Results 31 to 40 of about 68,403 (252)

Prospects for the use of allosteric drugs in real-world clinical practice

Реальная клиническая практика: данные и доказательства, 2023
While the clinical validity of the use of allosteric regulation is known, scientists are working on the discovery of new methods for the development of allosteric drugs that can modulate the functions of enzymes, depending on the desired therapeutic ...
I. R. Svechkareva, A. S. Kolbin
doaj   +1 more source

Novel allosteric inhibition of phosphoribulokinase identified by ensemble kinetic modeling of Synechocystis sp. PCC 6803 metabolism

Metabolic Engineering Communications, 2020
The present study attempted a computer simulation of the metabolism of a model cyanobacteria, Synechocystis sp. PCC 6803 (PCC 6803) to predict allosteric inhibitions that are likely to occur in photoautotrophic and mixotrophic conditions as well as in a ...
Hiroki Nishiguchi, James Liao, Hiroshi Shimizu, Fumio Matsuda   +3 more
doaj   +1 more source

Design, Synthesis and Characterization of a New Series of Fluorescent Metabotropic Glutamate Receptor Type 5 Negative Allosteric Modulators

Molecules, 2020
In recent years, new drug discovery approaches based on novel pharmacological concepts have emerged. Allosteric modulators, for example, target receptors at sites other than the orthosteric binding sites and can modulate agonist-mediated activation ...
Víctor Fernández-Dueñas, Mingcheng Qian, Josep Argerich, Carolina Amaral, Martijn D.P. Risseeuw, Serge Van Calenbergh, Francisco Ciruela   +6 more
doaj   +1 more source

Allosteres to regulate neurotransmitter sulfonation [PDF]

Journal of Biological Chemistry, 2019
Catecholamine neurotransmitter levels in the synapses of the brain shape human disposition-cognitive flexibility, aggression, depression, and reward seeking-and manipulating these levels is a major objective of the pharmaceutical industry. Certain neurotransmitters are extensively sulfonated and inactivated by human sulfotransferase 1A3 (SULT1A3).
Kristie, Darrah, Ting, Wang, Ian, Cook, Mary, Cacace, Alexander, Deiters, Thomas S, Leyh   +5 more
openaire   +2 more sources

Light-regulated allosteric switch enables temporal and subcellular control of enzyme activity

eLife, 2020
Engineered allosteric regulation of protein activity provides significant advantages for the development of robust and broadly applicable tools. However, the application of allosteric switches in optogenetics has been scarce and suffers from critical ...
Mark Shaaya, Jordan Fauser, Anastasia Zhurikhina, Jason E Conage-Pough, Vincent Huyot, Martin Brennan, Cameron T Flower, Jacob Matsche, Shahzeb Khan, Viswanathan Natarajan, Jalees Rehman, Pradeep Kota, Forest M White, Denis Tsygankov, Andrei V Karginov   +14 more
doaj   +1 more source

What is allosteric regulation? Exploring the exceptions that prove the rule! [PDF]

Journal of Biological Chemistry
Martin Mccullagh, Tonya N Zeczycki, Chathuri S Kariyawasam   +2 more
exaly   +2 more sources

Functional selectivity of insulin receptor revealed by aptamer-trapped receptor structures

Nature Communications, 2022
DNA aptamers can activate insulin receptor as selective agonists or positive allosteric modulators. Here, authors determine structures of the insulin receptor bound to aptamers and provide a basis for the selective activation or allosteric regulation of ...
Junhong Kim, Na-Oh Yunn, Mangeun Park, Jihan Kim, Seongeun Park, Yoojoong Kim, Jeongeun Noh, Sung Ho Ryu, Yunje Cho   +8 more
doaj   +1 more source

Modes of allosteric regulation of the ubiquitination machinery [PDF]

Current Opinion in Structural Biology, 2020
Ubiquitination is a post-translational modification crucial for cellular signaling. A diverse range of enzymes constitute the machinery that mediates attachment of ubiquitin onto target proteins. This diversity allows the targeting of various proteins in a highly regulated fashion.
Rennie, Martin L., Chaugule, Viduth K., Walden, Helen   +2 more
openaire   +2 more sources

Engineering allosteric regulation in protein kinases [PDF]

Science Signaling, 2018
Mutations in conserved surface regions facilitate the regulatory diversity of kinases.
David Pincus, Jai P. Pandey, Zoë A. Feder, Pau Creixell, Orna Resnekov, Kimberly A. Reynolds   +5 more
openaire   +2 more sources

Molecular basis for the allosteric activation mechanism of the heterodimeric imidazole glycerol phosphate synthase complex

Nature Communications, 2021
The allosteric regulation of the bienzyme complex imidazole glycerol phosphate synthase (HisFH) remains to be elucidated. Here, the authors provide structural insights into the dynamic allosteric mechanism by which ligand binding to the cyclase and ...
Jan Philip Wurm, Sihyun Sung, Andrea Christa Kneuttinger, Enrico Hupfeld, Reinhard Sterner, Matthias Wilmanns, Remco Sprangers   +6 more
doaj   +1 more source