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Abstract  

The over-expression of folate receptors in variety of neoplastic tissues makes radiolabeled folate conjugates potential agents for imaging and therapy of such cancers. With the aim of preparing an imaging agent for targeting folate receptors, folic acid has been conjugated with homocysteine for complexation with [99mTc(CO)3(H2O)3]+ core. The radiolabeled complex of the homocysteine-folate could be obtained in >95% radiochemical yield as observed by HPLC. Stability of complex in saline was studied and challenge studies with histidine and cysteine revealed kinetic stability of the complex. Lipophilicity of the radiolabeled complex (log P) was found to be 0.45. In vitro uptake of 99mTc(CO)3-labeled folic acid derivative was studied in KB cells and inhibition studies were carried out using 3H-folic acid and cold homocysteine–folate conjugate. The in vitro studies indicated loss of binding affinity of the derivative towards folate receptors.

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Exploring antibiotic resistant mechanism by microcalorimetry II

Determination of thermokinetic parameters of imipenem hydrolysis with metallo-β-lactamase ImiS

Journal of Thermal Analysis and Calorimetry
Authors: Xia Yang, Lei Feng, Kang-Zhen Xu, Hui-Zhou Gao, Chao Jia, Cheng-Cheng Liu, Jian-Min Xiao, Le Zhai, Li-Sheng Zhou, and Ke-Wu Yang

Stenotrophomonas maltophilia with microcalorimetric method [ 13 ]. In order to further probe the carbapenem hydrolysis with the B2 subclass MβLs, based on over-expression and purification of MβL ImiS, this article first reports the determination of thermokinetic

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