Design, synthesis and catalytic activity of a serine protease synthetic model

1997 ◽  
Vol 4 (4-6) ◽  
pp. 481-487 ◽  
Author(s):  
Athanassios Stavrakoudis ◽  
Ioannis N. Demetropoulos ◽  
Constantinos Sakarellos ◽  
Maria Sakarellos-Daitsiotis ◽  
Vassilios Tsikaris
2019 ◽  
Vol 126 ◽  
pp. 229-237 ◽  
Author(s):  
Naeem Mahmood Ashraf ◽  
Akshaya Krishnagopal ◽  
Aadil Hussain ◽  
David Kastner ◽  
Ahmed Mahmoud Mohammed Sayed ◽  
...  

2019 ◽  
Vol 20 (7) ◽  
pp. 1557 ◽  
Author(s):  
Natalia Gruba ◽  
Ewa Bielecka ◽  
Magdalena Wysocka ◽  
Anna Wojtysiak ◽  
Magdalena Brzezińska-Bodal ◽  
...  

Kallikrein 13 (KLK13) was first identified as an enzyme that is downregulated in a subset of breast tumors. This serine protease has since been implicated in a number of pathological processes including ovarian, lung and gastric cancers. Here we report the design, synthesis and deconvolution of libraries of internally quenched fluorogenic peptide substrates to determine the specificity of substrate binding subsites of KLK13 in prime and non-prime regions (according to the Schechter and Berger convention). The substrate with the consensus sequential motive ABZ-Val-Arg-Phe-Arg-ANB-NH2 demonstrated selectivity towards KLK13 and was successfully converted into an activity-based probe by the incorporation of a chloromethylketone warhead and biotin bait. The compounds described may serve as suitable tools to detect KLK13 activity in diverse biological samples, as exemplified by overexpression experiments and targeted labeling of KLK13 in cell lysates and saliva. In addition, we describe the development of selective activity-based probes targeting KLK13, to our knowledge the first tool to analyze the presence of the active enzyme in biological samples.


2018 ◽  
Vol 3 (2) ◽  
pp. 348-356 ◽  
Author(s):  
Danning Zheng ◽  
Tengfei Wang ◽  
Xinrui Zhu ◽  
Ci Chen ◽  
Tiegang Ren ◽  
...  

Three new protic pyrazolium ILs, HTMPzBr, HMM3PzBr, and HMM5PzBr, have been synthesized to explore their catalytic activity for the coupling reaction of carbon dioxide and propylene oxide.


2019 ◽  
Vol 16 (7) ◽  
pp. 1010-1023
Author(s):  
Behzad Zeynizadeh ◽  
Maryam Sadeghbari ◽  
Nader N. Pesyan

Aim and Objective: Nowadays, the design, synthesis and application of magnetically nanocomposite systems have attracted the attention of numerous scientists. The huge surface area and magnetic characteristic of nanoparticles as well as the inherent potentiality of the used metal species, makes them susceptible to have different reactivity in chemical reactions. In this context, we therefore encouraged to prepare a new design of magnetic nanocatalysts as CuFe2O4@SiO2@AAPTMS@Ni(II) and CuFe2O4@SiO2@AAPTMS@Cu(II) followed by monitoring of their catalytic activities towards reduction of nitroarenes with NaBH4. Materials and Methods: Magnetically nanoparticles of CuFe2 O4@SiO2@AAPTMS@Ni(II) and CuFe2O4@SiO2@AAPTMS@Cu(II) were prepared through a four-step procedure: i) preparation of CuFe2O4 MNPs, ii) coating of CuFe2O4 nucleus by silica-layer using tetraethyl orthosilicate (TEOS), iii) layering of CuFe2O4@SiO2 MNPs with [3-(2-aminoethylamino)propyl] trimethoxysilane (AAPTMS), and iv) the complexation of CuFe2O4@SiO2@AAPTMS MNPs with an aqueous solution of Ni(OAc)2·4H2O or Cu(OAc)2·H2O. Results: The catalytic activity of CuFe2O4@SiO2@AAPTMS@Ni(II) and the Cu(II)-analogue towards reduction of nitroarenes with NaBH4 was studied. The examinations resulted that using a molar ratio of 1:2 for ArNO2 and NaBH4 in the presence of 20 mg of nanocomposites in H2O under reflux conditions reduces various aromatic nitro compounds to arylamines in high yields. Conclusion: The immobilization of Ni(II) and Cu(II) species on silica-layered CuFe2O4 was investigated. Magnetically nanoparticles of CuFe2O4@SiO2@AAPTMS@Ni(II) and the Cu(II)-analogue showed the perfect catalytic activity towards reduction of nitroarenes with NaBH4 in H2O. All reactions were carried out within 2– 15 min to afford aniline products in high yields.


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