Middle molecular and conjugation strategies for development of bioactive middle molecules

Recently, development of bioactive molecules based on polypharmacology has attracted much attention. Conjugation of bioactive molecules can afford biofunctional middle molecules possessing polypharmacological action. These conjugated compounds are called small molecule drug conjugates (SMDC), which are a class of medium-sized drugs. A similar conjugation strategy, a self-adjuvanting strategy, has been used for vaccine development. Covalently linked antigen-adjuvant conjugates are used as self-adjuvanting vaccines. The antigen-adjuvant conjugates are taken up by the antigen-presenting cells via the interactions between innate immune receptors and their ligands, and the adjuvants activate the immune system and efficiently induce antibodies. Here, we developed cancer vaccine candidates consisting in tri-peptides of a tumor associated carbohydrate antigens (TACA), a lipopeptide adjuvant (a TLR2 ligand), and a T cell epitope. © 2020 Society of Synthetic Organic Chemistry. All rights reserved.