Design and Combinatorial Development of Shield-1 Peptide Mimetics Binding to Destabilized FKBP12 was written by Madsen, Daniel;Joergensen, Frederik P.;Palmer, Daniel;Roux, Milena E.;Olsen, Jakob V.;Bols, Mikael;Schoffelen, Sanne;Diness, Frederik;Meldal, Morten. And the article was included in ACS Combinatorial Science in 2020.Computed Properties of C21H21NO4 The following contents are mentioned in the article:
The destabilizing domain (DD) is a double point-mutated version of the human protein FKBP12, and it has proven its vast utility in several biol. systems, where the level of a fused protein-of-interest may be controlled by the addition of the stabilizing small mol. Shield-1 (Shld1). With the aim of developing small peptide derived ligands that mimic the Shld1-DD interaction, we here report the synthesis and screening of a one-bead one-compound library consisting of triazole containing tripeptides. The library of peptide mimetics was synthesized on MicroParticle Matrix encoded PEGA1900 beads and deconvoluted using a decoder apparatus Verification of the hit’s activities was performed using an on-bead binding assay, where the binding profile of the immobilized substrates were correlated to a solid-supported version of the known SLF* ligand. These studies guided the design of small peptide-like compounds, which were readily synthesized in solution or on solid-support. The binding affinity of these focused peptide libraries towards the DD was tested using a competitive fluorescence polarization assay, which led to the discovery of peptide-ligands with low micromolar binding affinity. This study involved multiple reactions and reactants, such as (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5Computed Properties of C21H21NO4).
(S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5) belongs to piperidine derivatives. The piperidine ring can be found not only in more than half of the currently known structures of alkaloids, but also in many natural or synthetic compounds with interesting biological activities. Piperidine derivatives bearing a masked aldehyde function in the 蔚-position are easily transformed into quinolizidine compounds through intramolecular reductive amination.Computed Properties of C21H21NO4
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem