PMID- 20000124
OWN - NLM
STAT- MEDLINE
DCOM- 20091224
LR  - 20140401
IS  - 2310-6972 (Print)
IS  - 2310-6905 (Linking)
VI  - 55
IP  - 4
DP  - 2009 Jul-Aug
TI  - [Biosensor analysis of interaction of potential dimerization inhibitors with 
      HIV-1 protease].
PG  - 462-78
AB  - Currently inhibitors of protein-protein interactions are considered as 
      perspective prototypes of new generation of drugs. The most attractive targets 
      for such inhibitors are the oligomeric enzymes which active sites are formed by 
      amino acid residues from different subunits. The classic example of such enzyme 
      is HIV protease (HIVp), active only in the homodimeric form. We have developed a 
      new approach for experimental screening of HIVp dimerization inhibitors. It is 
      based on the original biosensoric test-system for differential analysis of 
      interaction of tested substances with HIVp dimers and monomers. Using this 
      test-system we have analyzed the most perspective candidate substances predicted 
      by method of virtual screening, and some derivatives of glycyrrhizin, triterpenic 
      and steroid glycosides. As a result we found one compound, which mainly interacts 
      with HIVp monomers and inhibits in vitro activity of this enzyme with IC50 of 
      about 10(-6) M.
FAU - Ershov, P V
AU  - Ershov PV
FAU - Gnedenko, O V
AU  - Gnedenko OV
FAU - Mol'nar, A A
AU  - Mol'nar AA
FAU - Lisitsa, A V
AU  - Lisitsa AV
FAU - Ivanov, A S
AU  - Ivanov AS
FAU - Archakov, A I
AU  - Archakov AI
LA  - rus
PT  - English Abstract
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
PL  - Russia (Federation)
TA  - Biomed Khim
JT  - Biomeditsinskaia khimiia
JID - 101196966
RN  - 0 (Glycosides)
RN  - 0 (HIV Protease Inhibitors)
RN  - 0 (Steroids)
RN  - 0 (Triterpenes)
RN  - 6FO62043WK (Glycyrrhizic Acid)
RN  - EC 3.4.23.- (HIV Protease)
RN  - EC 3.4.23.- (p16 protease, Human immunodeficiency virus 1)
SB  - IM
MH  - Biosensing Techniques
MH  - Glycosides/chemistry
MH  - Glycyrrhizic Acid/analogs & derivatives/chemistry
MH  - HIV Protease/*chemistry
MH  - HIV Protease Inhibitors/*chemistry
MH  - Models, Molecular
MH  - Protein Multimerization
MH  - Steroids/chemistry
MH  - Structure-Activity Relationship
MH  - Triterpenes/chemistry
EDAT- 2009/12/17 06:00
MHDA- 2009/12/25 06:00
CRDT- 2009/12/17 06:00
PHST- 2009/12/17 06:00 [entrez]
PHST- 2009/12/17 06:00 [pubmed]
PHST- 2009/12/25 06:00 [medline]
PST - ppublish
SO  - Biomed Khim. 2009 Jul-Aug;55(4):462-78.