Antibody-drug Conjugates (ADC)

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  1. Monomethyl auristatin E (MMAE) is an antimitotic agent which inhibits cell division by blocking the polymerisation of tubulin, and also shows inhibition of antibody-drug conjugates (ADCs) activity.
  2. Fmoc-Val-Cit-PAB is a cleavable linker for antibody-drug-conjugation (ADC).
  3. 2-Aminoethyl-mono-amide-DOTA-tris(tBu ester) is a macrocycle DOTA derivative for tumor pretargeting.
  4. antibody-drug conjugate Linker

    Ozogamicin is an antibody-drug conjugate Linker.
  5. PAC, consists the ADCs linker and PROTACs, conjugated to an antibody. PAC extracts from patent WO2017201449A1, compound LP2. PAC conjugated to an antibody is a more marked estrogen receptor-alpha (ERα) degrader compared to PROTAC (without Ab).
  6. cleavable ADC linker

    Mc-Val-Cit-PAB-Cl is a cleavable ADC linker. Mc-Val-Cit-PAB-Cl can be used to conjugate MMAE and antibody to form antibody-MC-vc-MMAE .
  7. Daunorubicinol is a drug-linker conjugate for ADC with potent antitumor activity by using Aur0101 (DNA Topoisomerase II inhibitor), linked via the ADC linker.
  8. Vc-seco-DUBA is a drug-linker conjugate for ADC with potent antitumor activity by using DUBA (DNA alkylating agent), linked via the ADC linker Vc-seco.
  9. MC-VC-PABC-Aur0101 is a drug-linker conjugate for ADC with potent antitumor activity by using Aur0101 (an auristatin microtubule inhibitor), linked via the ADC linker MC-VC-PABC.
  10. Fmoc-Val-Cit-PAB-PNP is a cleavable peptide linker, is a linker for antibody-drug-conjugation (ADC).
  11. Monomethyl auristatin F (MMAF) is a synthetic antineoplastic agent. It is part of some experimental anti-cancer antibody-drug conjugates such as vorsetuzumab mafodotin and SGN-CD19A.
  12. alpha-Amanitin is the principal toxin of several deadly poisonous mushrooms, exerting its toxic function by inhibiting RNA-polymerase II.
  13. VcMMAE is an antibody-drug conjugate (ADC) with potent antitumor activity by using the anti-mitotic agent, monomethyl auristatin E (MMAE), linked via the lysosomally cleavable dipeptide, valine-citrulline (vc).
  14. Biotin PEG Linker

    Biotin-PEG3-amineis PEG derivative containing a biotin group and a terminal primary amine group.
  15. PSMA-617, also know as vipivotide tetraxetan. It is a ligand used to make 177Lu-PSMA-617, which is a radioactive molecule to fight cancer.
  16. cleavable ADC linker

    CL2 Linker is a cleavableADC linker. CL2-SN-38 and CL2A-SN-38 are equivalent in drug substitution (~6), cell binding (Kd ~1.2 nM), cytotoxicity (IC50 ~2.2 nM), and serum stability in vitro (t1/2 ~20 hours).
  17. DNA Topoisomerase I inhibitor

    CL2A-SN-38 is a drug-linker conjugate composed of a potent a DNA Topoisomerase I inhibitor SN-38 and a linker CL2A to make antibody drug conjugate (ADC). CL2A-SN-38 provides significant and specific antitumor effects against a range of human solid tumor types.
  18. L2A is a claevable complicated PEG8- and triazole-containing PABC-peptide-mc linker. CL2A is cleavable through pH sensitivity, giving rise to bystander effect, and binds the antibody at a cysteine residue via a disulfide bond. Labetuzumab govitecan used this linker.
  19. cleavable linker

    EC089 is a cleavable linker used in conjugates of tubulysins and folates, and extracted from patent WO2011069116A1.
  20. EC1167 is the linker for EC1169. EC1169 is prostate-specific membrane antigen targeting-tubulysin conjugate. EC1169 has the potential to treat recurrent metastatic, castration-resistant prostate cancer (MCRPC).
  21. 6-O-2-Propyn-1-yl-D-galactose is a nonclaevable glycolinker for the functionalization of cytotoxic drugs and applications in antibody-drug conjugation.
  22. Fmoc-PEA (Example 1-2) is a used as a cleavable linker for antibody-drug conjugates (ADC).
  23. SPP
    SPP is a cleavable disulfide linker, can be used to form cytotoxic compound- linker conjugate.
  24. heterobifunctional crosslinker

