Analyzing Resistance to Design Selective Chemical Inhibitors for AAA Proteins
نویسندگان
چکیده
منابع مشابه
Selective chemical inactivation of AAA proteins reveals distinct functions of proteasomal ATPases.
BACKGROUND The 26S proteasome contains six highly related ATPases of the AAA family. We have developed a strategy that allows selective inhibition of individual proteasomal ATPases in the intact proteasome. Mutation of a threonine in the active site of Sug1/Rpt6 or Sug2/Rpt4 to a cysteine sensitizes these proteins to inactivation through alkylation by the sulfhydryl modifying agent NEM. Using t...
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متن کاملPharmacophore Based Virtual Screening Approach to Identify Selective PDE4B Inhibitors
Phosphodiesterase 4 (PDE4) has been established as a promising target in asthma andchronic obstructive pulmonary disease. PDE4B subtype selective inhibitors are known toreduce the dose limiting adverse effect associated with non-selective PDE4B inhibitors. Thismakes the development of PDE4B subtype selective inhibitors a desirable research goal. Toachieve this goal, ligand based pharmacophore m...
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ژورنال
عنوان ژورنال: Cell Chemical Biology
سال: 2019
ISSN: 2451-9456
DOI: 10.1016/j.chembiol.2019.06.001