Studies on cis-DDP, [Pt(Dach)(MePhSO)Cl]+ and [PtNH3)2(N-Py)Cl]+ binding to fumarase.
Two platinum analogs which have suitable physical properties and show antineoplastic activities comparable or greater than that obtained with cis-DDP were synthesized: [cis-Pt A2 (Am) Cl] NO3 and [Pt (dach) (RR'SO) Cl] NO3 (A: ammonia, Am: pyridine, dach: transdiaminocyclohexane, RR'SO: methylphenylsulphoxide). Their interactions with fumarase were studied. The inhibition of fumarase activity by the platinum compounds was followed kinetically by a spectrophotometric method. These two platinum compounds generally inhibited fumarase less than cis-DDP at the concentrations and reaction media (phosphate buffer or NaCl-buffer) studied.
Yalçin
G
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University of Marmara, Faculty of Pharmacy, Department of Analytical Chemistry, Istanbul, Turkey.
D000818:Animals; D000970:Antineoplastic Agents / Q000378:metabolism* / Q000494:pharmacology; D001665:Binding Sites; D002945:Cisplatin / Q000031:analogs & derivatives* / Q000378:metabolism* / Q000494:pharmacology; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D005649:Fumarate Hydratase / Q000037:antagonists & inhibitors / Q000378:metabolism*; D006868:Hydrolysis; D007700:Kinetics; D009944:Organoplatinum Compounds / Q000138:chemical synthesis / Q000378:metabolism*; D011485:Protein Binding; D013552:Swine
D000970:Antineoplastic Agents; D004791:Enzyme Inhibitors; D009944:Organoplatinum Compounds; C098398:diamminechloro(pyridine)platinum(I); C098397:chloro(1,2-cyclohexanediamine-N,N')((methylsulfinyl)benzene-S)platinum(I); D005649:Fumarate Hydratase; D002945:Cisplatin