Triazaspiroalkenes as potential inhibitors of dihydrofolate reductase 2

... Methotrexate (MTX) 7 .2. 4.1 .2 Library P-IV 7 .2. 4 .2 Cell Cycle Analysis of MDA-MB -23 1 Post Compound Treatment 7 .2. 4 .2. 1 Library P-IV Conclusion 122 122 125 1 32 1 32 139 CONCLUSION AND FUTURE WORK CHAPTER ... points of library of P-IV 111 22 Recombinant human DHFR inhibitory activity of library P-IV 1 12 23 Percentage of cell viability of A549 and MDA-MB -23 1 afte...

Ngày tải lên: 14/09/2015, 08:50

... Program (Office of Life Science) and National University of Singapore for providing me the research scholarship I will also like to thank Dr Gigi Chiu (Department of Pharmacy), A/Prof Prof Yao ... supervisor A/Prof Chui Wai Keung, who has guided and supported me throughout my PhD study whilst allowing me the room to work in my own way Thanks to A/Prof Chan Sui Yung, Head of Department...

Ngày tải lên: 14/09/2015, 08:50

... review will be based on a particular enzyme of our interest The enzyme of interest here is dihydrofolate reductase (DHFR) DHFR catalyses the conversion of dihydrofolate to tetrahydrofolate It is ... has also led to revolution in the design of DHFR inhibitors These studies led to the development of two distinct classes of DHFR inhibitors, i.e classical and non-classical DH...

Ngày tải lên: 14/09/2015, 08:50

... attention has been given to the role of angiogenesis in cancer One of the earliest references to angiogenesis and cancer was made by Ide and Figure 1.3B Diseases Resulting from Abnormal Levels of Angiogenesis ... engaged in the development of dual inhibitors of angiogenesis and cancer cell proliferation This effort originated with the goal of modifying...

Ngày tải lên: 13/11/2014, 11:20

... thermal stability of site-selectively glycosylated dihydrofolate reductase ChemBioChem 6, 1338–1340 15 Baek WO & Vijayalakshmi MA (1997) Effect of chemical glycosylation of Rnase A on the protein stability ... simulation of Escherichia coli dihydrofolate reductase: thermal stability of protein domains and unfolding pathway Proteins 46, 308–320 42 Frieden C (1990) Refo...

Ngày tải lên: 15/03/2014, 11:20

... distinctly generated Synovial tissues released miRNAs similar to synovial fluid miRNAs To estimate the origin of plasma or synovial fluid miRNAs, FLSs, synovial tissues, PB MNCs, and synovial fluid ... the handiness of plasma and synovial fluid miRNAs as biomarkers Although we showed that synovial tissue is a main source of synovial fluid miRNA, the mec...

Ngày tải lên: 12/08/2014, 12:20

... ALDH 8A1 ALDH 6A1 9q21.13 15q 22. 1 15q26.3 9p11.1 12q24 .2 3q21 .2 2q23.3 1q23.1 6p 22. 2 6q23 .2 14q24.3 ALDH 3A1 ALDH 3A2 ALDH3B1 ALDH3B2 ALDH1 8A1 ALDH1 6A1 17p11 .2 17p11 .2 11q13 .2 11q13 .2 10q24.3 19q13.33 ... database (114, Adapted from Strickland et al., 20 11) Gene Name ALDH 4A1 ALDH 7A1 Chromosome location 1p36.13 5q31 ALDH 1A1 ALDH 1A2 ALDH 1A3 ALDH1B1 ALDH2 ALDH1L1 ALDH1...

Ngày tải lên: 24/08/2014, 09:58

... orally [27] Therefore, the aim of the present study was to evaluate the inhibitory effect of some thioglycosides synthesized in our laboratory on human hSGLT1 and hSGLT2 as a potential therapeutic ... O-glucosides involved in the biosynthesis of chrysomelidial and salicin These substances are synthesized and secreted as part of a defense mechanism used by la...

Ngày tải lên: 26/10/2012, 10:04

... such as the p38 MAPK pathway [17] The MAPKs operate as a series of kinase modules beginning with the MAPK kinase kinases (MKKKs), which phosphorylate MAPK kinases (MKKs), which ultimately phosphorylate ... model These data suggest that p38 inhibitors may be beneficial in the treatment of both joint degeneration and pain associated with OA Materials and...

Ngày tải lên: 11/08/2014, 08:22

... migration of endothelial cells.64 Thymidine phosphorylase promotes tumor metastasis It has been found that high TP expression was associated with metastasis, and TP was able to increase the metastatic ... derivatives as inhibitors of thymidine phosphorylase 23 ii 1.2.3.2 Purine derivatives as inhibitors of thymidine phosphorylase 29 1.2.3.3 Thymidine phosphorylase inhibit...

Ngày tải lên: 10/09/2015, 09:12

... SYNTHESIS OF GUANIDINO ANALOGUES AS POTENTIAL NITRIC OXIDE SYNTHASE INHIBITORS BONG YONG KOY 2004 SYNTHESIS OF GUANIDINO ANALOGUES AS POTENTIAL NITRIC OXIDE SYNTHASE INHIBITORS BONG ... Oxide Synthase (NOS) Isoforms of Nitric Oxide Synthase Physiological Roles of NO and Pathology of NO Overproduction Inhibition of Nitric Oxide Syn...

Ngày tải lên: 16/09/2015, 17:13

... of pravastatin in human erythrocytes The current work studies effect of time, temperature as well as drug concentration on the process of pravastatin loading into human erythrocytes by endocytosis ... characterization of pravastatin loaded erythrocytes Hematological Indices To determine the effect of loading process on erythrocytes, normal erythrocytes, erythrocyt...

Ngày tải lên: 25/10/2012, 11:10

... on fibrin polymerization in two kinds of assay In the first assay, the formation of fibrin was followed directly after the addition of thrombin In the second assay, previously prepared fibrin was ... reaction and the re-association of fibrin desAABB indicates that calixarene retards clotting not as a result of the inhibition of thrombin, but entirely because of th...

Ngày tải lên: 06/03/2014, 00:21

... ATGGCGCCATTTTTCTTGAGACATGCC-3¢; reverse, 5¢-CTGGGATCCGTCCGAATCAGGTTCCTTC-3¢ (purchased from Sigma), and the pKK plasmid as a template [32] The resulting fragment was cloned into NcoI and BamHI sites of the ... Suv3(D1-159) and WNV NTPase/helicases The NTPase/helicase domain of HCV NS3 was expressed in E coli and purified as described previously [30], with certain modi...

Ngày tải lên: 08/03/2014, 02:20

... determine experimentally either the Kd or the binding energies for the apoFNR :FAD complexes in any redox state However, as the reduction potentials of free and bound FAD are linked to the binding ... structural differences in FAD conformation and binding to the protein [5], the shifts observed in the binding affinities of the three FAD redox forms to apoFNR cannot be...

Ngày tải lên: 08/03/2014, 23:20