Ribosomal Synthesis of Topologically Defined Thioisoindole-Bridged Bicyclic Peptides. [PDF]
A flexible in vitro translation (FIT) system‐based strategy for ribosomal synthesis of thioisoindole‐bridged bicyclic (TiB) peptides is developed. The flexizyme substrate Ac‐Ala(NtBA)Sc‐CME is efficiently incorporated into FIT to generate ribosomal peptides bearing N‐terminal Ac‐Ala(NtBA)Sc as the cyclization handle, which after mild deprotection ...
Zhang Y, Vinogradov AA, Sun Y, Suga H.
europepmc +3 more sources
Development of a Partial Proteolysis Targeting Chimera Library Based on Achiral Cereblon E3 Ligase Ligands and its Application for Bruton's Tyrosine Kinase Degraders. [PDF]
A partial proteolysis targeting chimera (PROTAC) library bearing achiral phenyl dihydrouracil cereblon ligands is prepared. It is then applied to the rapid development of a full PROTAC library targeting Bruton's tyrosine kinase, which can be directly used for screening.
Almodóvar-Rivera CM +5 more
europepmc +2 more sources
The study was conducted to evaluate the toxicological effects, functional observation battery tests, and sexual maturity of semicarbazide oral gavage administration to juvenile Sprague-Dawley rats for 70 days at 0, 15, 30, and 60 mg/kg/day weaning to ...
Vijaykumar Malashetty +2 more
doaj +1 more source
Effects of Acute and Chronic Exposure to Semicarbazide on the Sea Cucumber Apostichopus japonicus
The effects of acute and chronic exposure to semicarbazide were carried out on the sea cucumber Apostichopus japonicus. A half-maximal lethal concentration of 3.72 g/L of semicarbazide hydrochloride (95% confidence interval 3.43–4.02 g/L) was deduced. At
Xiuhui Tian +11 more
doaj +1 more source
A Mechanistic Study on the Non-genotoxic Carcinogenicity of the Food Contaminant Semicarbazide
Semicarbazide was brought to the forefront of scientific discussions by the scientific community in the early 2000’s as the substance was discovered in several food products from both synthetic and natural sources.
Daniel P. Fitzpatrick
doaj +1 more source
Synthesis of 1,6-bis(semicarbazide)hexanes and 1,6-bis(1,2,4-triazol-5-one)hexanes and their antiproliferative and antimicrobial activity [PDF]
A series of 1,6-bis(3-substituted-4,5-dihydro-1H-1,2,4-triazol-5-on-4- yl)hexanes (3a-g) were synthesized by the cyclization reaction of 1,6-bis(1- substituted-semicarbazide-4-yl)hexanes (2a-g) in alkaline medium.
Pitucha M. +3 more
doaj +1 more source
Genomic and experimental evidence for multiple metabolic functions in the RidA/YjgF/YER057c/UK114 (Rid) protein family. [PDF]
BackgroundIt is now recognized that enzymatic or chemical side-reactions can convert normal metabolites to useless or toxic ones and that a suite of enzymes exists to mitigate such metabolite damage.
Cooper, Arthur JL +8 more
core +4 more sources
Study of the inhibitory effect of some thiourea compounds on the activity of enzyme purified polyamine oxidase from the blood of patients with type 1 diabetes [PDF]
The research included determination of polyamine oxidase (PAO) activity in normal and diabeti patients type I females. It was found that the activity of PAO in red blood cells (RBC) and plasma in patients were significantly higher than that of normal ...
Nashwan Abbou +2 more
doaj +1 more source
Azapeptides as an Efficient Tool to Improve the Activity of Biologically Effective Peptides
Peptides are highly potent biological active compounds with excellent selectivity and binding, but they have some drawbacks (e.g., low stability in vivo because of the enzymatic degradation, and fast elimination).
Karima Tarchoun +2 more
doaj +1 more source
Residue analyses and exposure assessment of the Irish population to nitrofuran metabolites from different food commodities in 2009–2010 [PDF]
peer-reviewedAn exposure assessment to nitrofuran residues was performed for three human populations (adults, teenagers and children), based on residue analyses of foods of animal origin (liver, honey, eggs and aquaculture) covering the 2-year period ...
Conroy, Emma-Rose +4 more
core +1 more source

