Antibody-drug conjugates (ADCs) are next-generation targeted anti-tumor agents that are constructed by the covalent coupling of a monoclonal antibody with a cytotoxic payload drug via a small molecular linker. As a key factor in an ADC, the payload drug dictates its efficacy.
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ADC Payloads https://www.creative-biolabs.com/adc
ADC Payloads • Antibody-drug conjugates (ADCs) are next-generation targeted anti-tumor agents that are constructed by the covalent coupling of a monoclonal antibody with a cytotoxic payload drug via a small molecular linker. As a key factor in an ADC, the payload drug dictates its efficacy. At this moment, a large variety of payload drugs have been exploited in ADC and the number is on the rise. T
To facilitate the unique needs for different ADC development projects, Creative Biolabs has established an advanced “DrugLnk” organic synthesis platform with a large collection of payload drugs and linkers in the “drug module” and the “linker module”, respectively. Our scientists are highly experienced in full chemical synthesis, chemical modification, as well as bio-conjugation. We are dedicated to help our clients prepare innovated payload-linker complexes for novel ADC developments.
01 Microtubule Toxins ADC Payloads 02 DNA Toxins 03 Transcription Toxins 04 Inhibitors 05 Other Payloads
01 Microtubule Toxins • Microtubule toxins are a successful group of anticancer drugs that inhibit tumor cell growth and promote apoptosis by disrupting the assembly and dynamics of microtubules. They are generally applied in combination with other treatments against malignancies. • In the form of an ADC, serious adverse effects of these microtubule toxins are greatly reduced, allowing the usage of these extremely potent agents for therapeutic applications.
02 DNA Toxins • DNA toxins induce DNA damage and subsequently cell death by various mechanisms, such as double stranded DNA cleavage, DNA cross-linking… They are highly toxic agents with in vitro potency down to the picomolar level against tumor cell lines. • With optimized linkers and conjugation strategies, DNA toxins are incorporated into ADCs for accurate drug delivery and an expanded therapeutic window.
03 Transcription Toxins • Toxins targeting the DNA transcription machineries have been demonstrated as good candidates for ADC development. • Currently, toxins against RNA polymerase II (the initial step in DNA transcription) and spliceosome (for correct mRNA maturation and processing) are being actively exploited.
04 Inhibitors • Various small molecule inhibitors, bearing unique chemical and cytotoxicity profiles, have also been exploited as ADC payloads. • The process inhibited include oxidative phosphorylation (oligomycins), ATP biosynthesis (ipatasertib), and other important enzymes such as dihydrofolate reductase (DHFR, methotrexate) …
05 Other Payloads • With the development of fusion protein expression technology and nanoscience, the warfare against cancer has expended exponentially and many novel payloads based on these technological platforms, such as Nano-carriers, protein toxins, and toxic proteins for antibody-directed enzyme prodrug therapy (ADEPT), have also been exploited for ADC development.
With our well-established “DrugLnk” organic synthesis platform, the experienced scientists here at Creative Biolabs is dedicated to help you prepare various customized payload-linker complexes using toxins in the Drug Module for ADC development in a timely and cost-effective manner.
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