Research Topics
| M S McQueneySummaryAffiliation: SmithKline Beecham Pharmaceuticals Country: USA Publications
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Detail Information
Publications
Autocatalytic activation of human cathepsin KM S McQueney
Department of Protein Biochemistry, SmithKline Beecham Pharmaceuticals, King of Prussia, Pennsylvania 19406, USA
J Biol Chem 272:13955-60. 1997..These results indicated that in vitro activation of the procathepsin K was an autocatalytic process...
Cynomolgus monkey (Macaca fascicularis) cathepsin K: cloning, expression, purification, and activationM S McQueney
Department of Protein Biochemistry, SmithKline Beecham Pharmaceuticals, King of Prussia, Pennsylvania, 19406, USA
Protein Expr Purif 14:387-94. 1998....
Potent dipeptidylketone inhibitors of the cysteine protease cathepsin KR W Marquis
Department of Medicinal Chemistry, SmithKline Beecham Pharmaceuticals, King of Prussia, PA 19406, USA
Bioorg Med Chem 7:581-8. 1999....
The crystal structure of human procathepsin KJ M LaLonde
Department of Structural Biology, SmithKline Beecham Pharmaceuticals, King of Prussia, Pennsylvania 19406, USA
Biochemistry 38:862-9. 1999..The structure of procathepsin K contributes to an understanding of the molecular basis of inhibition by the propeptide portion of the molecule and activation of this important member of the cysteine protease family...
Cyclic ketone inhibitors of the cysteine protease cathepsin KR W Marquis
Department of Medicinal Chemistry, GlaxoSmithKline, King of Prussia, Pennsylvania 19406, USA
J Med Chem 44:725-36. 2001..Epimerization issues associated with the labile alpha-amino ketone diastereomeric center contained within these inhibitor classes has proven to limit their utility despite promising pharmacokinetics displayed in both series of compounds...
Expression in Escherichia coli, refolding, and purification of human procathepsin K, an osteoclast-specific proteaseK J D'alessio
Department of Protein Biochemistry, SmithKline Beecham Pharmaceuticals, King of Prussia, Pennsylvania 19406, USA
Protein Expr Purif 15:213-20. 1999..This expression and refolding procedure yielded 50 mg of purified, glycosylation-free human procathepsin K from 1 liter of E. coli cell culture and enabled the determination of the structure of human procathepsin K at 2.6 A resolution...
Azepanone-based inhibitors of human and rat cathepsin KR W Marquis
Department of Medicinal Chemistry, GlaxoSmithKline, 709 Swedeland Road, King of Prussia, Pennsylvania 19406, USA
J Med Chem 44:1380-95. 2001....
cDNA sequence and characterization of the gene that encodes human myotrophin/V-1 protein, a mediator of cardiac hypertrophyK M Anderson
Department of Cardiovascular Pharmacology, SmithKline Beecham Pharmaceuticals, King of Prussia, PA 19406, USA
J Mol Cell Cardiol 31:705-19. 1999..We report the novel findings that myotrophin expression is elevated in ischemic hearts, and that myotrophin expression correlates positively with ventricular mass in a hypoxic rat model of induced right ventricular hypertrophy...
Potent and selective cathepsin L inhibitors do not inhibit human osteoclast resorption in vitroI E James
Departments of Bone and Cartilage Biology, Medicinal Chemistry, Protein Biochemistry, and Mechanistic Enzymology, SmithKline Beecham Pharmaceuticals, King of Prussia, Pennsylvania 19406, USA
J Biol Chem 276:11507-11. 2001..052 nm) and K (K(i) = 1.57 nm) was also active in both assays (IC(50) = 110 and 115 nm, respectively) These data confirm that cathepsin K and not cathepsin L is the major protease responsible for human osteoclastic bone resorption...
Design of potent and selective human cathepsin K inhibitors that span the active siteS K Thompson
Department of Medicinal Chemistry, SmithKline Beecham Pharmaceuticals, King of Prussia, PA 19406, USA
Proc Natl Acad Sci U S A 94:14249-54. 1997..Expansion of these inhibitor concepts can be envisioned for the many other cysteine proteases implicated for therapeutic intervention...
An integrated ten-pump, eight-channel parallel LC/MS system for automated high-throughput analysis of proteinsB Feng
Department of Gene Expression and Protein Biochemistry, Discovery Research, GlaxoSmithKline, King of Prussia, Pennsylvania 19406, USA
Anal Chem 73:5691-7. 2001..Using this off-line approach, it is practical to fully characterize protein-containing fractions from column chromatography with an overall analytical throughput of 1 min/protein sample with minimum operator involvement...
