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Duocarmycin

Duocarmycins are a series of natural products originally isolated from Streptomyces bacteria in 1988. They exhibit an impressively high cytotoxicity and are subsequently developed into anti-tumor agents. Duocarmycin analogues, among which CC-1065 and duocarmycin SA are the most widely used, represent a series of extremely powerful.

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Duocarmycin

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  1. Duocarmycin https://www.creative-biolabs.com/adc

  2. Duocarmycin ADC Duocarmycin mode of action (MOA) 01 Synthetic Analogs of Duocarmycin 02 Duocarmycins-based ADCs 03

  3. Duocarmycin mode of action (MOA) 01 • Duocarmycins are a series of natural products originally isolated from Streptomyces bacteria in 1988. They exhibit an impressively high cytotoxicity and are subsequently developed into anti-tumor agents.

  4. Two duocarmycin analogs: CC-1065 and duocarmycin SA with highlighted pharmacological active units (Toxins, 2009). Rightmost: a model representing the binding of duocarmycin analogs to DNA minor groove (the payload is shown in red, PNAS, 1996). Both CC-1065 and duocarmycin SA have been shown to be active against various tumor types in vivo and a broad spectrum of human tumor cell lines in vitro.

  5. Duocarmycin analogues, among which CC-1065 and duocarmycin SA are the most widely used, represent a series of extremely powerful antineoplastic compounds that display high cytotoxicity against the growing cancer cells in culture. • Duocarmycin analogues are DNA minor groove binding agents that also exert adenine-N3 alkylation activity and an AT-sequence selectivity. In terms of mode of action, duocarmycin analogues bind the minor groove of DNA and then induce irreversible DNA alkylation that hinders DNA architecture and structural integrity. Duocarmycin mode of action (MOA) 01

  6. Adozelesin, bizelesin and carzelesin are artificially synthesized analogs of duocarmycins and are members of the cyclopropylpyrroloindole family. These drugs have high research and clinical values and all of them have advanced into clinical trials for cancer treatments. Adozelesin is an alkylating small groove DNA binder which quickly restrains DNA replication in treated cells via a trans-acting mechanism. Adozelesin primarily arrests cells in S phase. Synthetic Analogs of Duocarmycin 02

  7. Generation of the active U-76074 from Carzelesin activation (Cancer Res, 1992).

  8. Duocarmycins-based ADCs 03 Duocarmycin analogs are effective in the picomolar range. They are excellent candidates as payloads that yield ADCs with maximized cell-killing potency for regular and more importantly, multi-drug resistant cancer cells.

  9. Duocarmycins by Creative Biolabs With our well-established “DrugLnk” organic synthesis platform, the experienced scientists here at Creative Biolabs is dedicated to help you develop duocarmycin-linker complexes using readily available or customized linkers for antibody conjugation in a timely and cost-effective manner. Our customarily tailored services and high quality products will contribute greatly to the success of your projects.

  10. Contact us 45-1 Ramsey Road, Shirley, NY 11967, USA Tel: 1-631-619-7922 Fax: 1-631-207-8356 Email: marketing@creative-biolabs.com

  11. H N S T A K

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