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lecture 8
lecture 8
15
Chemical Engineering
Post-Graduate
10/22/2013

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Term
What are 4 reasons to screen for novel exometabolites
Definition
to detect new and useful biological and pharmacological activity
to find new and patentable structures for semi synthesis, analogue development
to find new related strucutres with reduced side effects, broader spectrum, better delivery, patentability
Term
what are the critical limitations of metbolomics (transcriptome, proteasome, when searching for genes encoding antibiotic biosynthesis enzymes?
Definition
growth conditions, metabolite detection
Term
What are the 6 chemical classes of antibiotics?
Definition
1. beta lactams
2. b lactamase inhibitors
3. aminoglycosides
4. tetracyclines, polyketides
5. macrolides
6. peptides
Term
The antiinfective compound market is ___ and ___
Definition
large and growing
Term
since only __% of all soil microbes can be grown in the lab, __may open the door to a host of previously inaccessible antibiotic biosynthetic genes from unculturable microbes
Definition
1%, mutagenesis
Term
why search for new antibiotics?
Definition
resistance
Term
in regards to penicillin and vancomycin, provide the year of FDA approval, year of first reported resistance event, observed resistance, and subsequent drugs developed to counteract the resistant strain
Definition
penicillin 1943, first reported resistance 1940
drugs developed - cephalosporins, oxacillin
vancomysin 1972, 1987, quiopristomn
Term
Drug in 1936
Definition
sulfa
Term
Drug in 1940
Definition
Beta lactams
Term
drug in 1949
Definition
chloramphenicol tetracyclines
Term
drug in 2000
Definition
oxazolidinoes
Term
drug in 1958
Definition
glycopeptides
Term
New methods developed by ___ screening are being used to detect new compounds synthesized by ___
Definition
genomics, silent biosynthetic pathways
Term
What results were achieved from 1930 to 1960 with regards to core structures and what new methods were developed from 1990 to 2010 that enabled genomic screening for sbps?
Definition
1930-1960- (penicillin, streptomycin, DNA, bacterial operon sequenced)
1990-2010- fully microbial gene sequenced, structures predicted from gene sequence, co-culture technique)
Term
based on the diagram below identify each step in the overall screening process in novel lead compounds
Definition
draw
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