The Caenorhabditis elegans DPF‐3 and human DPP4 have tripeptidyl peptidase activity
The dipeptidyl peptidase IV (DPPIV) family comprises serine proteases classically defined by their ability to remove dipeptides from the N‐termini of substrates, a feature that gave the family its name. Here, we report the discovery of a previously unrecognized tripeptidyl peptidase activity in DPPIV family members from two different species.
Aditya Trivedi, Rajani Kanth Gudipati
wiley +1 more source
N -haloacetyl phenothiazines and derivatives: Preparation, characterization and structure-activity relationship for antifungal activity [PDF]
A serie of N-acetyl phenothiazines and related compounds was synthesized by means of the acetylation reaction of the corresponding phenothiazine with the appropriate reagent using microwave irradiation.
Afeltra, Javier +7 more
core +1 more source
Molecular bases of circadian magnesium rhythms across eukaryotes
Circadian rhythms in intracellular [Mg2+] exist across eukaryotic kingdoms. Central roles for Mg2+ in metabolism suggest that Mg2+ rhythms could regulate daily cellular energy and metabolism. In this Perspective paper, we propose that ancestral prokaryotic transport proteins could be responsible for mediating Mg2+ rhythms and posit a feedback model ...
Helen K. Feord, Gerben van Ooijen
wiley +1 more source
Design, Synthesis and Antifungal Activity of Psoralen Derivatives
A series of linear furanocoumarins with different substituents have been designed and synthesized. Their structures were confirmed by 1H-NMR spectroscopy, high resolution mass spectra (EI-MS), IR, and X-ray single-crystal diffraction.
Xiang Yu +5 more
doaj +1 more source
Structure-activity relationship studies on O-sulfated Hirudins [PDF]
Thesis (Ph. D. in Agriculture)--University of Tsukuba, (B), no.
Muramatsu Ryo, 村松 了
core
Synthesis and leishmanicidal activity of cinnamic acid esters: structure–activity relationship [PDF]
Several cinnamic acid esters were obtained via Fischer esterification of cinnamic acids derivatives with aliphatic alcohols. Structures of the products were elucidated by spectroscopic analysis.
Carda, Miguel +7 more
core +2 more sources
Peptide‐based ligand antagonists block a Vibrio cholerae adhesin
The structure of a peptide‐binding domain of the Vibrio cholerae adhesin FrhA was solved by X‐ray crystallography, revealing how the inhibitory peptide AGYTD binds tightly at its Ca2+‐coordinated pocket. Structure‐guided design incorporating D‐amino acids enhanced binding affinity, providing a foundation for developing anti‐adhesion therapeutics ...
Mingyu Wang +9 more
wiley +1 more source
A practical overview of quantitative structure-activity relationship [PDF]
Quantitative structure-activity relationship (QSAR) modeling pertains to the construction of predictive models of biological activities as a function of structural and molecular information of a compound library.
Isarankura-Na-Ayudhya, Chartchalerm +3 more
core
Real‐time assay of ribonucleotide reductase activity with a fluorescent RNA aptamer
Ribonucleotide reductases (RNR) synthesize DNA building blocks de novo, making them crucial in DNA replication and drug targeting. FLARE introduces the first single‐tube real‐time coupled RNR assay, which enables isothermal tracking of RNR activity at nanomolar enzyme levels and allows the reconstruction of allosteric regulatory patterns and rapid ...
Jacopo De Capitani +4 more
wiley +1 more source
On Exploring Structure–Activity Relationships [PDF]
Understanding structure-activity relationships (SARs) for a given set of molecules allows one to rationally explore chemical space and develop a chemical series optimizing multiple physicochemical and biological properties simultaneously, for instance, improving potency, reducing toxicity, and ensuring sufficient bioavailability.
openaire +2 more sources

