受体( Receptors) 类型 药物活性 举例 i-protein-coupled receptors Prostanoid receptors Agonists Misoprostol Purinergic Receptors P2Y12 antagonists Clopidogrel Serotonin receptors 5-HT1A partial agonists Buspirone 5-HT1B/1D agonists Sumatriptan 5-HTA antagonists Quetiapine, Ziprasidone 5-HT3 antagonists Granisetron Integrin receptors Glycoprotein IIb/IIIa Antagonists Tirofiban receptor Receptors associated with a tyrosine kinase Insulin receptor Direct agonists Insulin Sensitizers Biguanides
类型 药物活性 举例 G-protein-coupled receptors Prostanoid receptors Agonists Misoprostol Purinergic Receptors P2Y12 antagonists Clopidogrel Serotonin receptors 5-HT1A partial agonists Buspirone 5-HT1B/1D agonists Sumatriptan 5-HT2A antagonists Quetiapine, Ziprasidone 5-HT3 antagonists Granisetron Integrin receptors Glycoprotein IIb/IIIa receptor Antagonists Tirofiban Receptors associated with a tyrosine kinase Insulin receptor Direct agonists Insulin Sensitizers Biguanides Nature Reviews Drug Discovery, 2006, vol 5, 821 受 体 （Receptors）
受体( Receptors) 类型 药物活性 举例 Nuclear receptors(steroid hormone receptors and others) Mineralocorticoid Agonists Aldosterone receptor Antagonists Spironolactone Glucocorticoid receptor Agonists Glucocorticoids Oestrogen receptor Agonists Oestrogens (Partial) agonists Clomifene Antagonists Fulvestrant Modulators Tamoxifen Peroxisome proliferator PPARa agonists Fibrates activated receptor(PPAR) PPARY agonists Glitazones Thyroid hormone Agonists L-Thyroxine receptors
类型 药物活性 举例 Nuclear receptors (steroid hormone receptors and others) Mineralocorticoid receptor Agonists Aldosterone Antagonists Spironolactone Glucocorticoid receptor Agonists Glucocorticoids Oestrogen receptor Agonists Oestrogens (Partial) agonists Clomifene Antagonists Fulvestrant Modulators Tamoxifen Peroxisome proliferator activated receptor (PPAR) PPARα agonists Fibrates PPARγ agonists Glitazones Thyroid hormone receptors Agonists L-Thyroxine Nature Reviews Drug Discovery, 2006, vol 5, 821 受 体 （Receptors）
靶酶( Enzymes) 类型药物活性 举例 Hydrolases(proteases) Aspartyl proteases(viral) HIv protease inhibitor Saquinavir, indinavir Hydrolases(serine proteases) Bacterial serine protease Direct inhibitor lactams Bacterial lactamases Direct inhibitor Sulbactam Human antithrombin Activator Heparins Human plasminogen Activator Streptokinase Hydrolases(metalloproteases) Human ace Inhibitor Captopril Human hrd Inhibitor Cilastatin (dehydropeptidase) Hydrolases(other) 26S proteasome Inhibitor Bortezomib
靶 酶（Enzymes） 类型 药物活性 举例 Hydrolases (proteases) Aspartyl proteases (viral) HIV protease inhibitor Saquinavir, indinavir Hydrolases (serine proteases) Bacterial serine protease Direct inhibitor β-lactams Bacterial lactamases Direct inhibitor Sulbactam Human antithrombin Activator Heparins Human plasminogen Activator Streptokinase Hydrolases (metalloproteases) Human ACE Inhibitor Captopril Human HRD (dehydropeptidase) Inhibitor Cilastatin Hydrolases (other) 26S proteasome Inhibitor Bortezomib
靶酶( Enzymes) 类型 药物活性 举例 Hydrolases (other) Glycosidases (viral) a-glycosidase inhibitor Zanamivir, oseltamivir Glycosidases(human) a-glycosidase inhibitor Acarbose Esterases AChE inhibitor Physostigmine PDE3 inhibitor Amrinon milrinone PDE5 inhibitor Sildenafil doPa decarboxylase Inhibitor Carbidopa Carbonic anhydrase Inhibitor Acetazolamide Isomerases DNA gyrases(bacterial) Inhibitor Fluoroquinolones
类型 药物活性 举例 Hydrolases (other) Glycosidases (viral) α-glycosidase inhibitor Zanamivir, oseltamivir Glycosidases (human) α-glycosidase inhibitor Acarbose Esterases AChE inhibitor Physostigmine PDE3 inhibitor Amrinon, milrinone PDE5 inhibitor Sildenafil DOPA decarboxylase Inhibitor Carbidopa Carbonic anhydrase Inhibitor Acetazolamide Isomerases DNA gyrases (bacterial) Inhibitor Fluoroquinolones Nature Reviews Drug Discovery, 2006, vol 5, 821 靶 酶（Enzymes）
靶酶( Enzymes) 类型 药物活性 举例 Isomerases Topoisomerases Topoisomerase I inhibitor Camptothecin, Irinotecan Topoisomerase II inhibitor Etoposide △87 Isomerase( funga) Inhibitor Amorolfine Ligases(also known as synthases) ihydropteroate synthase Inhibitor Sulphonamides Thymidylate synthase Inhibitor fluorouracil (fungal and human) Oxidoreductases Monoamine oxidases MAO-A inhibitor Moclobemide (MAOS) MAO-B inhibitor Selegiline Cyclooxygenases(COXs) Inhibitor NSAIDS
类型 药物活性 举例 Isomerases Topoisomerases Topoisomerase I inhibitor Camptothecin, Irinotecan Topoisomerase II inhibitor Etoposide Δ8,7 isomerase (fungal) Inhibitor Amorolfin Ligases (also known as synthases) Dihydropteroate synthase Inhibitor Sulphonamides Thymidylate synthase (fungal and human) Inhibitor Fluorouracil Oxidoreductases Monoamine oxidases (MAOs) MAO-A inhibitor Moclobemide MAO-B inhibitor Selegiline Cyclooxygenases (COXs) Inhibitor NSAIDs Nature Reviews Drug Discovery, 2006, vol 5, 821 靶 酶（Enzymes）