Learn More
High-resolution X-ray structures of the complexes of HIV-1 protease (HIV-1PR) with peptidomimetic inhibitors reveal the presence of a structural water molecule which is hydrogen bonded to both the mobile flaps of the enzyme and the two carbonyls flanking the transition-state mimic of the inhibitors. Using the structure-activity relationships of C2-symmetric(More)
The molecular mechanism of carboplatin [cis-1,1-cyclobutanedicarboxylatodiammineplatinum(II)] activation is still unresolved. We studied the binding of carboplatin to calf thymus DNA in the presence of thiourea, glutathione, and human breast cancer MCF-7 cell cytoplasmic extracts by measurement of DNA-dependent ethidium bromide fluorescence and atomic(More)
We present several novel P1/P1' substituents that can replace the characteristic benzyl P1/P1' moiety of the cyclic urea based HIV protease inhibitor series. These substituents typically provide 5-10-fold improvements in binding affinity compared to the unsubstituted benzyl analogs. The best substituent was the 3,4-(ethylenedioxy)benzyl group. Proper(More)
Recent reports have shown that pH could also be used as a melting factor to monitor helix-coil transitions in DNA; the results being comparable to those obtained by Tm studies. The rapidity with which the method can be performed to obtain similar transition curves, and elimination of the evaporation factor (at high temperatures as seen in Tm studies) is one(More)
We have studied the cleavage of radioactively labelled double stranded d(GGAATTCC) in single turnover experiments with substrate and enzyme concentration both being in the ~M range. As can be seen in fig. I the reaction rate increases with enzyme concentration until a 1:1 ratio of substrate and enzyme (dimeric form) is reached, when the enzyme concentration(More)
Temperature jump and stopped flow methods were used to study at pH 6.3 and pH 7.0 the temperature dependence of elementary steps of the reactions of lysozyme with the /3(1 + 4)-linked trimer, tetramer, and hexamer of N-acetylglucosamine. The steady state rate of cleavage of the hexasaccharide was determined as a function of temperature (5”-40”) and pH (2 to(More)
  • 1