Structure−Activity Relationship of (1-Aryl-2-piperazinylethyl)piperazines:  Antagonists for the AGRP/Melanocortin Receptor Binding

2003 ◽  
Vol 46 (1) ◽  
pp. 9-11 ◽  
Author(s):  
Premilla N. Arasasingham ◽  
Christopher Fotsch ◽  
Xiaohu Ouyang ◽  
Mark H. Norman ◽  
Michael G. Kelly ◽  
...  
Keyword(s):  
Receptor Binding ◽  
Structure Activity Relationship ◽  
Melanocortin Receptor ◽  
Activity Relationship ◽  
Structure Activity ◽  
Relationship Of

scholarly journals Structure-Activity Relationship of Gelatinase Biosynthesis-Activating Pheromone of Enterococcus faecalis

2008 ◽  
Vol 191 (2) ◽  
pp. 641-650 ◽  
Author(s):  
Kenzo Nishiguchi ◽  
Koji Nagata ◽  
Masaru Tanokura ◽  
Kenji Sonomoto ◽  
Jiro Nakayama
Keyword(s):  
Enterococcus Faecalis ◽  
Receptor Binding ◽  
Structure Activity Relationship ◽  
Compact Form ◽  
Activity Relationship ◽  
Side Chains ◽  
Agonist Activity ◽  
The Core ◽  
Structure Activity ◽  
Relationship Of

ABSTRACT The expression of pathogenicity-related extracellular proteases, namely, gelatinase and serine protease, in Enterococcus faecalis is positively regulated by a quorum-sensing system mediated by an autoinducing peptide called gelatinase biosynthesis-activating pheromone (GBAP). GBAP is an 11-amino-acid-residue cyclic peptide containing a lactone linkage. To study the structure-activity relationship of GBAP, we synthesized a series of GBAP analogues and evaluated their activities by a gelatinase-inducing assay and newly developed receptor-binding assays in which fluorescence-labeled peptides bound onto the FsrC-overexpressing Lactococcus lactis cell surface were observed by fluorescent microscopy and quantified by using a fluorophotometer. Alanine-scanning analysis of GBAP showed that the entire ring region was involved in the GBAP agonist activity, while side chains of the tail region were not strictly recognized. The alanine substitution of Phe7 or Trp10 almost abolished their receptor-binding abilities and GBAP agonist activities, suggesting that these two aromatic side chains are strongly involved in receptor interaction and activation. Furthermore, the Trp10 substitution with natural and unnatural aromatic amino acids, except pentafluorophenylalanine, caused no loss of agonist activity. This suggested the importance of a negative electrostatic potential created by an π-electron cloud on the aromatic ring surface. Structural analysis of GBAP with nuclear magnetic resonance spectroscopy revealed that the ring region adopted a hairpin-like fold and was tightly packed into a compact form. The side chain of Trp10 was partially buried in the core structure, contributing to the stabilization of the compact form, while that of Phe7 was extended from the core structure into the solvent and was probably directly involved in receptor binding.

Structure-activity relationship of (-) mammea A/BB derivatives against Leishmania amazonensis

Planta Medica ◽  
2008 ◽  
Vol 74 (09) ◽  
Author(s):  
MA Brenzan ◽  
CV Nakamura ◽  
BPD Filho ◽  
T Ueda-Nakamura ◽  
MCM Young ◽  
...  
Keyword(s):  
Structure Activity Relationship ◽  
Leishmania Amazonensis ◽  
Activity Relationship ◽  
Structure Activity ◽  
Relationship Of

Antineoplastic Activity, Structural Modification, Synthesis and Structure-activity Relationship of Dammarane-type Ginsenosides: An Overview

2019 ◽  
Vol 23 (5) ◽  
pp. 503-516 ◽  
Author(s):  
Qiang Zhang ◽  
Xude Wang ◽  
Liyan Lv ◽  
Guangyue Su ◽  
Yuqing Zhao
Keyword(s):  
Structural Modification ◽  
Gastrointestinal Disease ◽  
Structure Activity Relationship ◽  
Cerebrovascular Diseases ◽  
Activity Relationship ◽  
Cycle Arrest ◽  
Structure Activity ◽  
Wide Range ◽  
Structural Association ◽  
Relationship Of

Dammarane-type ginsenosides are a class of tetracyclic triterpenoids with the same dammarane skeleton. These compounds have a wide range of pharmaceutical applications for neoplasms, diabetes mellitus and other metabolic syndromes, hyperlipidemia, cardiovascular and cerebrovascular diseases, aging, neurodegenerative disease, bone disease, liver disease, kidney disease, gastrointestinal disease and other conditions. In order to develop new antineoplastic drugs, it is necessary to improve the bioactivity, solubility and bioavailability, and illuminate the mechanism of action of these compounds. A large number of ginsenosides and their derivatives have been separated from certain herbs or synthesized, and tested in various experiments, such as anti-proliferation, induction of apoptosis, cell cycle arrest and cancer-involved signaling pathways. In this review, we have summarized the progress in structural modification, shed light on the structure-activity relationship (SAR), and offered insights into biosynthesis-structural association. This review is expected to provide a preliminary guide for the modification and synthesis of ginsenosides.

Design, Facile Synthesis, Antibacterial Activity and Structure-Activity Relationship of Novel Di- and Tri-Substituted 1,3,5-Triazines

2012 ◽  
Vol 9 (3) ◽  
pp. 329-335 ◽  
Author(s):  
Surajit Kumar Ghosh ◽  
Ashmita Saha ◽  
Bornali Hazarika ◽  
Udaya Pratap Singh ◽  
Hans Raj Bhat ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Facile Synthesis ◽  
Structure Activity ◽  
Relationship Of
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