Total chemical synthesis of a D-enzyme: the enantiomers of HIV-1 protease show reciprocal chiral substrate specificity [corrected]

Science ◽  
1992 ◽  
Vol 256 (5062) ◽  
pp. 1445-1448 ◽  
Author(s):  
R. Milton ◽  
S. Milton ◽  
S. Kent
Keyword(s):  
Substrate Specificity ◽  
Chemical Synthesis ◽  
Hiv 1

Molecular Docking, Synthesis and anti-HIV-1 Protease Activity of Novel Chalcones

2020 ◽  
Vol 26 (8) ◽  
pp. 802-814 ◽  
Author(s):  
Nemanja Turkovic ◽  
Branka Ivkovic ◽  
Jelena Kotur-Stevuljevic ◽  
Milica Tasic ◽  
Bojan Marković ◽  
...  
Keyword(s):  
Molecular Weight ◽  
Molecular Docking ◽  
Chemical Synthesis ◽  
Protease Activity ◽  
Molecular Mechanisms ◽  
Replication Cycle ◽  
Low Molecular Weight ◽  
Chalcone Derivatives ◽  
Anti Hiv ◽  
Hiv 1

Background: Since the beginning of the HIV/AIDS epidemic, 75 million people have been infected with the HIV and about 32 million people have died of AIDS. Investigation of the molecular mechanisms critical to the HIV replication cycle led to the identification of potential drug targets for AIDS therapy. One of the most important discoveries is HIV-1 protease, an enzyme that plays an essential role in the replication cycle of HIV. Objective: The aim of the present study is to synthesize and investigate anti-HIV-1 protease activity of some chalcone derivatives with the hope of discovering new lead structure devoid drug resistance. Methods: 20 structurally similar chalcone derivatives were synthesized and their physico-chemical characterization was performed. Binding of chalcones to HIV-1 protease was investigated by fluorimetric assay. Molecular docking studies were conducted to understand the interactions. Results: The obtained results revealed that all compounds showed anti-HIV-1 protease activity. Compound C1 showed the highest inhibitory activity with an IC50 value of 0.001 μM, which is comparable with commercial product Darunavir. Conclusion: It is difficult to provide general principles of inhibitor design. Structural properties of the compounds are not the only consideration; ease of chemical synthesis, low molecular weight, bioavailability, and stability are also of crucial importance. Compared to commercial products the main advantage of compound C1 is the ease of chemical synthesis and low molecular weight. Furthermore, compound C1 has a structure that is different to peptidomimetics, which could contribute to its stability and bioavailability.

Chemical Synthesis of 19F-labeled HIV-1 Protease using Fmoc-Chemistry and ChemMatrix Resin

2007 ◽  
Vol 13 (1-2) ◽  
pp. 221-227 ◽  
Author(s):  
Silvia Frutos ◽  
Judit Tulla-Puche ◽  
Fernando Albericio ◽  
Ernest Giralt
Keyword(s):  
Chemical Synthesis ◽  
Fmoc Chemistry ◽  
Hiv 1 ◽  
Chemmatrix Resin

Substrate specificity in HIV-1 protease by a biased sequence search method

2006 ◽  
Vol 64 (2) ◽  
pp. 444-456 ◽  
Author(s):  
Nevra Ozer ◽  
Turkan Haliloglu ◽  
Celia A. Schiffer
Keyword(s):  
Substrate Specificity ◽  
Search Method ◽  
Sequence Search ◽  
Hiv 1

Studies on the total chemical synthesis of crystalline [Aba67,95,167,195]HIV-1 proteinase

Peptides 1990 ◽  
1991 ◽  
pp. 172-173 ◽  
Author(s):  
Stephen B. H. Kent ◽  
Dianne Alewood ◽  
John L. Andrews ◽  
Doug Bergman ◽  
Ross Brinkworth ◽  
...  
Keyword(s):  
Chemical Synthesis ◽  
Hiv 1

Chemical synthesis and expression of a gene encoding HIV-1 TAT protein

1989 ◽  
Vol 160 (3) ◽  
pp. 1429-1437 ◽  
Author(s):  
B.Q. Ferguson ◽  
B.K. Friedland ◽  
E. Hendrickson ◽  
L. Strehl ◽  
S.R. Petteway ◽  
...  
Keyword(s):  
Chemical Synthesis ◽  
Tat Protein ◽  
Gene Encoding ◽  
Hiv 1
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