    AMAS is a nonclaevable heterobifunctional crosslinker with NHS ester and maleimide groups that allows covalent conjugation of amine- and sulfhydryl-containing molecules.
  25. Duocarmycin is based on its characteristic curved indole structure and a spirocyclopropylcyclohexadienone electrophile to act anticancer activity. Duocarmycin is a DNA minor groove binding alkylating agent and explored as drug?Cantibody conjugates (ADCs) .
  26. MC-Val-Cit-PAB-tubulysin5a is a drug-linker conjugate for ADC with potent antitumor activity by using tubulysin5a (a tubulin inhibitor), linked via the ADC linker MC-Val-Cit-PAB.
  27. MC-Val-Cit-PAB-rifabutin is a drug-linker conjugate for ADC with potent antitumor activity by using rifabutin (an DNA-dependent RNA polymerase inhibitor), linked via the ADC linker MC-Val-Cit-PAB.
  28. MC-Val-Cit-PAB-Indibulin is a drug-linker conjugate for ADC with potent antitumor activity by using Indibulin (an orally applicable inhibitor of tubulin assembly), linked via the ADC linker MC-Val-Cit-PAB.
  29. protein synthesis inhibitor

    MC-Val-Cit-PAB-clindamycin is a drug-linker conjugate for ADC with potent antitumor activity by using clindamycin (a protein synthesis inhibitor), linked via the ADC linker MC-Val-Cit-PAB.
  30. MC-Val-Cit-PAB-Retapamulin is a drug-linker conjugate for ADC with potent antitumor activity by using Retapamulin (a ribosome inhibitor), linked via the ADC linker MC-Val-Cit-PAB.
  31. MC-Val-Cit-PAB-dimethylDNA31 is a drug-linker conjugate for ADC with potent antitumor activity by using dimethylDNA31, linked via the ADC linker MC-Val-Cit-PAB.
  32. MC-Val-Cit-PAB-duocarmycin is a drug-linker conjugate for ADC with potent antitumor activity by using duocarmycin (a DNA minor groove binding alkylating agent), linked via the ADC linker MC-Val-Cit-PAB.
  33. MC-Val-Cit-PAB-carfilzomib is a drug-linker conjugate for ADC with potent antitumor activity by using carfilzomib (an irreversible proteasome inhibitor), linked via the ADC linker MC-Val-Cit-PAB.
  34. ADC peptide linker

    Mc-Val-Cit-PABC-PNP is a cathepsin cleavable ADC peptide linker.
  35. Dxd

    DNA topoisomerase I inhibitor

    Dxd (Exatecan derivative for ADC) is a potent DNA topoisomerase I inhibitor, with an IC50 of 0.31 μM, used as a conjugated drug of HER2-targeting ADC (DS-8201a).
  36. Deruxtecan is an ADC drug-linker conjugate composed of a derivative of DX-8951 (DXd) and a maleimide-GGFG peptide linker, used for synthesizing DS-8201 and U3-1402.
  37. ADC linker

    Val-cit-PAB-OH is a cleavable ADC linker.
  38. ADCs cytotoxin

    PNU-159682, a highly potent metabolite of the anthracycline nemorubicin (DNA topoisomerase II inhibitor) with outstanding cytotoxicity, is a potent ADCs cytotoxin.
  39. FBN33428, also known as Fmoc-Phe-?Lys(Boc)-PAB; is a Hydrolyzable linker for making ADC conjugate

  40. Val-Lys(Boc)-PAB is a ADC linker.
  41. MC-Gly-Gly-Phe is a cleavable linker used for antibody-drug conjugates (ADC).
  42. Boc-Gly-Gly-Phe-Gly-OH is a protease cleavable linker used for the antibody-drug conjugate (ADC).
  43. Boc-Dap-NE is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
  44. nonclaevable ADC linker

    Succinic anhydride is a cyclic anhydride and a nonclaevable ADC linker extracted from patent WO2009064913A1. Succinic anhydride can react with compound 4 of the patent to link the prodrug to an amine or hydroxy 1 group of a targeting polypeptide.
  45. antitubulin agent

    MMAF-Ome, an antitubulin agent, belongs to ADC.
  46. nonclaevable ADC linker

    Mal-amido-PEG8-C2-acid (example 142) is a nonclaevable ADC linker, extracted from patent US2018339985.
  47. sulfo-SPDB-DM4 is a drug-linker conjugate for ADC by using the maytansinebased payload (DM4, an antitubulin agent) via the sulfo-SPDB linker.
  48. MC-Val-Cit-PAB is a cathepsin cleavable ADC linker that is used for making antibody-drug conjugate. FDA approved drugs such as brentuximab vedotin use this linker.
  49. short-chain crosslinker

    SPDP (SPDP Crosslinker) is a short-chain crosslinker for amine-to-sulfhydryl conjugation via NHS-ester and pyridyldithiol reactive groups that form cleavable (reducible) disulfide bonds with cysteine sulfhydryls. It is a glutathione cleavable ADC linker used for the antibody-drug conjugates (ADCs).
  50. 10-Deacetyl-7-xylosyl paclitaxel is a Paclitaxel (a microtubule stabilizing agent; enhances tubulin polymerization) derivative with improved pharmacological features.

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