CRYSTAL STRUCTURE OF A DEACETYLASE AND INHIBITORS THEREOF
摘要
The present invention provides three-dimensional structural information from the hyperthermophilic bacterium Aquifex aeolicus which is a histone deacetylase-like protein (HDLP). HDLP shares 35.2% amino acid sequence identity with human histone deacetylase (HDAC1). The present invention furth er provides three-dimensional structural information of HDLP bound by inhibitor molecules. The three-dimensional structural information of the present invention is useful to design, isolate and screen deacetylase inhibitor compounds capable of inhibiting HDLP, HDAC family members and HDLP-related molecules. The invention also relates to nucleic acids encoding a mutant HDL P which facilitates the determination of the three-dimensional structure of HD LP in the presence of a zinc atom.
申请公布号
CA2383885(A1)
申请公布日期
2001.03.15
申请号
CA20002383885
申请日期
2000.09.08
申请人
THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK;SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCH
发明人
PAVLETICH, NIKOLA;BRESLOW, RONALD;FINNIN, MICHAEL;RICHON, VICTORIA;DONIGIAN, JILL;MARKS, PAUL A.;RIFKIND, RICHARD A.