Research Topics
| S AhmedSummaryAffiliation: Kingston University Country: UK Publications
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Detail Information
Publications
Structure activity relationship study of known inhibitors of the enzyme 5 alpha-reductase (5AR)S Ahmed
School of Applied Chemistry, Kingston University, Surrey
Bioorg Med Chem Lett 8:409-14. 1998....
Hydrophobicity, a physicochemical factor in the inhibition of the enzyme estrone sulfatase (ES)S Ahmed
School of Chemical and Pharmaceutical Sciences, Kingston University, Penrhyn Road, Kingston upon Thames, KT1 2EE, Surrey, UK
Bioorg Med Chem Lett 11:2525-8. 2001..Analysis of the SAR data shows a strong correlation between IC(50) and logP but also supports our previous study, which suggests a very strong relationship between pK(a) and IC(50)...
A novel molecular modelling study of inhibitors of the 17alpha-hydroxylase component of the enzyme system 17alpha-hydroxylase/17,20-lyase (P-450(17alpha))S Ahmed
School of Applied Chemistry, Kingston University, Kingston upon Thames, UK
Bioorg Med Chem 7:1487-96. 1999..Overall, the study suggests that the novel substrate-heme complex approach has provided a good approximation of the 17alpha-OHase active site and has proved to be a useful tool in drug design and discovery...
The mechanism of the irreversible inhibition of estrone sulfatase (ES) through the consideration of a range of methane- and amino-sulfonate-based compoundsSabbir Ahmed
School of Chemical and Pharmaceutical Sciences, Kingston University, Penrhyn Road, Surrey, KT1 2EE, Kingston upon Thames, UK
Bioorg Med Chem Lett 12:1279-82. 2002....
Inhibition of estrone sulfatase (ES) by derivatives of 4-[(aminosulfonyl)oxy] benzoic acidSabbir Ahmed
School of Chemical and Pharmaceutical Sciences, Kingston University, Kingston upon Thames, Surrey, UK
Bioorg Med Chem Lett 12:2391-4. 2002..Furthermore, the data suggest a strong correlation between logP and IC(50) and therefore adds further support to our previous report where we suggested a link between inhibitory activity and hydrophobicity...
Mechanism based representation of the active site of 5 alpha-reductase (5AR)S Ahmed
School of Applied Chemistry, Kingston University, Kingston upon Thames, Surrey, UK
Bioorg Med Chem Lett 8:2615-70. 1998....
Mechanism of 17 alpha-hydroxylase/17,20-lyase--an initial geometric perspective for the lyase of the C(17)-C(20) bond of C21 steroidsS Ahmed
School of Applied Chemistry, Kingston University, Kingston upon Thames, Surrey, UK
Bioorg Med Chem Lett 8:1023-8. 1998....
Novel inhibitors of the enzyme estrone sulfatase (ES)S Ahmed
School of Chemical and Pharmaceutical Sciences, Kingston University, Kingston upon Thames, Surrey, UK
Bioorg Med Chem Lett 11:841-4. 2001..The results of the study show that these compounds are potent inhibitors, possessing greater inhibitory activity than COUMATE, but weaker activity than EMATE. Furthermore, the compounds are observed to be irreversible inhibitors...
Determination and use of a transition state for the enzyme estrone sulfatase (ES) from a proposed reaction mechanismS Ahmed
School of Chemical and Pharmaceutical Sciences, Kingston University, Penrhyn Road, Kingston upon Thames, Surrey KT1 2EE, UK
Bioorg Med Chem Lett 11:3001-5. 2001..Using the derived structure, we have undertaken the molecular modelling of several steroidal and non-steroidal inhibitors in an attempt to rationalise the inhibitory activity of a number of potent inhibitors...
Acid dissociation constant, a potential physicochemical factor in the inhibition of the enzyme estrone sulfatase (ES)S Ahmed
School of Chemical and Pharmaceutical Sciences, Kingston University, Kingston upon Thames, Surrey, UK
Bioorg Med Chem Lett 11:899-902. 2001..We postulate that the stability of the phenoxide ion, as indicated by the acid dissociation constant, is an important factor in the irreversible inhibition of this enzyme...
First report of the investigation into the importance of pK(a) in the inhibition of estrone sulfatase by sulfamate containing compoundsS Ahmed
School of Chemical and Pharmaceutical Sciences, Kingston University, Kingston upon Thames, Surrey, United Kingdom
Biochem Biophys Res Commun 272:583-5. 2000..The results of the study suggest that there is a strong correlation between the inhibitory activity and the stability of the resulting O(-) anion (i.e., the pK(a) of the starting phenol)...
