Invention Grant
US09399653B2 Methods and systems for preparing irreversible inhibitors of protein tyrosine phosphatases
有权
用于制备蛋白酪氨酸磷酸酶不可逆抑制剂的方法和系统
- Patent Title: Methods and systems for preparing irreversible inhibitors of protein tyrosine phosphatases
- Patent Title (中): 用于制备蛋白酪氨酸磷酸酶不可逆抑制剂的方法和系统
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Application No.: US13582407Application Date: 2011-03-03
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Publication No.: US09399653B2Publication Date: 2016-07-26
- Inventor: Christopher Warren Cairo , Naresh Singh Tulsi , Alan Michael Downey
- Applicant: Christopher Warren Cairo , Naresh Singh Tulsi , Alan Michael Downey
- Applicant Address: CA Edmonton AB
- Assignee: The Governors of the University of Alberta
- Current Assignee: The Governors of the University of Alberta
- Current Assignee Address: CA Edmonton AB
- Agency: Lathrop & Gage LLP
- International Application: PCT/CA2011/050126 WO 20110303
- International Announcement: WO2011/106898 WO 20110909
- Main IPC: A01N43/00
- IPC: A01N43/00 ; A61K31/33 ; C40B30/04 ; C07D303/02 ; C07D303/36 ; C07F9/38 ; C07K5/08 ; C12Q1/42 ; C07F9/40 ; A61K38/00

Abstract:
Described herein are the preparation and use of novel bromo-phosphonomethylphenylalanine amino acid derivatives (BrPmp) and BrPmp-containing peptides as specific, irreversible protein tyrosine phosphatase inhibitors, which are suitable for application in peptide synthesis. These derivatives are particularly advantageous since their synthesis is both easy and scalable, and they are suitable for peptide synthesis. The BrPmp derivatives described herein can be appropriately protected to allow for solid phase peptide synthesis (SPPS) and incorporation into peptides for preparation of protein tyrosine phosphatase inhibitors and inhibitor libraries. The peptides and peptide libraries can be used to identify new protein tyrosine phosphatase specific sequences and profile protein tyrosine phosphatase activity in cell lysates, diagnostic samples and biopsy samples.
Public/Granted literature
- US20130165333A1 Methods and Systems for Preparing Irreversible Inhibitors of Protein Tyrosine Phosphatases Public/Granted day:2013-06-27
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