Fragment-based approaches to enzyme inhibition
نویسندگان
چکیده
منابع مشابه
Fragment based drug design: from experimental to computational approaches.
Fragment based drug design has emerged as an effective alternative to high throughput screening for the identification of lead compounds in drug discovery in the past fifteen years. Fragment based screening and optimization methods have achieved credible success in many drug discovery projects with one approved drug and many more compounds in clinical trials. The fragment based drug design star...
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There has been considerable interest recently in what is known as ;fragment-based lead discovery'. The novel feature of the approach is to begin with small low-affinity compounds. The main advantage is that a larger potential chemical diversity can be sampled with fewer compounds, which is particularly important for new target classes. The approach relies on careful design of the fragment libra...
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Silencing of abnormally activated genes can be accomplished in a highly specific manner using nucleic acid based approaches. The focus of this review includes the different nucleic acid based inhibition strategies such as antisense oligodeoxynucleotides, small interfering RNA (siRNA), dominant-negative constructs, G-quartet oligonucleotides and decoy oligonucleotides, their mechanism of action ...
متن کاملApproaches to enzyme stabilization.
much less stable in both cases (Wiseman et al., 1975). Reduced forms contain Fe", which is a high-spin-state form, and this may explain the lower stability, although there is a possibility of a conformational difference for the Fel* form associated with its mechanistic role in oxygen binding. This is another possible case, therefore, of a mechanistic advantage and stability being mutually exclu...
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Derivatives of phenyl-keto butenoic acids have been reported to be inhibitors of pyruvate decarboxylase, (PDC). The inhibition of transketolase, a thiamine requiring enzyme such as PDF, by meta nitrophenyl derivative of 2-oxo-3-butenoic acid (MNPB) is reported here. These studies indicate that the inhibitor binds to the enzyme at the active site. A two-step inhibition was observed, first th...
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ژورنال
عنوان ژورنال: Current Opinion in Biotechnology
سال: 2007
ISSN: 0958-1669
DOI: 10.1016/j.copbio.2007.09.003