Please use this identifier to cite or link to this item: http://scholarbank.nus.edu.sg/handle/10635/78637
Title: ACTIVITY-BASED PROTEIN PROFILING (ABPP) BY SMALL MOLECULES LABELING APPROACH
Authors: CHENG XIAMIN
Keywords: Activity-based Protein Profiling, C75, kinase inhibitor, Staurosporine, Lymphostin, Wortmannin
Issue Date: 11-Mar-2014
Source: CHENG XIAMIN (2014-03-11). ACTIVITY-BASED PROTEIN PROFILING (ABPP) BY SMALL MOLECULES LABELING APPROACH. ScholarBank@NUS Repository.
Abstract: Identification of unknown potential targets of bioactive compounds remains an urgent challenge. By taking advantages of Activity-based Protein Profiling (ABPP), in a novel chemical proteomics method, cell-permeable probes derived from the corresponding bioactive molecules have been developed to disclose protein¿small molecule interactions in large-scale under native cellular environments. In this thesis, firstly, we have developed a click-based in situ profiling approach to identify the targets of C75. (Chapter 2) Secondly, a new approach has been successfully established to develop covalent irreversible kinase inhibitors from Staurosporine. (Chapter 3) Thirdly, this approach was applied to scaffolds of Lymphostin (covalent inhibitor) and Ammosamide analogues (affinity inhibitors) (Chapter 4). Fourthly, a novel approach about cancer cell targeting cell-specific drug delivery of protein kinase inhibitors directed by cell penetrating peptide (CPP) is described (Chapter 5). Finally, the project about cancer cell targeting delivery of regenerable Wortmannin by Folic acid is introduced (Chapter 6).
URI: http://scholarbank.nus.edu.sg/handle/10635/78637
Appears in Collections:Ph.D Theses (Open)

Show full item record
Files in This Item:
File Description SizeFormatAccess SettingsVersion 
Cheng XM.pdf15.39 MBAdobe PDF

OPEN

NoneView/Download

Page view(s)

105
checked on Jan 19, 2018

Download(s)

36
checked on Jan 19, 2018

Google ScholarTM

Check


Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.