Eddy Arnold

TL;DR: Structural studies showed that this inhibitor and other diarylpyrimidine (DAPY) analogues can adapt to changes in the NNRTI-binding pocket in several ways, and adaptations appear to be critical for potency against wild-type and a wide range of drug-resistant mutant HIV-1 RTs.

TL;DR: Analysis of HIV-1 strains isolated at various times during therapy showed that the Q151M mutation developed first in vivo, at the time when the viremia level suddenly increased, followed by the F116Y and F77L mutations, and all five mutations ultimately developed, and the viresmia level rose even further.

TL;DR: A novel self-regulatory mechanism is proposed for HcIDH that mimics the phosphorylation mechanism used by the bacterial homologs, consistent with biochemical and biological data and might be applicable to other eukaryotic NADP-IDHs.

TL;DR: Crystal structures of functional transcription initiation complexes comprising Thermus thermophilus RNA polymerase, σA, and a promoter DNA fragment corresponding to the transcription bubble and downstream double-stranded DNA of the RNAP-promoter open complex show that σ recognize the –10 element and discriminator element through interactions that include the unstacking and insertion into pockets of three DNA bases and that RNAP recognizes the –4/+2 region.

TL;DR: R278474, a new diarylpyrimidine (DAPY) non-nucleoside reverse transcriptase inhibitor (NNRTI), appears to meet criteria and to be suitable for high compliance oral treatment of HIV-1 infection.