150629-67-7Relevant articles and documents
A Novel Lysine-protecting Procedure for Continuous Flow Solid Phase Synthesis of Branched Peptides
Bycroft, Barrie W.,Chan, Weng C.,Chhabra, Siri Ram,Hone, Neal D.
, p. 778 - 779 (1993)
A new amine protecting group which can be used orthogonally with both Fmoc and Boc protection is reported; by employing lysine protected appropriately as the branching motif, a 34 residue di-epitopic peptide has been constructed by continuous flow solid phase peptide synthesis.
One-Bead-Two-Compound Thioether Bridged Macrocyclic γ-AApeptide Screening Library against EphA2
Shi, Yan,Challa, Sridevi,Sang, Peng,She, Fengyu,Li, Chunpu,Gray, Geoffrey M.,Nimmagadda, Alekhya,Teng, Peng,Odom, Timothy,Wang, Yan,Van Der Vaart, Arjan,Li, Qi,Cai, Jianfeng
, p. 9290 - 9298 (2017/11/30)
Identification of molecular ligands that recognize peptides or proteins is significant but poses a fundamental challenge in chemical biology and biomedical sciences. Development of cyclic peptidomimetic library is scarce, and thus discovery of cyclic peptidomimetic ligands for protein targets is rare. Herein we report the unprecedented one-bead-two-compound (OBTC) combinatorial library based on a novel class of the macrocyclic peptidomimetics γ-AApeptides. In the library, we utilized the coding peptide tags synthesized with Dde-protected α-amino acids, which were orthogonal to solid phase synthesis of γ-AApeptides. Employing the thioether linkage, the desired macrocyclic γ-AApeptides were found to be effective for ligand identification. Screening the library against the receptor tyrosine kinase EphA2 led to the discovery of one lead compound that tightly bound to EphA2 (Kd = 81 nM) and potently antagonized EphA2-mediated signaling. This new approach of macrocyclic peptidomimetic library may lead to a novel platform for biomacromolecular surface recognition and function modulation.
OPTICAL IMAGING PROBES
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, (2014/05/20)
The present invention relates to methods of visualising cells especially although not exclusively in vivo using a dye, such as a dendrimer-dye molecule or polybranched-dye molecule which is internalised by the cells and thus permits subsequent visualisation by confocal fluorescence endomicroscopy or other optical detectors. There is also provided internally quenched probes for use in visualising cells especially although not exclusively in vivo by confocal fluorescence endomicroscopy and the use of internally quenched probes in combination with confocal fluorescence endomicroscopy, for visualising cells by virtue of internalisation and dequenching of a probe by the cells. In a particular embodiment the cells are activated neutrophils, such as within the lung of a subject.