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1 © 2. DRUG TARGETS Between species Antibacterial and antiviral agentsAntibacterial and antiviral agents Identify targets which are unique to the invading.

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Presentation on theme: "1 © 2. DRUG TARGETS Between species Antibacterial and antiviral agentsAntibacterial and antiviral agents Identify targets which are unique to the invading."— Presentation transcript:

1 1 © 2. DRUG TARGETS Between species Antibacterial and antiviral agentsAntibacterial and antiviral agents Identify targets which are unique to the invading pathogenIdentify targets which are unique to the invading pathogen Identify targets which are shared but which are significantly different in structureIdentify targets which are shared but which are significantly different in structure Within the body Selectivity between different enzymes, receptors etc.Selectivity between different enzymes, receptors etc. Selectivity between receptor types and subtypesSelectivity between receptor types and subtypes Selectivity between isozymesSelectivity between isozymes Organ selectivityOrgan selectivity TARGET SELECTIVITY

2 1 © Not easy to isolate membrane bound receptorsNot easy to isolate membrane bound receptors Carried out on whole cells, tissue cultures, or isolated organsCarried out on whole cells, tissue cultures, or isolated organs Affinity - strength with which compounds bind to a receptorAffinity - strength with which compounds bind to a receptor Efficacy - measure of maximum biochemical effect resulting from binding of a compound to a receptor.Efficacy - measure of maximum biochemical effect resulting from binding of a compound to a receptor. Potency - concentration of an agonist required to produce 50% of the maximum possible effect.Potency - concentration of an agonist required to produce 50% of the maximum possible effect. 3.2.2 Testing with Receptors

3 1 © 4.3 Lead Compounds from the Natural World PLANT EXTRACTS OPIUM - MorphineOPIUM - Morphine CINCHONA BARK - QuinineCINCHONA BARK - Quinine YEW TREE - TaxolYEW TREE - Taxol

4 1 © 4.3 Lead Compounds from the Natural World PLANT EXTRACTS WILLOW TREE - SALICYLIC ACID COCA BUSH - COCAINE Aspirin Procaine

5 1 © 4.3 Lead Compounds from the Natural World VENOMS AND TOXINS Captopril(anti-hypertensive) Teprotide

6 1 © 4.3 Lead Compounds from the Natural World ENDOGENOUS COMPOUNDS NATURAL LIGANDS FOR RECEPTORS Agonist Agonist

7 1 © 4.3 Lead Compounds from the Natural World ENDOGENOUS COMPOUNDS NATURAL LIGANDS FOR RECEPTORS Antagonist Antagonist

8 1 © PRONTOSIL 4.4 Lead Compounds from the Synthetic World

9 1 © SULFANILAMIDE

10 1 © TNT 4.4 Lead Compounds from the Synthetic World

11 1 © RUBBER INDUSTRY ANTABUSE 4.4 Lead Compounds from the Synthetic World

12 1 © AUTOMATED SYNTHETIC MACHINES COMBINATORIAL SYNTHESIS

13 1 © RESIN BEAD AMINO ACID AMINO ACIDS X PEPTIDE 4.4 Lead Compounds from the Synthetic World COMBINATORIAL SYNTHESIS - PEPTIDE SYNTHESIS

14 1 © N N YO CHR 1 R 2 RESIN BEAD 4.4 Lead Compounds from the Synthetic World COMBINATORIAL SYNTHESIS - HETEROCYCLIC SYNTHESIS

15 1 © RESIN BEADN N O R2R2 R3R3 H 4.4 Lead Compounds from the Synthetic World COMBINATORIAL SYNTHESIS - HETEROCYCLIC SYNTHESIS

16 1 © N N O O EtO O R2R2 R3R3 R4R4 R5R5 RESIN BEAD 4.4 Lead Compounds from the Synthetic World COMBINATORIAL SYNTHESIS - HETEROCYCLIC SYNTHESIS

17 1 © N N N NHNNHN O R2R2 R3R3 R4R4 R5R5 RESIN BEAD 4.4 Lead Compounds from the Synthetic World COMBINATORIAL SYNTHESIS - HETEROCYCLIC SYNTHESIS

18 1 © N N YN O R2R2 R3R3 R4R4 R5R5 HNHNHNHN RESIN BEAD 4.4 Lead Compounds from the Synthetic World COMBINATORIAL SYNTHESIS - HETEROCYCLIC SYNTHESIS

19 1 © The Past Lead Compound TargetsTargets Lead compounds The Future 4.5 Lead Compounds - Impact of the human genome project

20 1 © 4.6 Lead Compounds - de novo design

21 1 © X-RAY CRYSTALLOGRAPHY

22 1 © 4.6 Lead Compounds - de novo design PROTEIN STRUCTURE

23 1 © Receptor 4.6 Lead Compounds - de novo design

24 1 © Scaffold CO 2 - HO IONICBOND H- BON D VDWBOND Scaffold H3NH3N + O CH 3

25 1 © N HN O S O ONHN N N H2NH2NH2NH2N S O OON THYMIDYLATE KINASE INHIBITOR ANTICANCER AGENT LEAD COMPOUND Optimisation 4.6 Lead Compounds - de novo design

26 1 © 4.7 Design of Lead Compounds using NMR Spectroscopy NMR SPECTROSCOPY

27 1 © Binding Site Protein 4.7 Design of Lead Compounds using NMR Spectroscopy

28 1 © Protein NO OBSERVABLE BIOLOGICAL EFFECT 4.7 Design of Lead Compounds using NMR Spectroscopy

29 1 © 13 C NMR C C CH CH CH CH 2 CH 3 4.7 Design of Lead Compounds using NMR Spectroscopy

30 1 © CH 2 CH 3 4.7 Design of Lead Compounds using NMR Spectroscopy 13 C NMR C C CH CH CH CH 2 CH 3

31 1 © Protein 4.7 Design of Lead Compounds using NMR Spectroscopy Optimiseepitope

32 1 © Protein 4.7 Design of Lead Compounds using NMR Spectroscopy OptimiseepitopeOptimiseepitope

33 1 © Protein 4.7 Design of Lead Compounds using NMR Spectroscopy OptimiseepitopeOptimiseepitope Link

34 1 © LEAD COMPOUND 4.7 Design of Lead Compounds using NMR Spectroscopy

35 1 © Me Design of a lead compound as an immunosuppressant 4.7 Design of Lead Compounds using NMR Spectroscopy Epitope A Epitope B

36 1 © Me Design of a lead compound as an immunosuppressant 4.7 Design of Lead Compounds using NMR Spectroscopy Lead compound

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