Technological Challenges in Antibiotic Discovery and Development A Workshop Summary (2014) / Chapter Skim
Currently Skimming:
2 Challenges In Overcoming Antibiotic Resistance
2 Challenges In Overcoming Antibiotic Resistance
Pages 7-12
The Chapter Skim interface presents what we've algorithmically identified as the most significant single chunk of text within every page in the chapter.
Select key terms on the right to highlight them within pages of the chapter.
From page 7... ...
Two speakers With each parry by bacteria, medicinal chemists develaddressed these challenges. Lynn Silver, a consultant at LL oped new drugs that were not just molecules copied from Silver Consulting, LLC, discussed the need to select drug others but derivatives of existing antibiotic classes with better targets that are not subject to rapid resistance selection, and pharmacological properties or modifications that overcame Shahriar Mobashery, Professor of Life Sciences at Notre specific resistance mechanisms.
|
From page 8... ...
subject to rapid selection of resistance, and the second is In addition, there is no complete set of general rules or an the use of chemistries that are appropriate for antibacterial agreed upon rational approach to getting drugs into gramdiscovery. "Antibacterial agents have certain physiochemi- negative bacteria.
|
From page 9... ...
Silver noted that the field needs step target-based resistance. to explore additional pathways with similar active sites or Based on this evaluation, Silver concluded that success- ligands, such as the tRNA synthetases, the purine synthesis ful monotherapeutic antibacterials are not subject to single pathway, or cofactor synthesis pathways.
|
From page 10... ...
He noted that is complex, he explained, involving a set of genes whose these resistance mechanisms are complex, multistep pro origins were not from Staphylococcus aureus. The first such cesses, but each step along the way toward manifestation of gene codes for a signal transduction protein, BlaR1, that resistance offers the opportunity for intervention to reverse binds β-lactams irreversibly as a result of a decarboxylation the resistant phenotype.
|
From page 11... ...
Indeed, In response to a question about the use of nanotechnology ceftaroline, a fifth-generation cephalosporin that is active to develop novel antibiotics that might overcome resistance, against MRSA, appears to overcome resistance by binding Silver said that this is an avenue worth pursuing, but that she to mutated PBP2a at the allosteric site. Binding to the allo- worried about toxicity.
|
From page 12... ...
2011. Crystal structures of and that it may be possible to find compounds that are not bacterial peptidoglycan amidase AmpD and an unprecedented activation β-lactams that would bind to the allosteric site and synergize mechanism.
|
Key Terms
This material may be derived from roughly machine-read images, and so is provided only to facilitate research.
More
information on Chapter Skim is available.