopoietic stem cells) and the blood system leads to the decline of other organs. Rejuvenating aged HSCs improves the function of the blood system, slowing the aging of the heart, kidney, brain, and liver, and the occurrence of age‐related diseases.
Emilie L. Cerezo, Jonah Anderson, Emilie Dinh Vedrenne, Noël Yeh Martín, Jette Lengefeld   +4 more
wiley   +1 more source

BU10038 as a safe opioid analgesic with fewer side-effects after systemic and intrathecal administration in primates [PDF]

, 2019
© 2019 British Journal of Anaesthesia. Published by Elsevier Ltd. All rights reserved.Background: The marked increase in mis-use of prescription opioids has greatly affected our society. One potential solution is to develop improved analgesics which have
Cami-Kobeci, Gerta, Czoty, Paul W., DeLoid, Heather B., Ding, Huiping, Hsu, Fang Chi, Husbands, Stephen M., Kiguchi, Norikazu, Ko, Mei Chuan, Sukhtankar, Devki D., Toll, Lawrence   +9 more
core   +5 more sources

Integration of circadian and hypoxia signaling via non‐canonical heterodimerization

FEBS Letters, EarlyView.
CLOCK, BMAL1, and HIFs are basic helix‐loop‐helix and Per‐Arnt‐Sim domain (bHLH‐PAS) proteins, which function as transcription factors. bHLH‐PAS proteins are designated in two classes. Many class I proteins are regulated by environmental signals via their PAS domains, but such signals have not been identified for all.
Sicong Wang, Katja A. Lamia
wiley   +1 more source

5,6-dimethylxanthenone-4-acetic acid (DMXAA), a partial STING agonist, competes for human STING activation

Frontiers in Immunology
5,6-dimethylxanthenone-4-acetic acid (DMXAA) is a mouse-selective stimulator of interferon gene (STING) agonist exerting STING-dependent anti-tumor activity.
Burcu Temizoz, Burcu Temizoz, Burcu Temizoz, Takayuki Shibahara, Kou Hioki, Tomoya Hayashi, Tomoya Hayashi, Tomoya Hayashi, Kouji Kobiyama, Kouji Kobiyama, Kouji Kobiyama, Michelle Sue Jann Lee, Michelle Sue Jann Lee, Michelle Sue Jann Lee, Naz Surucu, Erdal Sag, Atsushi Kumanogoh, Atsushi Kumanogoh, Masahiro Yamamoto, Masahiro Yamamoto, Mayda Gursel, Seza Ozen, Etsushi Kuroda, Cevayir Coban, Cevayir Coban, Cevayir Coban, Cevayir Coban, Ken J. Ishii, Ken J. Ishii, Ken J. Ishii, Ken J. Ishii   +30 more
doaj   +1 more source

The NMDA agonist D-cycloserine facilitates fear memory consolidation in humans [PDF]

, 2009
Animal research suggests that the consolidation of fear and extinction memories depends on N-methyl D-aspartate (NMDA)- type glutamate receptors.
Amaral, Anthony, Ashburner, Bauer, Beatrice Holt, Benedetto De Martino, Blair, Bond, Bouton, Buchel, Carmichael, Carter, Christian Büchel, Corcoran, Corcoran, Critchley, Davis, Deichmann, Deichmann, Delamater, Duvernoy, Ekman, Frankland, Friston, Friston, Gould, Guastella, Heresco-Levy, Hetem, Hofmann, Honey, Izquierdo, Ji, Kalisch, Kalisch, Kalisch, Kalisch, Karcz-Kubicha, Kim, Klodzinska, Kushner, LaBar, LaBar, Ledgerwood, Lee, Mao, Maren, Martin, McGaugh, Morris, Myers, Parwani, Pavlov, Penny, Phelps, Predrag Petrovic, Raffael Kalisch, Raymond J. Dolan, Ressler, Rodrigues, Rubin, Runyan, Scavio, Schafe, Seymour, Sheinin, Sotres-Bayon, Spielberger, Stefan Klöppel, Stewart, Takehara, Trevisan, van Berckel, Vervliet, Walker, Yang, Zhu, Zorawski   +77 more
core   +2 more sources

Agonists and Partial Agonists of Rhodopsin:  Retinals with Ring Modifications [PDF]

Biochemistry, 2005
Activation of the visual pigment rhodopsin is initiated by isomerization of its retinal chromophore to the all-trans geometry, which drives the conformation of the protein to the active state. We have examined by FTIR spectroscopy the impact of a series of modifications at the ring of retinal on the activation process and on molecular interactions ...
Vogel, Reiner, Siebert, Friedrich, Lüdeke, Steffen, Hirshfeld, Amiram, Sheves, Mordechai   +4 more
openaire   +3 more sources

Function‐driven design of a surrogate interleukin‐2 receptor ligand

FEBS Letters, EarlyView.
Interleukin (IL)‐2 signaling can be achieved and precisely fine‐tuned through the affinity, distance, and orientation of the heterodimeric receptors with their ligands. We designed a biased IL‐2 surrogate ligand that selectively promotes effector T and natural killer cell activation and differentiation. Interleukin (IL) receptors play a pivotal role in
Ziwei Tang, Zelin Cheng, Teng Li, Fulian Wang, Liangminghui Zhang, Xiuxiu He, Lili Liu, Wei Wang, Aibin Liang, Guang Yang   +9 more
wiley   +1 more source