High-throughput docking for lead generation

被引:293
作者
Abagyan, R
Totrov, M
机构
[1] Scripps Res Inst, Dept Mol Biol, La Jolla, CA 92037 USA
[2] Molsoft, La Jolla, CA 92037 USA
关键词
D O I
10.1016/S1367-5931(00)00217-9
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
Recent improvements in flexible docking technology may lead to a bigger role for computational methods in lead discovery. Although fast and accurate computational prediction of binding affinities for an arbitrary molecule is still beyond the limits of current methods, the docking and screening procedures can select small sets of likely lead candidates from large libraries of either commercially or synthetically available compounds.
引用
收藏
页码:375 / 382
页数:8
相关论文
共 77 条
[1]   OPTIMAL PROTOCOL AND TRAJECTORY VISUALIZATION FOR CONFORMATIONAL SEARCHES OF PEPTIDES AND PROTEINS [J].
ABAGYAN, R ;
ARGOS, P .
JOURNAL OF MOLECULAR BIOLOGY, 1992, 225 (02) :519-532
[2]   BIASED PROBABILITY MONTE-CARLO CONFORMATIONAL SEARCHES AND ELECTROSTATIC CALCULATIONS FOR PEPTIDES AND PROTEINS [J].
ABAGYAN, R ;
TOTROV, M .
JOURNAL OF MOLECULAR BIOLOGY, 1994, 235 (03) :983-1002
[3]   ICM - A NEW METHOD FOR PROTEIN MODELING AND DESIGN - APPLICATIONS TO DOCKING AND STRUCTURE PREDICTION FROM THE DISTORTED NATIVE CONFORMATION [J].
ABAGYAN, R ;
TOTROV, M ;
KUZNETSOV, D .
JOURNAL OF COMPUTATIONAL CHEMISTRY, 1994, 15 (05) :488-506
[4]   Automation of X-ray crystallography [J].
Abola, E ;
Kuhn, P ;
Earnest, T ;
Stevens, RC .
NATURE STRUCTURAL BIOLOGY, 2000, 7 (Suppl 11) :973-977
[5]   THE PROTEIN-FOLDING PROBLEM - FINDING A FEW MINIMUMS IN A NEAR INFINITE SPACE [J].
ARGOS, P ;
ABAGYAN, R .
COMPUTERS & CHEMISTRY, 1994, 18 (03) :225-231
[6]   Rational design of selective submicromolar inhibitors of Tritrichomonas foetus hypoxanthine-guanine-xanthine phosphoribosyltransferase [J].
Aronov, AM ;
Munagala, NR ;
de Montellano, PRO ;
Kuntz, ID ;
Wang, CC .
BIOCHEMISTRY, 2000, 39 (16) :4684-4691
[7]   Protein-based virtual screening of chemical databases. 1. Evaluation of different docking/scoring combinations [J].
Bissantz, C ;
Folkers, G ;
Rognan, D .
JOURNAL OF MEDICINAL CHEMISTRY, 2000, 43 (25) :4759-4767
[8]   Novel inhibitors of DNA gyrase: 3D structure based biased needle screening, hit validation by biophysical methods, and 3D guided optimization. A promising alternative to random screening [J].
Boehm, HJ ;
Boehringer, M ;
Bur, D ;
Gmuender, H ;
Huber, W ;
Klaus, W ;
Kostrewa, D ;
Kuehne, H ;
Luebbers, T ;
Meunier-Keller, N .
JOURNAL OF MEDICINAL CHEMISTRY, 2000, 43 (14) :2664-2674
[9]   Combinatorial docking and combinatorial chemistry:: Design of potent non-peptide thrombin inhibitors [J].
Böhm, HJ ;
Banner, DW ;
Weber, L .
JOURNAL OF COMPUTER-AIDED MOLECULAR DESIGN, 1999, 13 (01) :51-56
[10]   LUDI - RULE-BASED AUTOMATIC DESIGN OF NEW SUBSTITUENTS FOR ENZYME-INHIBITOR LEADS [J].
BOHM, HJ .
JOURNAL OF COMPUTER-AIDED MOLECULAR DESIGN, 1992, 6 (06) :593-606