Cover Feature: Modulation of Src Kinase Activity by Selective Substrate Recognition with Pseudopeptidic Cages (Chem. Eur. J. 37/2021)
نویسندگان
چکیده
The modulation of the activity tyrosine kinases (TK) is an appealing topic current research. This work presents new pseudopeptidic cages that protect substrates from action TK enzyme, precluding corresponding Tyr phosphorylation, with a very good correlation between caging and kinase inhibition. results illustrate how signaling can be efficiently selectively modulated supramolecular complexes. More information found in Full Paper by W. T. Miller, I. Alfonso, et al. (DOI: 10.1002/chem.202100990).
منابع مشابه
Stereoselective recognition of the Ac-Glu-Tyr-OH dipeptide by pseudopeptidic cages.
Pseudopeptidic molecular cages are appealing receptors since they can display different polar and non-polar interaction sites in a modular framework and a controlled disposition. Inspired by previous host-guest knowledge, two pseudopeptidic molecular cages based on serine and threonine (CySer and CyThr, respectively) were designed and synthesized as hosts for the binding of the four possible st...
متن کاملModulation of TRPV1 by nonreceptor tyrosine kinase, c-Src kinase.
The capsaicin receptor TRPV1 is a nonselective cation channel that is expressed in sensory neurons. In this study, we examined the role of the nonreceptor cellular tyrosine kinase c-Src kinase in the modulation of the rat TRPV1. Capsaicin-induced currents in identified colonic dorsal root ganglion neurons were blocked by the c-Src kinase inhibitor PP2 and enhanced by the tyrosine phosphatase in...
متن کاملControl of src kinase activity by activators, inhibitors, and substrate chaperones.
The activities of src tyrosine kinases are greatly influenced by substrate modulators (chaperones). In the presence of bovine serum albumin, the phosphorylation of a random polymer of glutamic acid, alanine, and tyrosine (1:1:1) by src kinases is stimulated 20- to 100-fold, but there is little stimulation with a polymer of glutamic acid and tyrosine (4:1) as substrate. This suggests that serum ...
متن کاملSubstrate Recognition by Osteoclast Precursors Induces C-src/Microtubule Association
The osteoclast is distinguished from other macrophage polykaryons by its polarization, a feature induced by substrate recognition. The most striking component of the polarized osteoclast is its ruffled membrane, probably reflecting insertion of intracellular vesicles into the bone apposed plasmalemma. The failure of osteoclasts in c-src-/- osteopetrotic mice to form ruffled membranes indicates ...
متن کاملCoupling kinase activation to substrate recognition in SRC-family tyrosine kinases.
Signal transduction molecules translate extracellular inputs into their corresponding intracellular responses. Given the complexity and number of signaling pathways present in the eukaryotic cell, it is not surprising that the functions of signaling molecules are often tightly regulated. Autoinhibition is a prevalent mechanism for governing the function of signaling molecules. The relationship ...
متن کاملذخیره در منابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
ژورنال
عنوان ژورنال: Chemistry: A European Journal
سال: 2021
ISSN: ['0947-6539', '1521-3765']
DOI: https://doi.org/10.1002/chem.202101933