The Selectivity of Drugs

In: Outline Studies in Biology

Abstract

1 Introduction -- 1.1 What is Selectivity? -- 1.2 The aims and accomplishments of Selectivity -- References -- 2 Three principles that control selectivity -- 3 Steps in the correlation of structure with biological activity -- 3.1 Introduction -- 3.2 The first correlations -- 3.3 The concept of 'receptors' -- 3.4 The receptor as an enzyme or permease -- 3.5 The receptor as a nucleic acid -- 3.6 The receptor as a coenzyme, or other small molecule -- 3.7 Other aspects of receptors -- 3.8 Targets that are not necessarily receptors -- 3.9 Regression analysis -- 3.10 Conclusion -- References -- 4 Favourable differences in distribution: the first principle of selectivity -- 4.1 Some examples -- 4.2 Qualitative aspects of distribution -- 4.3 Quantitative aspects of distribution -- 4.4 The permeability of natural membranes -- 4.5 Metabolic change leading to activation -- 4.6 Metabolic change leading to inactivation -- 4.7 Synergism and antagonism -- 4.8 Conclusion -- References -- 5 Favourable differences in biochemistry: the second principle of selectivity -- 5.1 Introduction -- 5.2 Analogous enzymes -- 5.3 More analogous enzymes: the dihydrofolate reductases -- 5.4 Absence of enzymes from one of the species I. The sulphonamides and organophosphates -- 5.5 Absence of enzymes. II Further examples -- 5.6 Metabolite analogues (mostly antagonists) -- 5.7 Other utilizable biochemical differences -- 5.8 Conclusion -- References -- 6 Favourable differences in cell structure: the third principle of selectivity -- References -- 7 Acquired resistance to drugs: the loss of selectivity.