Drugs target

A more recent and related question to the specificity of chelating agents is that of metalloprotein targets. It is not surprising that many metalloproteins and metal- 

This chapter discusses four important considerations in drug discovery definition of drug targets, generating diversity, definition of lead structures, and qualifying leads for transition to early trials. Many of the examples will be drawn from the realm of cancer chemotherapy, but the principles should be broadly applicable to a wide variety of disease types. 

Copyright 2007 by Academic Press. Ail rights of reproduction in any form reserved. 

FIGURE 28.1 The screening funnel. Loss of compounds is to be expected as candidates proceed through the preclinical process. 

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Table 10.4-1, Drug targets and mechanisins of drug action.

Figure 10.4-1. Biochemical classes of the drug targets in current therapies.

C. R. Gardner and J. Alexander, in Drug Targeting, Elsevier Science PubHshers B.V. (Biomedical Division), New York, 1985, p. 145. 

Neubig, R. R., and Siderovski, D. P. (2002). Regulators of G-protein signaling as new central nervous system drug targets. Nature Rev. Drug Disc. 1 187—196. 

Yart A, Mayeux P, Raynal P (2003) Gabl, SHP-2 and Other Novel Regulators of Ras Targets for Anticancer Drug Discovery. Curr Cancer Drug Targets 3 177-192... 

Little attempt has been made to develop drugs targeted specifically to white adipose tissue and the production of adipokines. It is likely, however, that there will be an increasing emphasis on this approach to the pharmacological treatment of obesity-related diseases, given the current views on the centrality of the adipokines to these disorders. It is, of course, the diseases that obesity leads to, rather than obesity itself, that constitute the main medical challenge. 

Hardie DG (2007) AMP-Activated Protein Kinase as a Drug Target. Annu Rev Pharmacol Toxicol 47 185-210... 

Drugs Targets Mechanisms Functional Side effects... 

The preferred substrates of acetyltransferases are amino-groups of antibiotics, like chloramphenicol, strepto-gramin derivatives, and the various aminoglycosides. The modification is believed to block a functional group involved in the drug-target-interaction. All acetyltransferases use acetyl-coenzyme A as cofactor. 

Antiepileptic Drugs. Figure 2 Antifungal drugs - targets of antifungal activity. 

Leptin has proved to be an efficient treatment for the rare form of obesity associated with leptin deficiency. By contrast, the results of the fust clinical trial with human leptin in obese patients (without leptin deficiency) were less promising. This may be explained by leptin resistance in a high proportion of these patients. However, the mechanisms involved in the development of leptin resistance could become new drug targets. 

Proteins of this family are closely associated with human diseases. They have also been proven to be valuable in diagnosis and are considered to have potential as drug targets to improve therapies. 

Blagden S, de Bono J (2005) Drugging cell cycle kinases in cancer therapy. Curr Drug Targets 6 325-335... 

Any protein whose function is believed to be clinically relevant and suitable for modulation by a drug can be considered a drug target. Targets may be grouped... 

Overington JP, Al-Lazikani B, Hopkins AL (2006) How many drug targets are there Nat Rev 5 993-996... 

Ferguson, MAJ (2000) Glycosylphosphatidylinositol biosynthesis validated as a drug target for African sleeping sickness. Proc Natl Acad Sci USA 97 10673-10675... 

Currently no drugs directly modulating the LDL receptor family are known. The possible use of drugs targeting the LDL receptor family or downstream signaling proteins may be derived from Table 1. 

Smith CA, Baker EN (2002) Aminoglycoside antibiotic resistance by enzymatic deactivation. Curr Drug Targets Infect Disord 2 143-160... 

Bespalov MM, Saarma M (2002) GDNF family receptor complexes are emerging drug targets. Trends Pharmacol Sci 28 68-74. 

AA A1 A01.004 Memapsin-2 Potential drug target for Alzheimer s disease... 

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