Douat-Casassus, Celine published the artcileSynthetic anticancer vaccine candidates: rational design of antigenic peptide mimetics that activate tumor-specific T-cells, Synthetic Route of 167015-84-1, the publication is Journal of Medicinal Chemistry (2007), 50(7), 1598-1609, database is CAplus and MEDLINE.
A rational design approach was followed to develop peptidomimetic analogs of a cytotoxic T-cell epitope capable of stimulating T-cell responses as strong as or stronger (heteroclytic) than those of parental antigenic peptides. The work described herein focused on structural alterations of the central amino acids of the melanoma tumor-associated antigenic peptide Melan-A/MART-126-35 using nonpeptidic units. A screening was first realized in silico to select altered peptides potentially capable of fitting at the interface between the major histocompatibilty complex (MHC) class-I HLA-A2 mol. and T-cell receptors (TCRs). Two compounds appeared to be high-affinity ligands to the HLA-A2 mol. and stimulated several Melan-A/MART-1 specific T-cell clones. Most remarkably, one of them even managed to amplify the response of one clone. Together, these results indicate that central TCR-contact residues of antigenic peptides can be replaced by nonpeptidic motifs without loss of binding affinity to MHC class-I mols. and T-cell triggering capacity.
Journal of Medicinal Chemistry published new progress about 167015-84-1. 167015-84-1 belongs to indole-building-block, auxiliary class Indols, name is tert-Butyl 3-(2-aminoethyl)-1H-indole-1-carboxylate, and the molecular formula is C15H20N2O2, Synthetic Route of 167015-84-1.
Referemce:
https://www.nature.com/articles/s41429-020-0333-2,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles