JE-2147: a dipeptide protease inhibitor (PI) that potently inhibits multi-PI-resistant HIV-1.

@article{Yoshimura1999JE2147AD,
  title={JE-2147: a dipeptide protease inhibitor (PI) that potently inhibits multi-PI-resistant HIV-1.},
  author={K. Yoshimura and R. Kato and K. Yusa and M. Kavlick and V. Maroun and A. Nguyen and T. Mimoto and T. Ueno and M. Shintani and J. Falloon and H. Masur and H. Hayashi and J. Erickson and H. Mitsuya},
  journal={Proceedings of the National Academy of Sciences of the United States of America},
  year={1999},
  volume={96 15},
  pages={
          8675-80
        }
}
  • K. Yoshimura, R. Kato, +11 authors H. Mitsuya
  • Published 1999
  • Biology, Medicine
  • Proceedings of the National Academy of Sciences of the United States of America
We designed, synthesized, and identified JE-2147, an allophenylnorstatine-containing dipeptide HIV protease inhibitor (PI), which is potent against a wide spectrum of HIV-1, HIV-2, simian immunodeficiency virus, and various clinical HIV-1 strains in vitro. Drug-resistant clinical HIV-1 strains, isolated from seven patients who had failed 9-11 different anti-HIV therapeutics after 32-83 months, had a variety of drug-resistance-related amino acid substitutions and were highly and invariably… Expand
View on PubMed
pnas.org
87 Citations
Highly Influential Citations
3
Background Citations
28
Methods Citations
29
Results Citations
7

87 Citations

Citation Type

Citation Type

Unusual binding mode of an HIV-1 protease inhibitor explains its potency against multi-drug-resistant virus strains.
  • 37
GRL-02031, a Novel Nonpeptidic Protease Inhibitor (PI) Containing a Stereochemically Defined Fused Cyclopentanyltetrahydrofuran Potent against Multi-PI-Resistant Human Immunodeficiency Virus Type 1 In Vitro
  • 38
  • PDF
A Potent Human Immunodeficiency Virus Type 1 Protease Inhibitor, UIC-94003 (TMC-126), and Selection of a Novel (A28S) Mutation in the Protease Active Site
  • 120
  • PDF
GRL-0519, a Novel Oxatricyclic Ligand-Containing Nonpeptidic HIV-1 Protease Inhibitor (PI), Potently Suppresses Replication of a Wide Spectrum of Multi-PI-Resistant HIV-1 Variants In Vitro
  • 21
  • PDF
C-5-Modified Tetrahydropyrano-Tetrahydofuran-Derived Protease Inhibitors (PIs) Exert Potent Inhibition of the Replication of HIV-1 Variants Highly Resistant to Various PIs, including Darunavir
  • 10
  • PDF
Design of inhibitors against HIV, HTLV-I, and Plasmodium falciparum aspartic proteases
  • 32
Small-sized human immunodeficiency virus type-1 protease inhibitors containing allophenylnorstatine to explore the S2' pocket.
  • 15
Novel Protease Inhibitors Containing C-5-Modified bis-Tetrahydrofuranylurethane and Aminobenzothiazole as P2 and P2′ Ligands That Exert Potent Antiviral Activity against Highly Multidrug-Resistant HIV-1 with a High Genetic Barrier against the Emergence of Drug Resistance
  • 3
  • PDF
Characterisation of mutated proteinases derived from hiv-positive patients: Enzyme activity, vitality and inhibition
  • 6
Inhibition of HIV-1 replication by a peptide dimerization inhibitor of HIV-1 protease.
  • 32
...
1
2
3
4
5
...

References

SHOWING 1-10 OF 21 REFERENCES
In vitro anti-human immunodeficiency virus (HIV) activities of transition state mimetic HIV protease inhibitors containing allophenylnorstatine.
  • 85
  • PDF
Structure-activity relationship of small-sized HIV protease inhibitors containing allophenylnorstatine.
  • 58
Structure of HIV-1 protease with KNI-272, a tight-binding transition-state analog containing allophenylnorstatine.
  • 108
In vivo emergence of HIV-1 variants resistant to multiple protease inhibitors
  • 962
HIV-2 EHO isolate has a divergent envelope gene and induces single cell killing by apoptosis.
  • 37
Selection and analysis of human immunodeficiency virus type 1 variants with increased resistance to ABT-538, a novel protease inhibitor.
  • 214
  • PDF
Drug resistance during indinavir therapy is caused by mutations in the protease gene and in its Gag substrate cleavage sites.
  • 345
  • PDF
Kinetic characterization and cross-resistance patterns of HIV-1 protease mutants selected under drug pressure.
  • 242
Selection of multiple human immunodeficiency virus type 1 variants that encode viral proteases with decreased sensitivity to an inhibitor of the viral protease.
  • 172
  • PDF
In vitro induction of human immunodeficiency virus type 1 variants resistant to 2'-beta-Fluoro-2',3'-dideoxyadenosine.
  • 26
  • PDF
...
1
2
3
...