Derivation of a possible transition-state for the reaction catalysed by the enzyme estrone Sulfatase (ES)S Ahmed
School of Applied Chemistry, Kingston University, Kingston upon Thames, Surrey, UK
Bioorg Med Chem Lett 9:1645-50. 1999..Using the derived structure, we have superimposed several steroidal and non-steroidal inhibitors in an attempt to rationalise the inhibitory activity of a number of potent inhibitors...
The use of the substrate-heme complex approach in the design, synthesis, biochemical evaluation, and rationalization of the inhibitory activity of a range of azole compounds against cholesterol side chain cleavage enzymeS Ahmed
School of Chemical and Pharmaceutical Sciences, Kingston University, Penrhyn Road, Kingston upon Thames, Surrey, KT1 2EE, United Kingdom
Biochem Biophys Res Commun 275:75-6. 2000....
Synthesis and biochemical evaluation of novel inhibitors of aromatase (AR) using an enhanced representation of the active site of AR derived from the consideration of the reaction mechanismS Ahmed
School of Applied Chemistry, Kingston University, Penrhyn Road, Kingston upon Thames, Surrey, KT1 2EE, United Kingdom
Biochem Biophys Res Commun 267:356-61. 2000....
Structure-activity relationship study of steroidal and nonsteroidal inhibitors of the enzyme estrone sulfataseS Ahmed
School of Applied Chemistry, School of Life Sciences, Kingston University, Penrhyn Road, Kingston upon Thames, Surrey, KT1 2EE, United Kingdom
Biochem Biophys Res Commun 254:811-5. 1999..g., an inhibitor based upon trichloroethanol has been shown to possess 46% inhibition at 0.76mM)...
The use of the novel substrate-heme complex approach in the derivation of a representation of the active site of the enzyme cholesterol side chain cleavageS Ahmed
School of Chemical and Pharmaceutical Sciences, Kingston University, Penrhyn Road, Surrey, Kingston upon Thames, KT1 2EE, United Kingdom
Biochem Biophys Res Commun 274:821-4. 2000..Using the derived model, we have rationalised the inhibitory activity of a number of compounds including aminoglutethimide and pyridoglutethimide and the enantiomers of ketoconazole...
Folic acid prevents nitroglycerin-induced nitric oxide synthase dysfunction and nitrate tolerance: a human in vivo studyT Gori
Division of Cardiology, Department of Medicine, Mount Sinai Hospital, and the University of Toronto, Toronto, Canada
Circulation 104:1119-23. 2001..We hypothesize that the reduced bioavailability of tetrahydrobiopterin is involved in the pathogenesis of both phenomena. Our results confirm the view that oxidative stress contributes to nitrate tolerance...
Gleevec (STI571) influences metabolic enzyme activities and glucose carbon flow toward nucleic acid and fatty acid synthesis in myeloid tumor cellsJ Boren
Department of Biochemistry and Molecular Biology, Institut d'Investigacions Biomediques August Pi i Sunyer, University of Barcelona, Marti i Franques 1, Barcelona 08028, Spain
J Biol Chem 276:37747-53. 2001....
Hydrophobicity and functionality maps of farnesyltransferaseS Ahmed
Department of Biochemistry, , , Switzerland
J Mol Graph Model 19:307-17, 380-7. 2001..The functionality maps are also used to design a library of disubstituted indoles that might prevent the binding of the protein substrates...
An evolutionary approach for structure-based design of natural and non-natural peptidic ligandsN Budin
Department of Biochemistry, , Winterthurerstrasse 190, CH-8057, , Switzerland
Comb Chem High Throughput Screen 4:661-73. 2001..For farnesyltransferase, it is shown that electrostatic solvation is necessary for the correct design of peptidic inhibitors...
Abl inhibitor BMS354825 binding mode in Abelson kinase revealed by molecular docking studiesC Gambacorti-Passerini
Leukemia 19:1267-9. 2005
Effects of NOS inhibition on the cardiopulmonary system and brain microvascular markers after intermittent hypoxia in ratsG R Barer
Wolfson Research Centre, Institute for Ageing and Health, Newcastle General Hospital, Westgate Road, Newcastle upon Tyne NE4 6BE, UK
Brain Res 1098:196-203. 2006..However, whether cerebral effects are due to systemic hypertension or changes in cerebral nitric oxide production needs to be evaluated...
Arylpropanolamines: selective beta3 agonists arising from strategies to mitigate phase I metabolic transformationsW N Washburn
Bristol Myers Squibb Pharmaceutical Research Institute, PO Box 4000, Princeton, NJ 08543, USA
Bioorg Med Chem Lett 17:4290-6. 2007....
