be230cLecture11

Cyp cytochrome p450 cys cysteine nhr nuclear hormone

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Unformatted text preview:   Diversity libraries designed to represent ideal ADMET space, drug ­like properBes, and bind to funcBonal domains of proteins that are considered “druggable”, such as kinases and GPCRs. •  Advantage of promiscuity is that individual compounds can bind to mulBple proteins, increasing likelihood of finding a drug for the protein of interest. •  Disadvantage from perspecBve of interrogaBng the proteome is that idenBfying the target is extraordinarily challenging. •  From a clinical perspecBve, some lack of selecBvity could contribute to a beTer drug, for instance by inhibiBng mulBple proteins (e.g. kinases) Value of Non ­selecBve InteracBons with Targets Bridging the in vitro–in vivo divide. (a) Discovering small molecules using in vitro screens oten leads to molecules that cause undesirable effects in vivo. Although high ­throughput screening (HTS) may idenBfy a small molecule that inhibits t...
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This document was uploaded on 04/09/2014.

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