Drug Class Library
Recommended Article : 【Bioinformatics】 Drug Library
1. Overview
c. Drug Library
1. Overview
⑴ Additional information can be referenced from the curation of billions of papers at https://typeset.io/ and https://www.scinapse.io/.
2. Molecular Function
⑴ Signal transduction enhancers
○ AMPK : A769662
⑵ Signal transduction inhibitors
○ EGFR inhibitor : gefitinib, erlotinib (Tarceva), sapitinib, cetuximab, panitumumab, lapatinib, afatinib, nimotuzumab, 806
○ HER2 (erbB-2) inhibitor : pertuzumab, trastuzumab, margetuximab, lapatinib, afatinib, neratinib, sapitinib, CI-1033
○ HER3 (erbB-3) inhibitor : sapitinib
○ IGF-1R inhibitor : AXL1717, linsitinib
○ Muscarinic receptor inhibitors : atropine, sarin, DIFP, tabun
○ BRAF inhibitor : dabrafenib, vemurafenib (Zelboraf), PLX4720
○ mTORC1 inhibitor : rapamycin (sirolimus)
○ MEK1/2 inhibitor : trametinib (Mekinist), cobimetinib, refametinib
○ ERK1/2 inhibitor : MK-8353, SCH772984
○ AKT1/2 inhibitor : MK-2206
○ MAPK9 inhibitor : AS602801
○ PI3K inhibitor : LY294002, taselisib, alpelisib, MK-2206, 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
○ Phosphorylation signal transduction inhibitor : lapatinib
○ PARP1/2 inhibitor : olaparib
○ PLK4 inhibitor : CFI400945
○ p38 inhibitor : VX-745
○ CHEK1/2 inhibitor : AZD-7762, AZD7762
○ CHEK1-selective inhibitor : SAR-020106, rabusertib
○ CHEK2-selective inhibitor : CCT-241533
○ JNK inhibitor : JNK-IN-8
○ 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
⑶ Metabolic inhibitors
○ GLUT1 inhibitor : bay-876
○ Pfkp inhibitor : PFK15
○ 2-deoxy-D-glucose inhibitor : Gpi1
○ Lipofermata inhibitor : FATP2
○ Atglistatin inhibitor : ATGL
⑷ Mitochondrial Electron Transport Inhibitors
○ Rotenone
○ Barbituric acid
○ Piericidin
○ Malonic acid
○ Antimycin
○ KCN
○ CO
○ Oligomycin
○ DNP
○ Valinomycin
○ Thermogenin
○ 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
○ 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
○ 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