Examples of drug targets identified (by pathophysio or MOA of drugs)

• Zidovudine

• Saquinavir

• Disease: AIDS

• Target identified: reverse transcriptase HIV protease

zafirlukast

• Disease: asthma

• Target identified: cysteinyl leukotriene receptor

Trimethoprim

• Disease: bacterial infections

• Target identified: dihydrofolate reductase

• 6-mercaptopurine

• methotrexate

• Disease: malignant disease

• Target identified: dihydrofolate reductase

Fluoxetine

• Disease: depression

• Target identified: 5HT transporter

• Captopril

• Sildenafil

• Losartan

• Disease: hypertension

• Target identified:

  • Angiotensin-converting enzyme

  • Type 5 phosphodiesterase

  • Angiotensin-2 receptor

• Celecoxib

• Rofecoxib

• Disease: inflammatory disease

• Target identified: COX-2

Donepezil

• Disease: alzheimer’s disease

• Target identified: acetylcholinesterase

• Tamoxifen

• Herceptin

• Disease: breast cancer

• Target identified: oestrogen receptor

Imatinib

• Disease: chronic myeloid leukemia

• Target identified: Abl kinase

• Levodopa

• Selegiline

• Disease: parkinson’s disease

• Target identified:

  • Dopamine synthesis

  • MAO-B

Maclobemide

• Disease: depression

• Target identified: MAO-A

• Benzodiazepine

• Aspirin-like drugs

• Ciclosporin, FK506

• Vinca alkaloids

• Dihydropyridines

• Sulfonylureas

• Classic antipsychotic drugs

• TCA

• Fibrates

Targets identified via drug effects

Benzodiazepines

• Disease: anxiety, sleep disorders

• Target identified: BDZ binding site on GABAa receptor

Aspirin-like drugs

• Disease: inflammation, pain

• Target identified: COX enzymes

Ciclosporon, FK506

• Disease: transplant rejection

• Target identified: immunophilins

Vinca alkaloids

• Disease: cancers

• Target identified: tubulin

dihydropyridines

• Disease: cardiovascular disease

• Target identified: L-type calcium channels

Sulfonylureas

• Disease: diabetes

• Target identified: Katp channels

Classic antipsychotic drugs

• Disease: schizophrenia

• Target identified: dopamine D2 receptor

TCA

• Disease: depression

• Target identified: monoamine transporters

Fibrates

• Disease: raised blood cholesterol

• Target identified: PPARa