Results 251 to 260 of about 131,252 (300)

Exploration of the Isosteric Concept Applied to 1,2,4-Benzothiadiazine 1,1-Dioxides in the Discovery of Novel AMPA Receptor Positive Allosteric Modulators. [PDF]

ACS Omega
Colson T, Lesenfants C, Goffin E, Fraikin P, Schmitz A, de Tullio P, Danober L, Pirotte B, Francotte P.   +8 more
europepmc   +1 more source

Demystifying the Antidepressant Mechanism of Action of Stinels, a Novel Class of Neuroplastogens: Positive Allosteric Modulators of the NMDA Receptor. [PDF]

Pharmaceuticals (Basel)
Donello JE, McIntyre RS, Pickel DB, Stahl SM.   +3 more
europepmc   +1 more source

Rational design of allosteric modulators: Challenges and successes

Wiley Interdisciplinary Reviews: Computational Molecular Science, 2021
Recent advances in structural biology and computational techniques have revealed allosteric mechanisms for an abundance of targets leading to the establishment of rational design of allosteric modulators as a new avenue for drug discovery.
Alexios Chatzigoulas, Zoe Cournia
exaly   +4 more sources

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Olfaction: Allosteric modulation

Current Biology, 2023
New research indicates that the odor-evoked responses of human olfactory receptors can be enhanced via the non-competitive binding of an allosteric modulator. This modulatory mechanism adds an additional layer of complexity to the peripheral encoding of odors.
Samuel, Caton, Adam, Dewan
openaire   +2 more sources

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
openaire   +2 more sources

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
openaire   +5 more sources

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).
openaire   +2 more sources

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
openaire   +2 more sources