Peptide-based activity-based probes (ABPs) for target-specific profiling of protein tyrosine phosphatases (PTPs).
نویسندگان
چکیده
Synthesis of a novel unnatural amino acid (2-FMPT) for the solid-phase synthesis of peptide-based probes suitable for target-specific activity-based profiling of protein tyrosine phosphatases from crude proteomes is reported.
منابع مشابه
Probing the target-specific inhibition of sensitized protein tyrosine phosphatases with biarsenical probes.
Selective control of enzyme activity is critical for elucidating the roles of specific proteins in signaling pathways. One potential means for developing truly target-specific inhibitors involves the use of protein engineering to sensitize a target enzyme to inhibition by a small molecule that does not inhibit homologous wild-type enzymes. Previously, it has been shown that protein tyrosine pho...
متن کاملHypervalent organochalcogenanes as inhibitors of protein tyrosine phosphatases.
A series of organochalcogenanes was synthesized and evaluated as protein tyrosine phosphatases (PTPs) inhibitors. The results indicate that organochalcogenanes inactivate the PTPs in a time- and concentration-dependent fashion, most likely through covalent modification of the active site sulfur-moiety by the chalcogen atom. Consequently, organochalcogenanes represent a new class of mechanism-ba...
متن کاملSmall molecule probes that target Abl kinase.
Two different strategies, namely a dialdehyde-based cross-linking and photo-affinity labeling, have been developed to generate small molecule activity-based probes (ABPs) for the Abelson (Abl) tyrosine kinase, of which probe 13, derived from the photo-affinity approach, showed specific labeling of Abl kinase present in a crude mammalian proteome.
متن کاملDeep Insight Section
Tyrosine phosphorylation is a key mechanism for signal transduction and for the regulation of many cellular processes (Mustelin et al., 2005; Tonks, 2006). The protein tyrosine kinases (PTKs) phosphorylate at tyrosine residues and the protein tyrosine phosphatases (PTPs) dephosphorylate. The human PTP genes are divided into several families: Class I cysteine-based PTPs, class II cysteine-based ...
متن کاملProteinaceous Regulators and Inhibitors of Protein Tyrosine Phosphatases.
Proper control of the phosphotyrosine content in signal transduction proteins is essential for normal cell behavior and is lost in many pathologies. Attempts to normalize aberrant tyrosine phosphorylation levels in disease states currently involve either the application of small compounds that inhibit tyrosine kinases (TKs) or the addition of growth factors or their mimetics to boost receptor-t...
متن کاملذخیره در منابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
عنوان ژورنال:
- Chemical communications
دوره 46 4 شماره
صفحات -
تاریخ انتشار 2010