Search results for "Receptor binding"
showing 5 items of 25 documents
Synthesis, benzodiazepine receptor binding and molecular modelling of isochromeno[4,3-c]pyrazol-5(1H)-one derivatives
2012
Abstract A series of isochromeno[4,3-c]pyrazole-5(1H)-one derivatives 7b–h were prepared and tested at 10 μM for their ability to displace specific [3H]flunitrazepam from bovine brain membranes. The substitution pattern of the above derivatives was shown to influence the receptor affinity. The most active compound of the series was 7e, showing a 54% inhibition of [3H]flunitrazepam binding. Compounds 7a–d,i were compared with the known isomers chromeno[4,3-c]pyrazole-4(1H)-ones 14a–d,i, showing that the isochromene/chromene isomerism influences the activity.
Ein Bindungsstellenmodell für H2-Antagonisten vom 4-Pyrimidinon-Typ
1985
In einer Reihe von 17 Histamin-H2-antagonistisch wirksamen 5-substituierten 4-Pyrimidinonen wird durch Berechnung von Wechselwirkungsenergien ein Modell fur die Rezeptorbindungsstelle des Substituenten am C-5 des Pyrimidinons vorgeschlagen. Als Bindungsstelle fungiert die Aminosaure Arginin. A Binding Site Model for H2-Receptor Antagonists of the 4-Pyrimidone Type Based on calculations of the energies of interaction for a series of seventeen 5-substituted 4-pyrimidones with H2-antagonistic activity, a receptor binding site model for substituents at C-5 of the pyrimidone ring is proposed. The binding site is modeled using the amino acid arginine.
DEVELOPMENT AND QUALIFICATION OF BIOANALYTICAL METHODS FOR DEAMIDATED IFNβ-1a AND INVESTIGATION ABOUT THE MECHANISM OF ACTION
2021
Interferon beta-1a (IFNβ-1a) is a recombinant IFNβ with the tradename Rebif involved in several biological activities. Recently, it has been reported that artificial deamidation of IFNb-1a increases its biological response. Given the therapeutical potential, an investigation on the deamidated variant has been carried out via different approaches to discover the mechanism underlying this biological effect. The antiviral and immunomodulatory activity of deamidated cytokine was assessed using two precise and accurate cell-based assays. As expected, deamidated IFNβ-1a showed an increase in the biological response and its canonical pathway and receptor binding affinity were thorough analysed. De…
Receptor Recognition Sites of Cytokines Are Organized as Exchangeable Modules
1999
Interleukin-6 (IL-6) and ciliary neurotrophic factor (CNTF) are "4-helical bundle" cytokines of the IL-6 type family of neuropoietic and hematopoietic cytokines. IL-6 signals by induction of a gp130 homodimer (e.g. IL-6), whereas CNTF and leukemia inhibitory factor (LIF) signal via a heterodimer of gp130 and LIF receptor (LIFR). Despite binding to the same receptor component (gp130) and a similar protein structure, IL-6 and CNTF share only 6% sequence identity. Using molecular modeling we defined a putative LIFR binding epitope on CNTF that consists of three distinct regions (C-terminal A-helix/N-terminal AB loop, BC loop, C-terminal CD-loop/N-terminal D-helix). A corresponding gp130-bindin…