Chemistry is an experimental science, Recommanded Product: 4-Ethoxy-3-(1-methyl-7-oxo-3-propyl-6,7-dihydro-1H-pyrazolo[4,3-d]pyrimidin-5-yl)benzene-1-sulfonyl chloride, and the best way to enjoy it and learn about it is performing experiments.Introducing a new discovery about 139756-22-2, Name is 4-Ethoxy-3-(1-methyl-7-oxo-3-propyl-6,7-dihydro-1H-pyrazolo[4,3-d]pyrimidin-5-yl)benzene-1-sulfonyl chloride, molecular formula is C17H19ClN4O4S, belongs to pyrimidines compound. In a document, author is Holanda, Rudson J..
Plasmodium falciparum purine nucleoside phosphorylase as a model in the search for new inhibitors by high throughput screening
Studies have shown that inhibition of Plasmodium falciparum Purine Nucleoside Phosphorylase (PfPNP) blocks the purine salvage pathway in vitro and in vivo. In this study, PfPNP was evaluated as a model in the search for new inhibitors using surface plasmon resonance (SPR). Its expression, purification, oligomeric state, kinetic constants, calorimetric parameters and kinetic mechanisms were obtained. PfPNP was immobilized on a CM5 sensor chip and sensorgrams were produced through binding the enzyme to the substrate MESG and interactions between molecules contained in 10 fractions of natural extracts. The oligomeric state showed that recombinant PfPNP is a hexamer. The true steady-state kinetic parameters for the substrate inosine were: K-M 17 mu M, k(cat) 1.2 s(-1), V-Max 2.2 U/mg and k(cat)/K-M 7 x 10(-4); for MESG they were: K-M 131 mu M, k(cat) 2.4 s(-1), V-Max 4.4 U/mg and k(cat)/K-M 1.8 x 10(-4). The thermodynamic parameters for the substrate Phosphate were: Delta(G) – 5.8 cal mol(-1), Delta(H) – 6.5 cal mol(-1) and Delta(S) – 2.25 cal mol(-1)/degree. The ITC results demonstrated that the binding of phosphate to free PfPNP led to a significant change in heat and association constants and thermodynamic parameters. A sequential ordered mechanism was proposed as the kinetic mechanism. Three plant extracts contained molecules capable of interacting with PfPNP, showing different levels of affinity. The identification of plant extract fractions containing molecules that interact with recombinant PfPNP using SRP validates this target as a model in the search for new inhibitors. In this study, we showed for the first time the true steady-state kinetic parameters for reactions catalyzed by PfPNP and a model using PfPNP as a target for High-throughput Screening for new inhibitors through SPR. This knowledge will allow for the development of more efficient research methods in the search for new drugs against malaria. (c) 2020 Published by Elsevier B.V.
Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law. In my other articles, you can also check out more blogs about 139756-22-2. Recommanded Product: 4-Ethoxy-3-(1-methyl-7-oxo-3-propyl-6,7-dihydro-1H-pyrazolo[4,3-d]pyrimidin-5-yl)benzene-1-sulfonyl chloride.
Reference:
Pyrimidine | C4H4N2 – PubChem,
,Pyrimidine – Wikipedia