Results 1 to 10 of about 2,022 (94)

Characterization of enzyme activities and cofactors involved in bioactivation and bioinactivation of chemical carcinogens in the tester strains Escherichia coli K12 MX100 and Salmonella typhimurium LT2 TA100. [PDF]

open access: yes, 1997
MX100 is an Escherichia coli K12 genotoxicity tester strain, especially developed for mechanistic studies of chemical mutagens and carcinogens. For the study of the role of specific enzymes in the bioactivation and bioinactivation of carcinogens, it is ...
Rueff, J.   +5 more
core   +2 more sources

Homozygous gene deletions of the glutathione S-transferases M1, and T1 are associated with thimerosal sensitization

open access: yes, 2000
Objective: Thimerosal is an important preservative in vaccines and ophthalmologic preparations. The substance is known to be a type IV sensitizing agent.
Bauer, A.   +10 more
core   +1 more source

In silico prediction of human carboxylesterase-1 (hCES1) metabolism combining docking analyses and MD simulations

open access: yes, 2010
Metabolic problems lead to numerous failures during clinical trials, and much effort is now devoted in developing in silico models predicting metabolic stability and metabolites.
G. Vistoli   +7 more
core   +1 more source

Biocatalytic organofluorine synthesis via hemoprotein-catalyzed carbene transfer reactions

open access: yes, 2021
Thesis (Ph. D.)--University of Rochester. Department of Chemistry, 2020.Protein engineering efforts in our laboratory led to the development of efficient hemoprotein-based biocatalysts for abiological carbene transfer reactions.
Fasan, Rudi, Tinoco Valencia, Antonio
core  

Design, synthesis, and evaluation of sugar amino acid based inhibitors of protein prenyl transferases PFT and PGGT-1

open access: yes, 2004
Eleven analogues of the C-terminal Ca1a2X motif found in natural substrates of the prenyl transferases PFT and PGGT-1 were synthesized and evaluated for their inhibition potency and selectivity against PFT and PGGT-1. Replacement of the central dipeptide
Boom, J.H. van   +8 more
core  

Synthesis and biological evaluation of lipophilic Ca1a 2L analogues as potential bisubstrate inhibitors of protein:geranylgeranyl transferase-1

open access: yes, 2005
Ca1a2L analogues, having the central dipeptide a 1a2 replaced by a sugar amino acid, were provided at the N-terminal end directly or via a spacer with a lipid. The inhibitory potency toward PGGT-1 of the set of lipophilic Ca1a2L analogues was improved in
Overkleeft, H.S.   +7 more
core  

A combinatorial approach toward the generation of ambiphilic peptide-based inhibitors of protein:geranylgeranyl transferase-1

open access: yes, 2005
A combinatorial synthesis of oligopeptide analogues and their evaluation as protein:geranylgeranyl transferase inhibitors is presented. The combinatorial strategy is based on the random mutation, in each new generation, of one of any of the four amino ...
Overkleeft, H.S.   +8 more
core  

Inhibitors of prenylation of Ras and other G-proteins and their application as therapeutics

open access: yes, 2000
Anchoring of small G-proteins to cellular membranes via a covalently bound lipophylic prenyl group is essential for the functioning of these proteins. For example, the farnesylation of Ras by the action of the enzyme protein:farnesyl transferase (PFT) is
Boom, J.H. van   +6 more
core  

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