Proteinaceous Regulators and Inhibitors of Protein Tyrosine Phosphatases.

摘要: Proper control of the phosphotyrosine content in signal transduction proteins is essential for normal cell behavior and lost many pathologies. Attempts to normalize aberrant tyrosine phosphorylation levels disease states currently involve either application small compounds that inhibit kinases (TKs) or addition growth factors their mimetics boost receptor-type TK activity. Therapies target enzymatic counterparts, multi-enzyme family protein phosphatases (PTPs), are still lacking despite undisputed involvement human diseases. Efforts pharmacologically modulate PTP activity have been frustrated by conserved structure catalytic core, providing a daunting problem with respect specificity. Over years, however, different interaction-based regulatory mechanisms uncovered, alternative possibilities PTPs individually. Here, we review these principles, discuss existing biologics proteinaceous affect activity, mention future opportunities drug via concepts.