Desirability-Based Multi-Objective QSAR in Drug Discovery

被引:15
作者
Cruz-Monteagudo, Maykel [1 ,2 ,3 ]
Cordeiro, M. Natalia D. S. [4 ]
Tejera, Eduardo [5 ]
Rosa Dominguez, Elena [2 ,3 ,6 ]
Borges, Fernanda [1 ]
机构
[1] Univ Porto, Fac Sci, Dept Chem & Biochem, CIQ, P-4169007 Oporto, Portugal
[2] Cent Univ Las Villas, Fac Chem & Pharm, Appl Chem Res Ctr, Santa Clara 54830, Cuba
[3] Cent Univ Las Villas, Chem Bioact Ctr, Mol Simulat & Drug Design Grp, Santa Clara 54830, Cuba
[4] Univ Porto, Fac Sci, Dept Chem & Biochem, REQUIMTE, P-4169007 Oporto, Portugal
[5] Univ Porto, Fac Pharm, Dept Biochem, P-4150047 Oporto, Portugal
[6] ITT, Metepec 52140, Mexico
关键词
MOOP-DESIRE methodology; desirability theory; multi-objective QSAR; drug discovery; COMPUTATIONAL CHEMISTRY APPROACH; A(3) ADENOSINE RECEPTOR; PARTITIONING PUMP-RP; IN-SILICO; CONFORMATIONAL FLEXIBILITY; SIMULTANEOUS-OPTIMIZATION; LIQUID-CHROMATOGRAPHY; 5-HT2A RECEPTOR; UNIFIED QSAR; GLOBAL QSAR;
D O I
10.2174/138955712802762329
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The adjustment of multiple criteria in hit-to-lead identification and lead optimization is a major advance in drug discovery. Thus, the development of approaches able to handle additional criteria for the early simultaneous treatment of the most important properties determining the pharmaceutical profile of a drug candidate is an emergent issue in this area. In this paper, we review a desirability-based multi-objective QSAR method allowing the joint handling of multiple properties of interest in drug discovery: the MOOP-DESIRE methodology. This methodology adapts desirability theory concepts allowing the holistic modeling of the many and conflicting biological properties determining the therapeutic utility of a drug candidate. Here we survey their suitability for key tasks involving the use of chemoinformatics methods in medicinal chemistry and drug discovery.
引用
收藏
页码:920 / 935
页数:16
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