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Pharmacology I

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An introduction to general pharmacology


The biological substance (usually a protein molecule/DNA/RNA/ribosome), drugs act by binding and altering it's physiological role, is called the target molecule. Till now, 435 proteins a re identified as drug target and 989 drugs act by affecting these targets. There are other 609 non therapeutic targets and 103 drugs, act on unknown target, used as therapeutic agents [Mathias RA et. al., 2011].

Potential drug targets

Fig.1. Representation of percentage of potential drug targets [Mathias RA et. al., 2011]

Examples of drug target

1. Enzyme as drug target: Cyclooxygenase 2 is targeted for the management of inflammatory disorders (like fever, pain, migraine, inflammatory bowl diseases etc.) [Imming P et. al., 2007].

2. Receptors as drug target: $\gamma$-amino butyric acid (GABAA) is the target for benzodiazepins as sedative, hypnotics, anti-epileptics, muscle relaxants etc [Imming P et. al., 2007].

3. Ion channels as drug target: Carbamazepine acts as anti epileptic drug by inhibiting Sodium channel [Imming P et. al., 2007].

4. Transporter protein as drug target: Omeprazole acts by inhibiting Na+H+ATPase antitransport protein [Imming P et. al., 2007].

5. Deoxyribonuclic acid (DNA) as drug target: Bleomycin is used to treat Hodgkin's disease, which causes the oxidative degradation of DNA [Imming P et. al., 2007].

6. Ribonuclic acid (RNA) as drug target: Aminoglycosides are used as bacteriocidal agents, which act by inhibiting protein synthesis [Imming P et. al., 2007].

7. Ribosomes as drug target: Tetracyclines (antibacterial) act by inhibiting the 30S unit of ribosome [Imming P et. al., 2007].

8. Targets of monoclonal antibodies: Adalimumab and infliximab are used as anti-rheumatic agents, act by inhibiting tumour necrosis factor-$\alpha$ [Imming P et. al., 2007].

9. Structural proteins as drug target: Tubulin (helps in cell division, mitosis) is the target for colchicines, vinca alkaloids and paclitaxel as anti-cancer agent [Imming P et. al., 2007].

10. Regulators as drug targets: Losartan acts as anti-hypertensive agent by inhibiting angiotensin II receptor [Rang MP et. al., 2007].

11. Hormones as drug target: Thyroid hormone synthesis inhibitors (methimazole, carbimazole) are used to treat thyrotoxicosis, toxic nodular goiter and Grave's diseases [Tripathi KD, 2004].

12. Signaling proteins as drug target: Regulator of G protein signaling (RGS) proteins interact with G$\alpha$ protein to turn off the excessive action of G-protein coupled receptors (GPCR) [Luc DV et. al., 2000].

Chemotherapeutic agents

This type of chemical acts on the causative agents of the disease (eg. virus, bacteria, protozoa etc.) either by inhibiting their multiplication (static effect) or by killing the organisms (cidal action) in stead of affecting the host cells. Example: Isoniazid acts as anti-tubercular agent by inhibiting the of mycolic acid synthesis of mycobacterium tuberculosis (bacteriocidal) .


[Mathias RA et. al., 2011] Mathias RA, Markus SA, Helgi BS, Trends in the exploitation of novel drug targets, Nature review, Vol. 10, 579-590, 2011.
[Imming P et. al., 2007] Imming P, Sinning C, Meyer A, Drugs, their targets and the nature and number of drug targets, Nature publishing groups, vol. 5, 821-835, 2007.
[Rang MP et. al., 2007] Rang HP, Dale MM, Ritter J M, Moore P K, Pharmacology, 5th Edition, Elsevier, 2-752, 2007.
[Luc DV et. al., 2000] Luc DV, Bin Z, Thierry F, Eric Elenko, Marilyn GF, The Regulator of G Protein Signaling Family, Pharmacology and Toxicology, Vol. 40, 235-271, 2000.
[Tripathi KD, 2004] Tripathi KD, Essential of Medical Pharmacology, 5th Edition, Jaypee Brothers Medical Publishers Limited, 3-123, 2004.

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