A variety of 2-oxoamides and related amides based on natural and non-natural amino acids were synthesized. Their activity on two human intracellular phospholipases (GIVA cPLA(2) and GVIA iPLA(2)) and one human secretory phospholipase (GV sPLA(2)) was evaluated. We show that an amide based on (R)-gamma-norleucine is a highly selective inhibitor of GV sPLA(2).
Download full-text PDF |
Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2796434 | PMC |
| http://dx.doi.org/10.1016/j.bmc.2008.10.046 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Effect of Treatment with Progestins and Antiplatelet Agents on IVF in Women with Adenomyosis and Recurrent Implantation Failure.
Diagnostics (Basel)
December 2024
Department of Obstetrics & Gynecology, Faculty of Medicine, "Carol Davila" University of Medicine and Pharmacy, 020021 Bucharest, Romania.
This prospective study aims to identify the effect of the dienogest 2 mg/day and aspirin 150 mg/day combined treatment for two months before frozen ET on the assisted reproduction outcome in women with adenomyosis and recurrent implantation failure (RIF). Patients were selected based on specific criteria and divided into two groups (with and without treatment). Preimplantation biochemical parameters and ultrasonographic features (endometrial thickness, uterine peristalsis, and junctional zone thickness) were compared with pregnancy rate in a non-natural cycle frozen embryo transfer technique.
View Article and Find Full Text PDFIn Vitro Selection of Collagen-Binding Vascular Endothelial Growth Factor Containing Genetically Encoded Mussel-Inspired Adhesive Amino Acids.
Chemistry
January 2025
RIKEN: Rikagaku Kenkyujo, Cluster for Pioneering Research, Hirosawa 2-1, 351-0198, Wako, JAPAN.
Protein immobilization technology is important in medical and industrial applications. We previously reported all-in-one in vitro selection, wherein a collagen-binding vascular endothelial growth factor (CB-VEGF) was identified from a fusion library of random and VEGF sequences. However, its interaction chemistry is mainly limited to the interaction established by the 20 canonical amino acids.
View Article and Find Full Text PDFCatalytic Asymmetric Total Synthesis of (+)-Chamaecydin and (+)-Isochamaecydin and their Stereoisomers.
Angew Chem Int Ed Engl
January 2025
Changchun Institute of Applied Chemistry Chinese Academy of Sciences: Chang Chun Institute of Applied Chemistry Chinese Academy of Sciences, Jilin Province Key Lab of Green Chemistry and Process, CHINA.
A modular approach was developed for the first catalytic asymmetric total syntheses of naturally occurring C30 terpene quinone methides and their non-natural stereoisomers, which feature the presence of an unprecedented spiro[4.4]nonane-containing 6-6-6-5-5-3 hexacyclic skeleton. Resting on a chiral phosphinamide-catalyzed enantioselective reduction of 2,2-disubstituted cyclohexane-1,3-dione, a concise route for the synthesis of enantioenriched 6-6 bicyclic fragment was developed.
View Article and Find Full Text PDFPepFuNN: Novo Nordisk Open-Source Toolkit to Enable Peptide in Silico Analysis.
J Pept Sci
February 2025
Novo Nordisk Research Center Seattle, Novo Nordisk A/S, Seattle, Washington, USA.
We present PepFuNN, a new open-source version of the PepFun package with functions to study the chemical space of peptide libraries and perform structure-activity relationship analyses. PepFuNN is a Python package comprising five modules to study peptides with natural amino acids and, in some cases, sequences with non-natural amino acids based on the availability of a public monomer dictionary. The modules allow calculating physicochemical properties, performing similarity analysis using different peptide representations, clustering peptides using molecular fingerprints or calculated descriptors, designing peptide libraries based on specific requirements, and a module dedicated to extracting matched pairs from experimental campaigns to guide the selection of the most relevant mutations in design new rounds.
View Article and Find Full Text PDFArtificial Metalloenzymes with Two Catalytic Cofactors for Tandem Abiotic Transformations.
Angew Chem Int Ed Engl
January 2025
Laboratory of Inorganic Synthesis and Catalysis, Institute of Chemical Sciences and Engineering, École Polytechnique Fédérale de Lausanne, I, SIC-LSCI, BCH 3305, Lausanne, 1015, Switzerland Website.
Artificial metalloenzymes (ArMs) enable the integration of abiotic cofactors within a native protein scaffold, allowing for non-natural catalytic activities. Previous ArMs, however, have primarily relied on single cofactor systems, limiting them to only one catalytic function. Here we present an approach to construct ArMs embedding two catalytic cofactors based on the biotin-streptavidin technology.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!