ผลต่างระหว่างรุ่นของ "ผู้ใช้:Thomson Walt/กระบะทราย 2"
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Thomson Walt (คุย | ส่วนร่วม) |
Thomson Walt (คุย | ส่วนร่วม) |
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บรรทัด 88:
==การใช้ประโยชน์ทางการแพทย์==
Nitroxoline has been shown to [[Enzyme inhibitor|inhibit the enzymatic activity]] of [[cathepsin B]].<ref>{{cite journal |authors=Mirkovic B, Renko M, Turk S, Sosic I, Jevnikar Z, Obermajer N, Turk D, Gobec S, Kos J |title=Novel Mechanism of Cathepsin B Inhibition by Antibiotic Nitroxoline and Related Compounds |journal=ChemMedChem |volume=6 |pages=1351–1356 |year=2011 |doi=10.1002/cmdc.201100098}}</ref> Cathepsin B degrades extra-cellular membrane proteins in tumor cells, allowing them to proliferate more freely, and metastasize throughout the body. Nitroxoline was shown to be a noncompetitive, reversible inhibitor of these actions in MCF-10A neoT cells. The ''K''<sub>i</sub> ([[dissociation constant]]) values it demonstrates are comparable to other reversible inhibitors of cathepsin B. This indicates that it may be a candidate for further trials as an anticancer drug, especially given its history as an antimicrobial agent and its well-known [[pharmacokinetic]] profile. The mechanism of action by which nitroxoline inhibits cathepsin B may also suggest that further research of noncovalent, noncompetitive inhibitors of cathepsin B could be warranted. In fact, it was recently shown that a balance exists between the potency and the kinetics of a molecule, reflected in the molecular weight, which must be optimized in order to create the best drug for inhibition of a target enzyme.<ref>{{cite journal |authors=Sosic I, Mirkovic B, Arenz K, Stefane B, Kos J, Gobec S |title=Development of New Cathepsin B Inhibitors: Combining Bioisosteric Replacements and Structure-Based Design To Explore the Structure-Activity Relationships of Nitroxoline Derivatives |journal=J Med Chem |volume=56 |pages=521–533 |year=2013 |url=http://pubs.acs.org/doi/abs/10.1021/jm301544x |doi=10.1021/jm301544x}}</ref> For example, a certain inhibitor may have a high affinity for an enzyme, but it may prove impractical to use in a clinical setting for treatment because of its size.
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