PubMed Health⌕ Search

Biomedical subjects

A A Krayevsky

Publications and source records attributed to A A Krayevsky.

54 records · Page 3Linked to original sources

Catalysis of the peptide bond formation by 50 S subunits of E. coli ribosomes with N-(formyl) methionine ester of adenylic acid as peptide donor.

50 S subunits of E. coli ribosomes catalyze the reaction of the 2'(3')-N-(formyl) methionine ester of adenosine 5'-phosphate and Phe-tRNA resulting in peptide bond synthesis. Cytidine 5'-phosphate stimulates this process on 50 S ribosomal subunits as well as on intact ribosomes. The obtained data show that the areas of the peptidyltransferase donor site which binds the 3'-terminal fragment of peptidyl-tRNA possess completely formed structures on 50 S ribosomal subunits.

Acyltransferases↗

Peptidyl transferase centre of bacterial ribosomes: substrate specificity and binding sites.

A detailed scheme of the Peptidyl Transferase Centre of bacterial ribosomes is proposed by summarizing the literature data on the substrate specificity of the acceptor and donor sites. According to the proposed scheme only the elements of the donor and acceptor having a stable structure bind with the ribosome. The present paper proposes such main elements for the donor and acceptor.

Acyltransferases↗

Thioacyl esters of nucleotides: synthesis of 3'(2')-O-thiobenzoyl nucleoside 5'-phosphates.

The synthesis of 3'(2')-O-thiobenzoyl nucleoside 5'-phosphates based on the condensation of N-(thiobenzoyl)-imidazole with nucleside 5'-phosphates was carried out. The UV absorption spectra, CD spectra, PMR spectra and chromatographic and electrophoretic characteristics of synthesized compounds were obtained. By means of PMR it was shown that the 2':3' isomer ratio in water at ambient temperature is about 2:3.

Benzoates↗

P-(alkyl)-nucleoside 5'-hydrogenphosphonates as depot forms of antiviral nucleotide analogues.

P-(Alkyl)esters of AZT 5'-hydrogenphosphonate were synthesized and their stabilities in the phosphate buffer and human serum were evaluated. The esters bearing residues of primary and secondary alcohols were degraded to give AZT, whereas those containing tertiary alkyl groups yielded AZT 5'-hydrogenphosphonate. The corresponding derivatives of d2A and d4T showed the same properties.

Anti-HIV Agents↗

Reasons and limits of substrate activity of modified L-dNTP in DNA biosynthesis.

Theoretical and experimental analysis of interaction of modified D- and L- dNTP as substrates for template-dependent and template-independent DNA polymerases was performed. It is shown that if the modified nucleoside 5'-triphosphates do not contain a substituent in position 3' DNA chains can be extended by both strereoisomeric series with the same kinetic parameters. But the presence of even a 3'-hydroxy group in L-dNTP prevents their incorporation into the DNA chain.

DNA Replication↗

Antiviral activity and resistance profile of phosphazid--a novel prodrug of AZT.

Both AZT and its novel 5'-hydrogen phosphonate derivative, Phosphazid, possess similar in vitro activity and resistance profiles. Experiments involving AZT-resistant virus isolates revealed a strong correlation between resistance to AZT and cross-resistance to Phosphazid. In vitro selection for resistance to Phosphazid yielded viruses that were about 15-fold less sensitive than wild-type virus to this drug. Sequencing of the reverse transcriptase region of seven Phosphazid-selected viruses revealed a single codon mutation, D67N, that is associated with resistance to AZT.

Anti-HIV Agents↗

Anti-HIV activity of novel phosphonate derivatives of AZT, d4T, and ddA.

Anti-HIV activity and cytotoxicity were tested for novel phosphonate derivatives of AZT, d4T and ddA. For d4T phosphonate derivatives the most active was 2',3'-Dideoxy-2',3'-didehydrothymidine 5'-isopropylphosphite and among the AZT phosphonate derivatives highest activity was shown by 2',3'-Dideoxy-3'-azidothymidine 5'-cyclohexylphosphite.

Anti-HIV Agents↗