Strategies and recent technologies in drug discovery. 1995

H Kubinyi
Drug Design, BASF, Ludwigshafen.

In the last years, the paradigms of drug research changed significantly. New technologies were developed, in several different fields. Combinatorial chemistry and high-throughput screening increase our chances to find new lead structures, with less effort than by dedicated syntheses. Gene technology, in addition to providing therapeutically useful proteins, significantly contributes to rational drug design. The primary structure of a protein can be derived from the DNA sequence of the corresponding gene. Its relevance for a certain disease is investigated in transgenic animals. Expression of the protein in bacteria or in cell culture produces material for screening systems and for 3D structure determination by protein crystallography. NMR techniques, or electron cryo-microscopy. Structure-based and computer-aided design methods are applied to optimize lead structures with the least effort. A serious problem in the application of such techniques is their limitation to ligand-protein interactions. For the design of a therapeutically useful drug, also absorption, distribution, metabolism and elimination have to be considered. QSAR methods help in this respect. Scope and limitations of the new technologies are discussed in the context of conventional approaches in drug discovery.

UI MeSH Term Description Entries
D010600 Pharmacology The study of the origin, nature, properties, and actions of drugs and their effects on living organisms. Pharmacologies
D012107 Research Design A plan for collecting and utilizing data so that desired information can be obtained with sufficient precision or so that an hypothesis can be tested properly. Experimental Design,Data Adjustment,Data Reporting,Design, Experimental,Designs, Experimental,Error Sources,Experimental Designs,Matched Groups,Methodology, Research,Problem Formulation,Research Methodology,Research Proposal,Research Strategy,Research Technics,Research Techniques,Scoring Methods,Adjustment, Data,Adjustments, Data,Data Adjustments,Design, Research,Designs, Research,Error Source,Formulation, Problem,Formulations, Problem,Group, Matched,Groups, Matched,Matched Group,Method, Scoring,Methods, Scoring,Problem Formulations,Proposal, Research,Proposals, Research,Reporting, Data,Research Designs,Research Proposals,Research Strategies,Research Technic,Research Technique,Scoring Method,Source, Error,Sources, Error,Strategies, Research,Strategy, Research,Technic, Research,Technics, Research,Technique, Research,Techniques, Research
D005818 Genetic Engineering Directed modification of the gene complement of a living organism by such techniques as altering the DNA, substituting genetic material by means of a virus, transplanting whole nuclei, transplanting cell hybrids, etc. Genetic Intervention,Engineering, Genetic,Intervention, Genetic,Genetic Interventions,Interventions, Genetic
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D013678 Technology, Pharmaceutical The application of scientific knowledge or technology to pharmacy and the pharmaceutical industry. It includes methods, techniques, and instrumentation in the manufacture, preparation, compounding, dispensing, packaging, and storing of drugs and other preparations used in diagnostic and determinative procedures, and in the treatment of patients. Technology, Pharmacy,Pharmaceutic Technology,Pharmaceutical Technology,Pharmacy Technology,Technology, Pharmaceutic

Related Publications

Copied contents to your clipboard!