34914-36-8Relevant articles and documents
Ribosomal Synthesis of Backbone-Cyclic Peptides Compatible with in Vitro Display
Takatsuji, Ryo,Shinbara, Koki,Katoh, Takayuki,Goto, Yuki,Passioura, Toby,Yajima, Ryo,Komatsu, Yamato,Suga, Hiroaki
supporting information, (2019/02/14)
Backbone-cyclic peptides are an attractive class for therapeutic development. However, in vitro display technologies coupled with ribosomal synthesis are intrinsically inapplicable to such "phenotypes" because of loss of the C-terminal peptide region linking to "genotype". Here, we report a methodology enabling the display of backbone-cyclic peptides. To achieve this, genetic code reprogramming was utilized to implement a rearrangement strategy involving the ribosomal incorporation of a designer initiator containing a thiazolidine-protected cysteine and 2-chloroacetoamide (ClAc) side chain, followed by an α-thio acid and cysteine at downstream positions. Upon expression of the linear peptide, spontaneous thioester rearrangement occurs between the α-thioester and the thiol group of the cysteine, liberating the α-thio group and resulting in cross-linking to the upstream ClAc side-chain group. Then selective deprotection of the thiazolidine-protected cysteine immediately promotes intramolecular native chemical ligation, as demonstrated for various sequences and ring sizes. In this approach, the backbone-cyclic peptides retain their C-terminal peptide regions via the side-chain thioether covalent linkage, making them compatible with in vitro display.
Synthesis of functionalized amides of 2-(arylamino)pyrimidine series
Ignatovich, Zh. V.,Koroleva
, p. 251 - 257 (2017/04/21)
New amides of 2-(arylamino)pyrimidine series were synthesized with pharmacophoric fragments of tyrosine kinase and histone deacetylase inhibitors and functional groups providing chemosorption of compounds on nanocarriers.
RADIOTRACER PRECURSOR BANI FOR IMAGING OF HYPOXIC TISSUE, RADIOTRACER, AND METHOD FOR PREPARING THE SAME
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, (2015/02/18)
The present invention relates to a radiotracer precursor for imaging of hypoxic tissues, a radiotracer and a method for preparing the same. The radiotracer precursor, BANI, includes a nitroimidazole functional group with a feature of retention in hypoxic