be230cLecture11

Lowering cholesterol alone appears to be insucient to

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Unformatted text preview: c gene families color ­coded as proteases (purple), lipophilic GPCRs (blue) and kinases (red)). The independent intersecBon of compounds with drug ­ like properBes, that is those in a region of chemical space defined by the possession of absorpBon, distribuBon, metabolism and excreBon properBes consistent with orally administered drugs — ADME space — is shown in green The 'rule ­of ­five’ developed by Lipinski et al. shows that poor absorpBon or permeaBon of a compound are more likely when there are more than five hydrogen ­ bond donors; the molecular mass is more than 500 Da; the lipophilicity is high (expressed as cLogP > 5); and the sum of nitrogen and oxygen atoms is more than 10. These guidelines do not cover drugs that are derived from natural products, for which other absorpBon mechanisms are involved. Value in Promiscuity ...
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This document was uploaded on 04/09/2014.

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