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C A Janson

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Articles 48
Citations 1080
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Recent Articles
1.
Head M, Ryan M, Lee D, Feng Y, Janson C, Concha N, et al.
J Comput Aided Mol Des . 2002 Aug; 15(12):1105-17. PMID: 12160093
Structure-based design of a combinatorial array was carried out in order to identify non-peptidic thiomethylketone inhibitors of caspases 3 and 8. Five compounds from the designed array were active against...
2.
Qiu X, Janson C, Smith W, Green S, McDevitt P, Johanson K, et al.
Protein Sci . 2001 Sep; 10(10):2008-16. PMID: 11567092
SB-219383 and its analogues are a class of potent and specific inhibitors of bacterial tyrosyl-tRNA synthetases. Crystal structures of these inhibitors have been solved in complex with the tyrosyl-tRNA synthetase...
3.
Seefeld M, Miller W, Newlander K, BURGESS W, Payne D, Rittenhouse S, et al.
Bioorg Med Chem Lett . 2001 Aug; 11(17):2241-4. PMID: 11527706
An SAR study of a screening lead has led to the identification of 2,9-disubstituted 1,2,3,4-tetrahydropyrido[3,4-b]indoles as inhibitors of Staphylococcus aureus enoyl acyl carrier protein reductase (FabI).
4.
Heerding D, Chan G, DeWolf W, Fosberry A, Janson C, Jaworski D, et al.
Bioorg Med Chem Lett . 2001 Aug; 11(16):2061-5. PMID: 11514139
1,4-Disubstituted imidazole inhibitors of Staphylococcus aureus and Escherichia coli enoyl acyl carrier protein reductase (FabI) have been identified. Crystal structure data shows the inhibitor 1 bound in the enzyme active...
5.
Marquis R, Ru Y, LoCastro S, Zeng J, Yamashita D, Oh H, et al.
J Med Chem . 2001 Apr; 44(9):1380-95. PMID: 11311061
The synthesis, in vitro activities, and pharmacokinetics of a series of azepanone-based inhibitors of the cysteine protease cathepsin K (EC 3.4.22.38) are described. These compounds show improved configurational stability of...
6.
Marquis R, Ru Y, Zeng J, Trout R, LoCastro S, Gribble A, et al.
J Med Chem . 2001 Mar; 44(5):725-36. PMID: 11262083
Cathepsin K (EC 3.4.22.38), a cysteine protease of the papain superfamily, is predominantly expressed in osteoclasts and has been postulated as a target for the treatment of osteoporosis. Crystallographic and...
7.
Qiu X, Janson C, Smith W, Head M, Lonsdale J, Konstantinidis A
J Mol Biol . 2001 Mar; 307(1):341-56. PMID: 11243824
beta-Ketoacyl-acyl carrier protein synthase III (FabH) is a condensing enzyme that plays central roles in fatty acid biosynthesis. Three-dimensional structures of E. coli FabH in the presence and absence of...
8.
Lee D, Long S, Adams J, Chan G, Vaidya K, Francis T, et al.
J Biol Chem . 2000 May; 275(21):16007-14. PMID: 10821855
Caspases have been strongly implicated to play an essential role in apoptosis. A critical question regarding the role(s) of these proteases is whether selective inhibition of an effector caspase(s) will...
9.
Janson C, Konstantinidis A, Lonsdale J, Qiu X
Acta Crystallogr D Biol Crystallogr . 2000 May; 56(Pt 6):747-8. PMID: 10818351
beta-Ketoacyl-acyl carrier protein (ACP) synthase III (FabH) is a condensing enzyme active in the fatty-acid biosynthesis pathway of bacteria. The enzymes of this pathway provide a set of targets for...
10.
Concha N, Janson C, Rowling P, Pearson S, Cheever C, Clarke B, et al.
Biochemistry . 2000 Apr; 39(15):4288-98. PMID: 10757977
Metallo beta-lactamase enzymes confer antibiotic resistance to bacteria by catalyzing the hydrolysis of beta-lactam antibiotics. This relatively new form of resistance is spreading unchallenged as there is a current lack...