Selective Formation of Homo- and Heterobivalent Peptidomimetics

Abstract

Methodology is presented for assembling fluorescently labeled bivalent molecules from monovalent constituents, without side chain protection or coupling agents. To illustrate the procedure, a series of bivalent peptidomimetics directed toward the Trk receptors were prepared and screened via fluorescent activated cell sorting scan assays.

Thermal, Spectral, Fluorescence, and Antimicrobial Studies of Cobalt, Nickel, Copper, and Zinc Complexes Derived from 4-[(5-Bromo-thiophen-2-ylmethylene)-amino]-3-mercapto-6-methyl-5-oxo-[1,2,4]triazine

“…, and 3 A 2g (F) → 3 T 1g (P) (ν 3 ), respectively. The position of these bands indicates that the complexes have an octahedral geometry around the Ni(II) complexes [13,19,[27][28][29][30][31].…”

“…The electronic spectra of Ni(II) complexes display three absorption bands in the range 11261-11376, 16200-16345, and 26115-26238 cm −1 . These bands may be assigned to three spin allowed transitions 3…”

“…Triazine chemistry has attracted attention due to the utility of melamine derivatives as starting material for a variety of polymers [1], as scavenging resins in organic manipulations [2] and in medicinal chemistry [3]. They provide a wide range of applications in the field of optics [4], herbicides [5], and pharmaceuticals [6].…”

Modulation of Protein-Protein Interactions by Stabilizing/Mimicking Protein Secondary Structure Elements

“…Authors claimed that this kind of focused libraries, designed specifically to target receptor hot-spots, may be a general approach to discover functional ligands for PPIs. The assembly of this kind of monomeric peptidomimetics into dimeric structures has once again been explored, leading to some homo-and heterobivalent molecules for further investigation [96,97]. The same group at Texas University has recently published the synthesis of interesting triazole-based β-turn mimetics, as 25, able to favor type I and type II β-turn conformational states, but no indication about biological activity has yet been reported [98].…”

De novo identification of highly active fluorescent kappa opioid ligands from a rhodamine labeled tetrapeptide positional scanning library

“…A recent study has described a combinatorial method for assembling fluorescently labeled compounds that can be screened in direct binding assays to identify small molecule mimics. 23 The rhodamine labeled positional scanning library is composed of four sublibraries, in which each of the four positions are defined with a single amino acid (O) with the three remaining positions made up of a mixture of 52 different l-, d-and unnatural amino acids (X). 11,13 Thus, there are 52 tetrapeptide mixtures per positional sublibrary totaling 208 tetrapeptide mixtures, each made up of 140,608 labeled tetrapeptides, with the library containing a diversity of 7,311,616 tetrapeptides.…”