Results 101 to 110 of about 4,995,094 (293)

Targeting breast cancer cells by MRS1477, a positive allosteric modulator of TRPV1 channels.

PLoS ONE, 2017
There is convincing epidemiological and experimental evidence that capsaicin, a potent natural transient receptor potential cation channel vanilloid member 1 (TRPV1) agonist, has anticancer activity.
Mustafa Nazıroğlu, Bilal Çiğ, Walter Blum, Csaba Vizler, Andrea Buhala, Annamária Marton, Róbert Katona, Katalin Jósvay, Beat Schwaller, Zoltán Oláh, László Pecze   +10 more
doaj   +1 more source

Development of novel, cns penetrant mglu3 selective negative allosteric modulator probes derived from a closely related mglu5 positive allosteric modulator

, 2012
Metabotropic glutamate (mGlu) receptors are examples of family C G-protein-coupled receptors that possess vast roles in the pathophysiology of central nervous system (CNS) disorders.
Bruner, Joshua Andrew
core  

Switching Spike Plasticity Shapes ACE2 Engagement Across SARS‐CoV‐2 Variants

Advanced Science, EarlyView.
Conformational plasticity governs SARS‐CoV‐2 spike function and ACE2 recognition. Using high‐speed AFM and single‐molecule force spectroscopy, we analyzed the ancestral spike and nine variants, revealing progressive rigidification from Delta, variable plasticity in Omicron sublineages, and JN.1 compaction.
Sarah Stainer, Rong Zhu, Manuel Reithofer, Gerhard Stadlmayr, Katharina Stadlbauer, Panchika Prangkio, Christoph Rippel, Markus Hahn, Aniko Eva Kasztner, Stefanie Stohl, Petr Bednar, Daniel Ruzek, David Glück, Robert Tampé, Gordana Wozniak‐Knopp, Yoo Jin Oh, Miriam Klausberger, Peter Hinterdorfer   +17 more
wiley   +1 more source

Sex-dependent anti-stress effect of an α5 subunit containing GABAA receptor positive allosteric modulator

Frontiers in Pharmacology, 2016
Rationale: Current first-line treatments for stress-related disorders such as Major Depressive Disorder (MDD) act on monoaminergic systems and take weeks to achieve a therapeutic effect with poor response and low remission rates.
Sean C. Piantadosi, Sean C. Piantadosi, Beverly J French, Michael M Poe, Tamara Timić, Bojan Marković, Mohan Pabba, Marianne Seney, Hyunjung Oh, Beverley Anne Orser, Miroslav M Savic, James M Cook, Etienne Sibille, Etienne Sibille, Etienne Sibille, Etienne Sibille   +15 more
doaj   +1 more source

Supramolecular Degraders: An Emerging Paradigm in Targeted Protein Degradation

Advanced Science, EarlyView.
Dynamic supramolecular assembly reshapes targeted protein degradation by coordinating modular degrader construction, delivery, functional integration, and intracellular assembly or activation across proteasomal, endosomal–lysosomal, and autophagy–lysosomal pathways.
Kongjun Liu, Xue Yuan, Yan Zhou, Rui Yuan, Shaocheng Xie, Yong Chen, Peiyi Wang, Jianmei Gao, Qihai Gong   +8 more
wiley   +1 more source

Antipsychotic profiles of TASP0443294, a novel and orally active positive allosteric modulator of metabotropic glutamate 2 receptor

Journal of Pharmacological Sciences, 2015
Glutamatergic dysfunction has been implicated in psychiatric disorders such as schizophrenia. The stimulation of metabotropic glutamate (mGlu) 2 receptor has been shown to be effective in a number of animal models of schizophrenia.
Hirohiko Hikichi, Tetsuaki Hiyoshi, Toshiyuki Marumo, Yasumitsu Tomishima, Ayaka Kaku, Izumi Iida, Hiroki Urabe, Tomoko Tamita, Akito Yasuhara, Jun-ichi Karasawa, Shigeyuki Chaki   +10 more
doaj   +1 more source

Targeting β2‐Adrenergic Receptor Stability With Lycorine Reveals a Host‐Directed Pathway for Antiviral Defense Against Poxviruses

Advanced Science, EarlyView.
Chronic stress drives autophagy‐mediated β2‐AR degradation, impairing antiviral immunity and promoting poxvirus lethality. Lycorine directly stabilizes β2‐AR to restore host defense, suppress excessive inflammation and improve survival. ABSTRACT Psychological stress is a pervasive yet poorly understood modulator of infectious disease outcomes. Here, we
Xin Zhang, Shuqin Xu, Zixuan Zhang, Chenwen Wan, Xiaoqin Wang, Peihua Wang, Huini Yang, Tianxiao Huang, Yijia Yuan, Faiza Atique, Rui Yang, Yingli He, Zhijun Liu   +12 more
wiley   +1 more source

The positive allosteric GABAB receptor modulator rac-BHFF enhances baclofen-mediated analgesia in neuropathic mice.

, 2016
Neuropathic pain is associated with impaired inhibitory control of spinal dorsal horn neurons, which are involved in processing pain signals. The metabotropic GABAB receptor is an important component of the inhibitory system and is highly expressed in ...
Malherbe, Pari, Benke, Dietmar, Khaled Zemoura, William T. Ralvenius, Zemoura, Khaled, Ralvenius, William T, Pari Malherbe, Dietmar Benke   +7 more
core   +1 more source

A Synthetic Platform for Antibody Junctional Diversification Beyond Natural Constraints

Advanced Science, EarlyView.
ARESEC is a synthetic platform that reconstructs functional V(D)J recombination in HEK293T cells. By introducing RSS elements and co‐expressing RAG1/2 and TdT across all three antibody CDRs, it enables programmable junctional diversification and direct generation of high‐affinity variants targeting PD‐1/PD‐L1, overcoming the evolutionary constraints of
Wang Liu, Jun Yang, Yuhang Zhang, Xiaoli Xue   +3 more
wiley   +1 more source

S 47445 Produces Antidepressant- and Anxiolytic-Like Effects through Neurogenesis Dependent and Independent Mechanisms

Frontiers in Pharmacology, 2017
Glutamatergic dysfunctions are observed in the pathophysiology of depression. The glutamatergic synapse as well as the AMPA receptor’s (AMPAR) activation may represent new potential targets for therapeutic intervention in the context of major depressive ...
Indira Mendez-David, Jean-Philippe Guilloux, Mariusz Papp, Laurent Tritschler, Elisabeth Mocaer, Alain M. Gardier, Sylvie Bretin, Denis J. David   +7 more
doaj   +1 more source