Crystal Structure of HsEg5 in Complex with S-trityl-L-cysteine
نویسندگان
چکیده
منابع مشابه
Org . On Cysteine and Cystine Peptides . Part V . l S - Trityl - and S - Diphenyl - methyl - cysteine and - cysteine Peptides
A new method for the preparation of S-trityl(i.e. triphenylmethyl) and S-diphenylmethyl-cysteines or -cysteine peptides involves treatment of cysteine or cysteine peptides with aralkylcarbinols in the presence of trifluoroacetic acid or hydrogen halides in acetic acid solution. The optimal conditions for the removal of these S-protecting aralkyl groups by trifluoroacetic acid or hydrogen halide...
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Derivatives of aziridinecarboxylates play an im portant role in bioorganic chemistry, e.g. for the syn thesis of amino acids [1-3], antibiotics [4, 5] and selective inhibitors [6]. Recently, we reported that 2-aziridinecarboxylic acid may represent a promis ing handle to develop aziridine-containing com pounds as a new class of cysteine proteinase inhibi tors [7], In this context 1 could c...
متن کاملDocetaxel-resistant prostate cancer cells remain sensitive to S-trityl-L-cysteine-mediated Eg5 inhibition.
Castrate-resistant prostate cancer remains a major clinical challenge. Due to the toxicity profile of taxane-based chemotherapy and treatment failure in some patients, novel agents with improved efficacy to side effect profiles are urgently needed. Eg5, a member of the kinesin-5 family, controls the formation of the bipolar spindle during cell division, and suppressed Eg5 function leads to mito...
متن کاملS-trityl-L-cysteine is a reversible, tight binding inhibitor of the human kinesin Eg5 that specifically blocks mitotic progression.
Human Eg5, responsible for the formation of the bipolar mitotic spindle, has been identified recently as one of the targets of S-trityl-L-cysteine, a potent tumor growth inhibitor in the NCI 60 tumor cell line screen. Here we show that in cell-based assays S-trityl-L-cysteine does not prevent cell cycle progression at the S or G(2) phases but inhibits both separation of the duplicated centrosom...
متن کاملS-Trityl-L-cysteine Is a Reversible, Tight Binding Inhibitor of the Human Kinesin Eg5 That Specifically Blocks
From the Laboratoire des Protéines du Cytosquelette and Laboratoire de Moteurs Moléculaires, Institut de Biologie Structurale (Commissariat à l’Energie Atomique-CNRS-UJF), 41 Rue Jules Horowitz, 38027 Grenoble Cedex 01, France, Laboratoire du Cytosquelette, INSERM Unite 366, Commissariat à l’Energie Atomique, 38054 Grenoble Cedex 9, France, Laboratoire de Chimie Organique Appliquée, Institut Gi...
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ژورنال
عنوان ژورنال: Biophysical Journal
سال: 2009
ISSN: 0006-3495
DOI: 10.1016/j.bpj.2008.12.2617