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Literature summary for 3.4.23.B4 extracted from

  • Heaslet, H.; Lin, Y.C.; Tam, K.; Torbett, B.E.; Elder, J.H.; Stout, C.D.
    Crystal structure of an FIV/HIV chimeric protease complexed with the broad-based inhibitor, TL-3 (2007), Retrovirology, 4, 1.
    View publication on PubMedView publication on EuropePMC

Crystallization (Commentary)

Crystallization (Comment) Organism
crystal structure (1.7 A) of FIV protease is obtained in which 12 critical residues around the active site have been substituted with the structurally equivalent residues of HIV PR (12XFIV PR). The chimeric PR is crystallized in complex with inhibitor TL-3. Comparison of the crystal structures of the TL-3 complexes of 12X FIV and wild-type FIV PR reveal the information of additional van der Waals interactions between the enzyme inhibitor in the mutant PR feline immunodeficiency virus

Protein Variants

Protein Variants Comment Organism
I37V/N55M/M56I/I57G/V59I/G62F/K63I/L97T/I98P/Q99V/P100N/L101I crystal structure (1.7 A) of FIV protease is obtained in which 12 critical residues around the active site have been substituted with the structurally equivalent residues of HIV PR (12XFIV PR). The chimeric PR is crystallized in complex with inhibitor TL-3. Comparison of the crystal structures of the TL-3 complexes of 12X FIV and wild-type FIV PR reveal the information of additional van der Waals interactions between the enzyme inhibitor in the mutant PR. The 12X FIV PR retains the hydrogen bonding interactions between residues in the flap regions and active site involving the enzyme and the TL-3 inhibitor in comparison to both FIV PR and HIV PR. However, the flap regions of the 12X FIV PR more closely resemble those of HIV PR, having gained several stabilizing intra-flap interactions not present in wild type FIV PR feline immunodeficiency virus

Inhibitors

Inhibitors Comment Organism Structure
N-[benzyloxycarbonyl]-L-Ala-N-[(1S)-1-benzyl-2-hydroxyethyl]-L-valinamide ie. TL-3 feline immunodeficiency virus

Organism

Organism UniProt Comment Textmining
feline immunodeficiency virus P16088
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-

Synonyms

Synonyms Comment Organism
FIV protease
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feline immunodeficiency virus