Results 51 to 60 of about 131,252 (300)
Structurally similar allosteric modulators of α7 nicotinic acetylcholine receptors exhibit five distinct pharmacological effects. [PDF]
, 2015 Activation of nicotinic acetylcholine receptors (nAChRs) is associated with the binding of agonists such as acetylcholine to an extracellular site that is located at the interface between two adjacent receptor subunits.
Dhankher, P +4 more
core
Linearized and High Frequency Electrooptic Modulators [PDF]
, 2005 An analysis is performed of many standard and linearized electrooptic modulators known in the industry. The transfer functions of these modulators are evaluated under a consistent set of performance figures of merit, which are gain and spur-free dynamic
Cummings, Uri Vaughan
core +1 more source
Engineering peptides into antibodies—opportunities and strategies for therapeutic innovation
FEBS Letters, EarlyView.Peptides and antibodies occupy complementary therapeutic niches. Peptides recognize difficult targets in a compact format, while antibodies add specificity, long half‐life, and effector functions. This review examines strategies that merge both modalities—peptide grafting into loops, terminal and Fc fusions, and bioconjugation—highlighting how ...
Jinling Wang +2 more
wiley +1 more source
Cryptic pocket formation underlies allosteric modulator selectivity at muscarinic GPCRs
Nature Communications, 2019 Allosteric GPCR modulators can achieve exquisite subtype selectivity, but the underlying mechanism is unclear. Using molecular dynamics simulations, the authors here identify a previously undetected dynamic pocket in muscarinic GPCRs that is critical for
Scott A. Hollingsworth +12 more
doaj +1 more source
Pharmaceuticals, 2020 Schizophrenia was first described by Emil Krapelin in the 19th century as one of the major mental illnesses causing disability worldwide. Since the introduction of chlorpromazine in 1952, strategies aimed at modifying the activity of dopamine receptors ...
Irene Fasciani +7 more
doaj +1 more source
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 +8 more
doaj +1 more source
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
The Shewanella oneidensis Fic enzyme SoFic targets the switch‐I region of EF‐Tu for AMPylation
FEBS Letters, EarlyView.Fic enzymes mediate diverse post‐translational modifications across all domains of life, including AMPylation. Prokaryotic EF‐Tu can be AMPylated and deAMPylated by the conserved Fic enzyme SoFic. Structural and biochemical approaches were used to characterize the effect of AMPylation on EF‐Tu, SoFic's enzymatic activities, and the enzyme‐target ...
Svenja Runge +6 more
wiley +1 more source
Allosteric small molecule modulators of nuclear receptors [PDF]
, 2019 Nuclear Receptors (NRs) are multi-domain proteins, whose natural regulation occurs via ligands for a classical, orthosteric, binding pocket and via intra- and inter-domain allosteric mechanisms.
Gevel, IA van de +3 more
core +3 more sources
Prospecting the protein design landscape
FEBS Letters, EarlyView.This review outlines the current state of various protein design approaches. We discuss the current possibilities enabled by recently released tools, highlight future avenues to pursue in protein design, and underscore the crucial role of key databases and resources for successful protein design workflows.
Jakob R. Riccabona +4 more
wiley +1 more source