Identification of new peptide amides as selective cathepsin L inhibitors: The first step towards selective irreversible inhibitors?
摘要:
A small library of peptide amides was designed to profile the cathepsin L active site. Within the cathepsin family of cysteine proteases, the first round of selection was on cathepsin L and cathepsin B, and then selected hits were further evaluated for binding to cathepsin K and cathepsin S. Five highly selective sequences with submicromolar affinities towards cathepsin L were identified. An acyloxymethyl ketone warhead was then attached to these sequences. Although these original irreversible inhibitors inactivate cathepsin L, it appears that the nature of the warhead drastically impact the selectivity profile of the resulting covalent inhibitors. (C) 2013 Elsevier Ltd. All rights reserved.
Efficient synthesis of protein-oligonucleotide conjugates
申请人:——
公开号:US20030092901A1
公开(公告)日:2003-05-15
The present invention relates to an improved method for forming a protein-oligonucleotide conjugate. The method is particularly amenable for forming antibody-oligonucleotide conjugates. The invention further concerns the conjugate molecules produced using such improved methods.
EFFICIENT SYNTHESIS OF PROTEIN-OLIGONUCLEOTIDE CONJUGATES
申请人:Beckman-Coulter, Inc.
公开号:EP1485500A2
公开(公告)日:2004-12-15
EP1485500A4
申请人:——
公开号:EP1485500A4
公开(公告)日:2005-12-07
Cell-based microarrays, and methods for their preparation and use
申请人:Reddy Parameswara M.
公开号:US20060292559A1
公开(公告)日:2006-12-28
The present invention is in the field of chemistry and biotechnology. The present invention relates to cell-based microarrays, improved methods for forming such arrays, and methods for using such arrays in diagnostics, therapeutics and research. The invention particularly concerns microarrays in which ligands of a target cells are immobilized to the array support via ligand-binding molecules bound to an oligonucleotide that is hybridized to a support-immobilized oligonucleotide.