Results 241 to 250 of about 3,750,504 (279)

In search of negative allosteric modulators of biological targets

Drug Discovery Today, 2009
The value of using negative allosteric modulators of protein function in therapeutic treatment of human diseases is becoming more apparent. Many current screening paradigms, however, are not consciously designed to discover negative allosteric modulators, and those that are serendipitously discovered can be easily overlooked during the hit-picking ...
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PKCε acts as negative allosteric modulator of EGF receptor signalling

Cellular Signalling, 2011
Protein kinase C ε (PKCε) is a transforming oncogene and plays a pivotal role in numerous cellular processes including proliferation, invasion and differentiation. Recently, we described a function of PKCε as a scaffold protein linking PLCγ1 to the EGFR module.
Simona, Weisheit, Claudia, Schäfer, Carmen, Mertens, Alexander, Berndt, Claus, Liebmann   +4 more
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Extracellular binding sites of positive and negative allosteric P2X4 receptor modulators

Life Sciences, 2022
P2X receptors are ATP-gated ion channels which play a role in many pathophysiological conditions. They are considered as novel drug targets, particularly in the fields of pain, (neuro) inflammation, and cancer. Due to difficulties in developing drug-like orthosteric ligands that bind to the highly polar ATP binding site, the design of positive and ...
Stephanie Weinhausen, Jessica Nagel, Vigneshwaran Namasivayam, Claudia Spanier, Aliaa Abdelrahman, Theodor Hanck, Ralf Hausmann, Christa E. Müller   +7 more
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The discovery of novel calcium sensing receptor negative allosteric modulators

Bioorganic & Medicinal Chemistry Letters, 2009
The design and profile of a series of zwitterionic calcium sensing receptor negative allosteric modulators is described. Evaluation of key analogues using a rat model demonstrate a robust response, significantly improved potency over ronacaleret and have the potential as an oral, anabolic treatment for osteoporosis.
Gayatri, Balan, Jonathan, Bauman, Samit, Bhattacharya, Mayda, Castrodad, David R, Healy, Michael, Herr, Paul, Humphries, Sandra, Jennings, Amit S, Kalgutkar, Brendon, Kapinos, Vishal, Khot, Kimberly, Lazarra, Mei, Li, Yan, Li, Constantin, Neagu, Robert, Oliver, David W, Piotrowski, David, Price, Hong, Qi, Holly A, Simmons, James, Southers, Liuqing, Wei, Yan, Zhang, Vishwas M, Paralkar   +23 more
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A negative allosteric modulator modulates GABAB-receptor signalling through GB2 subunits

Biochemical Journal, 2016
An γ-aminobutyric acid type B (GABAB)-receptor mediates slow and prolonged synaptic inhibition in the central nervous system, which represents an interesting target for the treatment of various diseases and disorders of the central nervous system.
Bing, Sun, Linhai, Chen, Lei, Liu, Zhixiong, Xia, Jean-Philippe, Pin, Fajun, Nan, Jianfeng, Liu   +6 more
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Characterization of an mGluR2/3 Negative Allosteric Modulator in Rodent Models of Depression

Journal of Neurogenetics, 2011
There is growing evidence suggesting that antagonists of group II metabotropic glutamate receptors (mGluR2/3) exhibit antidepressant-like properties in several preclinical models of depression. However, all those studies have been performed using competitive group II non-selective orthosteric antagonists.
Campo, Brice, Kalinichev, Mikhail, Lambeng, Nathalie, El Yacoubi, Malika, Royer-Urios, Isabelle, Schneider, Manfred, Legrand, Coline, Parron, Delphine, Girard, Francoise, Bessif, Abdelhak, Poli, Sonia, Vaugeois, Jean-Marie, Le Poul, Emmanuel, Celanire, Sylvain   +13 more
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Nanobodies as negative allosteric modulators for human calcium sensing receptor

Biochemical and Biophysical Research Communications
Human calcium sensing receptor (CaSR) senses calcium ion concentrations in vivo and is an important class of drug targets. Mutations in the receptor can lead to disorders of calcium homeostasis, including hypercalcemia and hypocalcemia. Here, 127 CaSR-targeted nanobodies were generated from camels, and four nanobodies with inhibitory function were ...
Qianqian Cui, Lu Wang, Haonan Wang, Xiaochen Chen, Li Han, Tengjie Geng, Yongjun Kou, Wenqing Zhang, Mei Dai, Huarui Qiao, Zengchao Sun, Lingyun Li, Zhongyun Lan, Hongxi Xu, Jiaqiang Xu, Yuanyuan Dai, Yong Geng   +16 more
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COR758, a negative allosteric modulator of GABA receptors

Neuropharmacology, 2021
Miriam Melis, Valeria Sogos, Federico Corelli   +2 more
exaly  

Understanding the Allosteric Modulation of PTH1R by a Negative Allosteric Modulator

Cells, 2023
Lili Xi, Mengrong Li, Yiqiong Bao
exaly  

Identification of a β-arrestin-biased negative allosteric modulator for the β2-adrenergic receptor

Proceedings of the National Academy of Sciences of the United States of America, 2023
Joseph M Salvino, Charles Scott, Leon Sakkal   +2 more
exaly