Results 261 to 270 of about 22,949 (304)

Allosteric modulation of caspases

Pharmacology & Therapeutics, 2011
Caspases are proteolytic enzymes mainly involved in the induction and execution phases of apoptosis. This type of programmed cell death is an essential regulatory process required to maintain the integrity and homeostasis of multicellular organisms. Inappropriate apoptosis is attributed a key role in many human diseases, including neurodegenerative ...
Hans-Georg, Häcker, Mihiret Tekeste, Sisay, Michael, Gütschow   +2 more
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Allosteric modulation of monomeric proteins*

Biochemistry and Molecular Biology Education, 2005
AbstractMultimeric proteins (e.g. hemoglobin) are considered to be the prototypes of allosteric enzymes, whereas monomeric proteins (e.g. myoglobin) usually are assumed to be nonallosteric. However, the modulation of the functional properties of monomeric proteins by heterotropic allosteric effectors casts doubts on this assumption.
ASCENZI P, BOCEDI A, BOLLI A, FASANO, MAURO, NOTARI S, POLTICELLI F.   +5 more
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Neurotensin Receptor Allosterism Revealed in Complex with a Biased Allosteric Modulator

Biochemistry, 2023
The NTSR1 neurotensin receptor (NTSR1) is a G protein-coupled receptor (GPCR) found in the brain and peripheral tissues with neurotensin (NTS) being its endogenous peptide ligand. In the brain, NTS modulates dopamine neuronal activity, induces opioid-independent analgesia, and regulates food intake.
Brian E. Krumm, Jeffrey F. DiBerto, Reid H. J. Olsen, Hye Jin Kang, Samuel T. Slocum, Shicheng Zhang, Ryan T. Strachan, Xi-Ping Huang, Lauren M. Slosky, Anthony B. Pinkerton, Lawrence S. Barak, Marc G. Caron, Terry Kenakin, Jonathan F. Fay, Bryan L. Roth   +14 more
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Allosteric Agonist Modulators

Journal of Receptors and Signal Transduction, 2007
This article discusses a model to describe the effects of molecules that bind to a site on the receptor separate from that of the endogenous agonist to actively produce receptor signals (direct agonism). In addition, these molecules also modify the biological responses of the endogenous agonist (either potentiation or antagonism).
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Tuning Down the Pain – An Overview of Allosteric Modulation of Opioid Receptors: Mechanisms of Modulation, Allosteric Sites, Modulator Syntheses

Current Topics in Medicinal Chemistry, 2020
Opioid signaling plays a central role in pain perception. As such, it remains the main target in the development of antinociceptive agents, despite serious side effects involved. In recent years, hopes for improved opioid painkillers are rising, together with our understanding of allosterism and biased signaling mechanisms.
Damian Bartuzi, Tomasz M. Wróbel, Agnieszka A. Kaczor, Dariusz Matosiuk   +3 more
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GPCR Allosteric Modulator Discovery

2019
G protein-coupled receptors (GPCRs) influence virtually every aspect of human physiology; about one-third of all marketed drugs target members of this family. GPCR allosteric ligands hold the promise of improved subtype selectivity, spatiotemporal sensitivity, and possible biased property over typical orthosteric ligands.
Yiran, Wu, Jiahui, Tong, Kang, Ding, Qingtong, Zhou, Suwen, Zhao   +4 more
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Profiling Allosteric Modulators of CB ₁ R with an Allosteric Fluoroprobe

Angewandte Chemie
Abstract Allosteric modulation of cannabinoid receptor type 1 (CB 1 R) offers a promising alternative to conventional therapeutic approaches using orthosteric ligands (OLs).
Miroslav Kosar, Themiya Perera, Rudolf L. Z. Ganzoni, Roman C. Sarott, Leire Borrega‐Roman, Rosa Maria Vitale, Alessia Ligresti, Arne C. Rufer, Wolfgang Guba, Uwe Grether, Erick M. Carreira, Dmitry B. Veprintsev, David A. Sykes   +12 more
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The concept of allosteric modulation: an overview

Drug Discovery Today: Technologies, 2013
A brief historical overview of the concept of allosteric interaction is presented together with the different kinds of allosteric control recognized, in the past decades, with the model system of pentameric ligandgated ion channels. Multiple levels of allosteric modulation are identified that include sites distributed in the extracellular ligand ...
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Allosteric modulation of neurotransmission

Biochemical Pharmacology
The therapeutic effects of allosteric modulators on neurotransmission are described. The two unique features of allosteric modulators are: (1) separate binding sites on proteins, and (2) the production of altered receptor conformation upon binding.
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Allosteric Modulation of Dopamine Receptors

Mini-Reviews in Medicinal Chemistry, 2005
Allosteric modulators allow for the fine-tuning of receptor responses to endogenous neurotransmitters and exogenous therapeutic agents. Different types of allosteric modulation of dopamine receptors are discussed as well as the significance of such modulation in the control of normal biological processes and in the treatment of disease.
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