Linear indices of the 'macromolecular graph's nucleotides adjacency matrix' as a promising approach for bioinformatics studies. Part 1: prediction of paromomycin's affinity constant with HIV-1 psi-RNA packaging region

Bioorg Med Chem. 2005 May 16;13(10):3397-404. doi: 10.1016/j.bmc.2005.03.010.

Abstract

The design of novel anti-HIV compounds has now become a crucial area for scientists around the world. In this paper a new set of macromolecular descriptors (that are calculated from the macromolecular graph's nucleotide adjacency matrix) of relevance to nucleic acid QSAR/QSPR studies, nucleic acids' linear indices. A study of the interaction of the antibiotic Paromomycin with the packaging region of the HIV-1 psi-RNA has been performed as example of this approach. A multiple linear regression model predicted the local binding affinity constants [Log K (10(-4) M(-1))] between a specific nucleotide and the aforementioned antibiotic. The linear model explains more than 87% of the variance of the experimental Log K (R = 0.93 and s = 0.102 x 10(-4) M(-1)) and leave-one-out press statistics evidenced its predictive ability (q2 = 0.82 and s(cv) = 0.108 x 10(-4) M(-1)). The comparison with other approaches (macromolecular quadratic indices, Markovian Negentropies and 'stochastic' spectral moments) reveals a good behavior of our method.

MeSH terms

  • Anti-Bacterial Agents / chemistry*
  • Base Pairing
  • Base Sequence
  • Computational Biology*
  • DNA Footprinting
  • Drug Design
  • HIV-1 / chemistry*
  • Humans
  • Models, Chemical
  • Models, Molecular*
  • Molecular Sequence Data
  • Paromomycin / chemistry*
  • Predictive Value of Tests
  • Quantitative Structure-Activity Relationship
  • RNA, Viral / chemistry*
  • RNA, Viral / metabolism
  • Sequence Analysis, RNA*
  • Software

Substances

  • Anti-Bacterial Agents
  • RNA, Viral
  • Paromomycin