A complete gene cluster from Streptomyces nanchangensis NS3226 encoding biosynthesis of the polyether ionophore nanchangmycin [0.03%]
Yuhui Sun,Xiufen Zhou,Hui Dong et al.
Yuhui Sun et al.
The PKS genes for biosynthesis of the polyether nanchangmycin are organized to encode two sets of proteins (six and seven ORFs, respectively), but are separated by independent ORFs that encode an epimerase, epoxidase, and epoxide hydrolase,...
Characterization of the mupirocin biosynthesis gene cluster from Pseudomonas fluorescens NCIMB 10586 [0.03%]
A Kassem El-Sayed,Joanne Hothersall,Sian M Cooper et al.
A Kassem El-Sayed et al.
The polyketide antibiotic mupirocin (pseudomonic acid) produced by Pseudomonas fluorescens NCIMB 10586 competitively inhibits bacterial isoleucyl-tRNA synthase and is useful in controlling Staphylococcus aureus, particularly methicillin-res...
Rational design and molecular diversity for the construction of anti-alpha-bungarotoxin antidotes with high affinity and in vivo efficiency [0.03%]
Luisa Lozzi,Barbara Lelli,Ylenia Runci et al.
Luisa Lozzi et al.
The structure of peptide p6.7, a mimotope of the nicotinic receptor ligand site that binds alpha-bungarotoxin and neutralizes its toxicity, was compared to that of the acetylcholine binding protein. The central loop of p6.7, when complexed ...
Comparative Study
Chemistry & biology. 2003 May;10(5):411-7. DOI:10.1016/s1074-5521(03)00094-2 2003
Chemical genetic modifier screens: small molecule trichostatin suppressors as probes of intracellular histone and tubulin acetylation [0.03%]
Kathryn M Koeller,Stephen J Haggarty,Brian D Perkins et al.
Kathryn M Koeller et al.
Histone deacetylase (HDAC) inhibitors are being developed as new clinical agents in cancer therapy, in part because they interrupt cell cycle progression in transformed cell lines. To examine cell cycle arrest induced by HDAC inhibitor tric...
Multidimensional chemical genetic analysis of diversity-oriented synthesis-derived deacetylase inhibitors using cell-based assays [0.03%]
Stephen J Haggarty,Kathryn M Koeller,Jason C Wong et al.
Stephen J Haggarty et al.
Systematic chemical genetics aims to explore the space representing interactions between small molecules and biological systems. Beyond measuring binding interactions and enzyme inhibition, measuring changes in the activity of proteins in i...
Understanding HTLV-I protease [0.03%]
Suzanne Beckham Shuker,Victoria L Mariani,Bryan E Herger et al.
Suzanne Beckham Shuker et al.
Nicole Ballew
Nicole Ballew
Joseph M Jez,Julian C-H Chen,Giulio Rastelli et al.
Joseph M Jez et al.
Hsp90 is an attractive chemotherapeutic target because it chaperones the folding of proteins found in multiple signal transduction pathways. We describe the 1.75 A resolution crystal structure of human Hsp90 alpha (residues 9-236) complexed...
Rational engineering of a DNA glycosylase specific for an unnatural cytosine:pyrene base pair [0.03%]
Keehwan Kwon,Yu Lin Jiang,James T Stivers
Keehwan Kwon
A novel site-specific cytosine DNA glycosylase has been rationally engineered from the active site scaffold of the DNA repair enzyme uracil DNA glycosylase (UDG). UDG, which operates by a nucleotide flipping mechanism, was first converted i...
Crystal structure of human carboxylesterase 1 complexed with the Alzheimer's drug tacrine: from binding promiscuity to selective inhibition [0.03%]
Sompop Bencharit,Christopher L Morton,Janice L Hyatt et al.
Sompop Bencharit et al.
Human carboxylesterase 1 (hCE1) is a broad-spectrum bioscavenger that plays important roles in narcotic metabolism, clinical prodrug activation, and the processing of fatty acid and cholesterol derivatives. We determined the 2.4 A crystal s...