Albers, Aaron E.; Garofalo, Albert W.; Drake, Penelope M.; Kudirka, Romas; de Hart, Gregory W.; Barfield, Robyn M.; Baker, Jeanne; Banas, Stefanie; Rabuka, David published the artcile< Exploring the effects of linker composition on site-specifically modified antibody-drug conjugates>, Quality Control of 112-63-0, the main research area is immunoconjugate HER2 antibody crosslinker maytansine antitumor; Aldehyde tag; Antibody–drug conjugate; Noncleavable linker.
In the context of antibody-drug conjugates (ADCs), noncleavable linkers provide a means to deliver cytotoxic small mols. to cell targets while reducing systemic toxicity caused by nontargeted release of the free drug. Addnl., noncleavable linkers afford an opportunity to change the chem. properties of the small mol. to improve potency or diminish affinity for multidrug transporters, thereby improving efficacy. We employed the aldehyde tag coupled with the hydrazino-iso-Pictet-Spengler (HIPS) ligation to generate a panel of site-specifically conjugated ADCs that varied only in the noncleavable linker portion. The ADC panel comprised antibodies carrying a maytansine payload ligated through one of five different linkers. Both the linker-maytansine constructs alone and the resulting ADC panel were characterized in a variety of in vitro and in vivo assays measuring biophys. and functional properties. We observed that slight differences in linker design affected these parameters in disparate ways, and noted that efficacy could be improved by selecting for particular attributes. These studies serve as a starting point for the exploration of more potent noncleavable linker systems.
European Journal of Medicinal Chemistry published new progress about Aldehydes Role: RCT (Reactant), RACT (Reactant or Reagent). 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Quality Control of 112-63-0.
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