○ PI3K inhibitor: LY294002, wortmannin, taselisib, alpelisib, idelalisib (CAL-101), dactolisib (BEZ-235), everolimus, pictilisib (GDC-0941), apitolisib (GDC-0980)

○ IκB inhibitor: Bortezomib

○ sPLA2-IIa inhibitor: cFLSYR, c(2NapA)LS(2NapA)R

○ AMPK inhibitor: dorsomorphin, A769662

○ Phosphorylation signal transduction inhibitor: lapatinib

○ PARP1/2 inhibitor: olaparib

○ PLK4 inhibitor: CFI400945

○ p38 inhibitor: VX-745

○ CHEK1/2 inhibitor: AZD-7762

○ CHEK1-selective inhibitor: SAR-020106, rabusertib

○ CHEK2-selective inhibitor: CCT-241533

○ JNK inhibitor: JNK-IN-8, SP600125

○ ATM inhibitor: AZD-1390

○ CCL7 inhibitor: Bindarit

○ MST1R inhibitor: MK-8033

○ TGFβR inhibitor: RepSox

○ DDR1 inhibitor: 7rh

○ Rock1 inhibitor: Y-27632

○ CCR4 inhibitor: C021

○ Hif-1a inhibitor: KC7F2

○ WEE1, PLK1 inhibitor: MK-1775

○ BCL2, BCL-XL, BCL-W inhibitor: navitoclax

○ ATPase inhibitor: NaN3

○ anti-VEGF: ranibizumab, aflibercept, bevacizumab

○ VEGFR tyrosine kinase inhibitor: sunitinib, pazopanib, axitinib, IM2C6, CDP791

○ Tyrosine phosphorylation enzyme inhibitors: imatinib (Glivec), dasatinib (Sprycel), sunitinib (Sutent), nilotinib (Tasigna), sorafenib (Nexavr), temsirolimus (Torisel)

3. Cellular Component

⑴ Endocytosis inhibitors

○ Macropinocytosis inhibitor: EPIA (5-(N-ethyl-N-isopropyl)amiloride)

○ Mannose receptor-mediated endocytosis inhibitor: mannan

○ Clathrin-mediated endocytosis inhibitor: dynasore (dynamin inhibitor), chlorpromazine

○ Caveolar-mediated endocytosis inhibitor: dynasore (dynamin inhibitor), nystatin

○ Endosomal escape inhibitors

○ Nocodazole: Disrupts microtubules to alter endosomal progression

○ Bafilomycin

○ Macrolide antibiotics. Inhibitors of V-type H+ pumps

○ Inhibits endosomal acidification → inhibits transformation of early endosomes to late endosomes and lysosomes

⑵ Macropinocytosis enhancers

○ Small molecule with membrane-destabilizing property: chloroquine, siramesine, amitriptyline

○ Endosomal escape activator

○ 𝛽-sitosterol: a cholesterol analogue

⑶ Metabolic inhibitors

○ GLUT1 inhibitor: bay-876

○ Pfkp inhibitor: PFK15

○ 2-deoxy-D-glucose inhibitor: Gpi1

○ FATP2 inhibitor: lipofermata

○ ATGL inhibitor: atglistatin

⑷ Mitochondrial Electron Transport Inhibitors

○ Rotenone

○ Barbituric acid

○ Piericidin

○ Malonic acid

○ Antimycin

○ KCN

○ CO

○ Oligomycin

○ DNP

○ Valinomycin

○ Thermogenin

⑸ Cell Division Inhibitors

○ Epothilones

○ Halichondrin B analogue

○ Taxanes

○ Vinca alkaloid

○ Anthracemedione

○ Anthracycline

○ Epipodophyllotoxin

○ Folate antagonist

○ Purine analogue

○ Pyrimidine analogue

○ Hydroxyurea

○ Methotrexate

○ Anthracemedione

○ Anthracycline

○ Epipodophyllotoxin

○ Bleomycin

○ Dactinomycin

○ Mitomycin

○ Alkyl sulfonate

○ Ethylenimine

○ Nitrogen mustard

○ Nitrosurea

○ Platinum analogue

○ Triazene

⑹ Central Dogma-related Inhibitors

○ Acyclovir (acycloguanosine): Antiviral agent. Inhibits viral DNA synthesis by reacting with viral thymidine kinase (tk).

○ AraC (cytosine arabinoside, cytarabine): Anticancer agent

○ AraA (adenine arabinoside, vidarabine): Antiviral agent

○ Antinomycin D: Binds to the groove of DNA to prevent replication. Can also affect eukaryotic cells.

