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1To determine whether the compounds inhibited bromodomain-histone binding we utilized a peptide displacement assay based on AlphaScreen technology.
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2 to investigate the selectivity of these compounds against other bromodomain, we employed a binding assay based on protein stablity shift.
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3 To order to confirm that the dimethylisoxazole moiety was acting as a KAc minic and to elucidate structure-activity profiles for these compounds , we obtained the cocrystal structures of -------.
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zhang881007

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cz_rubygd: ½ð±Ò+4, лл£¬protein stablity shiftÊÇʲôÇé¿ö£¿ 2013-01-06 22:54:33
Сµ¤Ä¾Ä¾: ½ð±Ò+3, ¹ÄÀø½»Á÷ 2013-01-07 16:30:31
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1. alpha Screen:  http://www.proteomebinders.org/meetings/alpbach/talks/Chevet.pdf
2.A bromodomain is a protein domain that recognizes acetylated lysine residues such as those on the N-terminal tails of histonesËùÒÔÊDzⶨ»¯ºÏÎï¶ÔBromodomain»îÐÔµÄÒÖÖÆ×÷ÓÃ
3.ÕâÊÇÑо¿µ°°×½á¹¹ÐÔÖʵķ½·¨£¬¿ÉÒÔÔĶÁ±¾ÎÄhttp://www.ncbi.nlm.nih.gov/pubmed/21674662
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ccharlien

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cz_rubygd: ½ð±Ò+2, лл 2013-01-06 22:54:27
Сµ¤Ä¾Ä¾: ½ð±Ò+2, ¹ÄÀø½»Á÷ 2013-01-07 16:30:47
3. ʵÑéÊÒÀïKAc Ò»°ãÊÇ´×Ëá¼ØµÄËõд£¨Potassium acetate£©£¬Ã»ÓÐÉÏÏÂÎÄ£¬²»È·¶¨
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zhang881007

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cz_rubygd: ½ð±Ò+2, лл£¡Âé·³½üÁ½Ìì¹Ø×¢ÎÒÔÚÉúÎï°å¿éµÄÆäËûÇóÖúÌû£¬¹ØÓÚ·Ö×Ó¶Ô½ÓµÄ 2013-01-07 13:09:30
KAc, ÄãµÃ¿´¿´ÎÄÖÐÊÇ·ñÏà·û¡£ÎÒ¸øÄãµÄÎÄÏ×ÓÐһƪ¾ÍÊÇ×östability shift¡£ ÀýÈ磬ÄãÓÃÈȱäÐÔÀ´¿¼²ìµ°°×Îȶ¨ÐÔ£¬ ÓÉÓÚÌõ¼þµÄ¸Ä±ä£¬¼Óµ×Î µÃµ½µÄÇúÏßÓëÎÞµ×ÎïµÄ¾Í²»Ò»Ö¡£Õâ¾ÍÊÇÎȶ¨ÐÔÆ¯ÒÆ£¡
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