Triazaspiroalkenes as potential inhibitors of dihydrofolate reductase 1

... 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

... 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

... 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

... which was slightly active on the wild-type RT RNase H function, showed a sixfold increase in the inhibition potency of the RNase H function, although it retained its inhibition potency on the ... AQ derivatives and other RT inhibitors (A) YonetaniTheorell plot of the combination of K-49 and RDS 1643 on the HIV-1 RT polymeraseindependent RNase H a...

Ngày tải lên: 22/03/2014, 16:20

... 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

... treated with lM OA for h, and then with 10 lM taxol for 10 Cytoskeletons were isolated and incubated for the stated times to determine the amount of tubulin carboxypeptidase activity associated with ... Exposure of cells to OA induces redistribution of tubulin carboxypeptidase activity between the microtubuleassociated and nonassociated states The sca...

Ngày tải lên: 23/03/2014, 15:21

... ,doirep latnemirepxe eritne eht tuohguorht mutibil da retaw pat gniknird dna )aeroK ,gnaymaS( teid lamron a nevig erew slaminA aeroK ni ytisrevinU lanoitaN nowgnaK ta ytilicaf lamina devorppa na ni ... edixO cirtiN sisenegonicrac detaidem-noitammalfni fo ledom a : htiw detcefni sretsmah ni egamad AND evitartin inirreviv sihcrohtsipO dna evitadixo detaidem-ON fo msinahceM S ihsinawaK ,P...

Ngày tải lên: 07/08/2014, 18:21

... 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

... 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

... 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

... presence of four families of type II transmembrane serine proteinase [30] The matriptase subfamily constitutes three members (matriptase, matriptase and matriptase 3) It is conceivable that some of ... analyses of purified matriptase Soluble matriptase was purified from the conditioned medium of DLD-1 cells as described in the text The purified matriptase (approximate...

Ngày tải lên: 19/02/2014, 07:20