○ Fluoroquinolones (ciprofloxacin): Inhibits DNA gyrase

○ Carboplatin: Anticancer agent that inhibits DNA synthesis

○ Irinotecan: TOP1 inhibitor

○ Topotecan: TOP1 inhibitor

○ Camptothecin: TOP1 inhibitor

○ Diflomotecan: TOP1 inhibitor

○ Lamellarin D: TOP1 inhibitor

○ Etoposide: TOP2 inhibitor

○ Teniposide: TOP2 inhibitor

○ Doxorubicin: TOP2 inhibitor

○ Daunorubicin: TOP2 inhibitor

○ Mitoxantrone: TOP2 inhibitor

○ Amsacrine: TOP2 inhibitor

○ Ellipticines: TOP2 inhibitor

○ Aurintricarboxylic acid: TOP2 inhibitor

○ HU-331: TOP2 inhibitor

○ Antinomycin D: Transcription inhibitor

○ Cycloheximide: Translation inhibitor in eukaryotic cells

○ Chloramphenicol: Inhibits translation in bacteria

○ Erythromycin: Inhibits translation in bacteria

○ Neomycin: Inhibits translation in bacteria

○ Streptomycin: Inhibits translation in bacteria

○ Tetracycline: Inhibits translation in bacteria

○ AZT (Zidovudine): Reverse transcriptase inhibitor

○ Combivir (AZT + Epivir): Reverse transcriptase inhibitor

○ Emtriva (emtricitabine): Reverse transcriptase inhibitor

○ Epivir (Lamivudine): Reverse transcriptase inhibitor

○ Epzicom (Abacavir + Epivir): Reverse transcriptase inhibitor

○ Hivid (ddC): Reverse transcriptase inhibitor

○ Trizivir (Abacavir + AZT + Epivir): Reverse transcriptase inhibitor

○ Videx & Videx EC (ddI): Reverse transcriptase inhibitor

○ Zerit (D4T): Reverse transcriptase inhibitor

○ Ziagen (Abacavir): Reverse transcriptase inhibitor

⑺ Cytochrome P450 Inhibitors

○ Cimetidine

○ Ciprofloxacin

○ Disulfiram

○ Erythromycin

○ Fluconazole

○ Fluoxetine

○ Furafylline

○ Isoniazid

○ Ketoconazole

○ Methadone

○ Mibefradil

○ Orphenadrine

○ Paroxetine

○ Quinidine

○ Ritonavir

○ Sulfaphenazole

○ Ticlopidine

○ Tranylcypromine

○ Troglitazone

⑻ Protease

○ Crixsivan: One of the HIV protease inhibitors used for AIDS treatment

○ MG132: Proteasomal inhibitor

4. Biological Process

⑴ Cholinesterase Inhibitors

○ Aricept® (donepezil)

○ Exelon® (rivastigmine)

○ Razadyne® (galantamine)

○ Reminyl® (galantamine)

⑵ Neuronal Activity Inhibitors

○ Tetrodotoxin: Irreversibly blocks voltage-gated sodium channels in excitable cells

○ Tetraethylammonium: Blocks voltage-gated potassium channels

○ Botox : Blocks voltage-gated calcium ion channels in neuromuscular junctions → Impairs acetylcholine release → Muscle paralysis

○ CPZ: Decreases or inhibits neurotransmitter release

⑶ Blood Coagulation Inhibitors

○ Prostacyclin (PGI2)

○ Nitric oxide (NO)

○ Aspirin

○ Heparin

○ Hirudin

○ EDTA

○ Sodium citrate

○ Sodium oxalate

○ Plasmin

○ Fondaparinux

○ Rivaroxaban

○ Apixaban

○ Dabigatran

○ Bivalirudin

○ Argatroban

○ Clopidogrel

○ Prasugrel

○ Ticagrelor

○ Tirofiban

○ HBA(hydroxybenzy alcohol)

⑷ Immunosuppressants

○ Cyclosporin

⑸ Vascular Action Inhibitors

○ Thrombospondin-1: Inhibitor of vascular neogenesis. Binds to CD36.

⑹ Lymphatic marker

○ LYVE1

⑺ Monitoring marker for chronic hepatitis

○ HCV-RNA level

Input: 2021.10.07 11:53

Modified: 2022.09.03 17:39

311

Drug Class Library

1. Overview

2. Molecular Function

3. Cellular Component

4. Biological Process

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