Discovery of inhibitors of the channel-activating protease prostasin (CAP1/PRSS8) utilizing structure-based design

Bioorganic and Medicinal Chemistry Letters

Volumn 18, Issue 22, 2008, Pages 5895-5899

  Tully, David C ^a   Vidal, Agnès ^a   Chatterjee, Arnab K ^a   Williams, Jennifer A ^a   Roberts, Michael J ^a   Petrassi, H Michael ^a   Spraggon, Glen ^a   Bursulaya, Badry ^a   Pacoma, Reynand ^a   Shipway, Aaron ^a   Schumacher, Andrew M ^a   Danahay, Henry ^b   Harris, Jennifer L ^a  

^a GENOMICS INSTITUTE OF THE NOVARTIS RESEARCH FOUNDATION   (United States)

^b NOVARTIS INSTITUTES FOR BIOMEDICAL RESEARCH   (United States)

Author keywords

Channel activating protease; ENaC activation; hCAP; Ketoheterocycle inhibitor; Peptidomimetic; Prostasin; PRSS8

Indexed keywords

ENZYME INHIBITOR; PROSTASIN; PROTEINASE;

ARTICLE; CRYSTAL STRUCTURE; DRUG DESIGN; ENZYME ACTIVE SITE; ENZYME SPECIFICITY; ENZYME SUBSTRATE; X RAY CRYSTALLOGRAPHY;

COMBINATORIAL CHEMISTRY TECHNIQUES; CRYSTALLOGRAPHY, X-RAY; MOLECULAR MIMICRY; MOLECULAR STRUCTURE; PROTEIN CONFORMATION; SERINE ENDOPEPTIDASES; SERINE PROTEINASE INHIBITORS; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 55249094543     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2008.08.029     Document Type: Article

References (14)

1. Yu J.X., Chao L., and Chao J. J. Biol. Chem. 269 (1994) 18843
2. Shipway A., Danahay H., Williams J.A., Tully D.C., Backes B.J., and Harris J.L. Biochem. Biophys. Res. Commun. 324 (2004) 953
3. Adachi M., Kitamura K., Miyoshi T., Narikiyo T., Iwashita K., Shiraishi N., Nonoguchi H., and Tomita K. J. Am. Soc. Nephrol. 12 (2001) 1114
4. Donaldson S.H., Hirsh A., Li D.C., Holloway G., Chao J., Boucher R.C., and Gabriel S.E. J. Biol. Chem. 277 (2002) 8338
5. Tong Z., Illek B., Bhagwandin V.J., Verghese G.M., and Caughey G.H. Am. J. Physiol. Lung. Cell. Mol. Physiol. 287 (2004) L928
6. McKenna E.E., Luke C.J., Frizzell R.A., Kleyman T.R., and Pilewski J.M. Am. J. Physiol. Lung. Cell. Mol. Physiol. 294 (2008) L932
7. Edwards P.D., Meyer Jr. E.F., Vijayalakshmi J., Tuthill P.A., Andisik D.A., Gomes B., and Strimpler A. J. Am. Chem. Soc. 114 (1992) 1854
8. Edwards P.D., Wolanin D.J., Andisik D.W., and Davis M.W. J. Med. Chem. 38 (1995) 76
9. Edwards P.D., Zottola M.A., Davis M.W., Williams J., and Tuthill P.A. J. Med. Chem. 38 (1995) 3972
10. Costanzo M.J., Maryanoff B.E., Hecker L.R., Schott M.R., Yabut S.C., Zhang H.-C., Andrade-Gordon P., Kauffman J.A., Lewis J.M., Krishnan R., and Tulinsky A. J. Med. Chem. 39 (1996) 3039
11. Costanzo M.J., Almond Jr. H.R., Hecker L.R., Schott M.R., Yabut S.C., Zhang H.-C., Andrade-Gordon P., Corcoran T.W., Giardino E.C., Kauffman J.A., Lewis J.M., deGaravilla L., Haertlein B.J., and Maryanoff B.E. J. Med. Chem. 48 (2005) 1984
12. A comprehensive review on the subject of α-ketoheterocycle protease inhibitors:. Maryanoff B.E., and Costanzo M.J. Bioorg. Med. Chem. 16 (2008) 1562
13. Matthews J.H., Krishnan R., Costanzo M.J., Maryanoff B.E., and Tulinsky A. Biophys. J. 71 (1996) 2830
14. Recacha R., Costanzo M.J., Maryanoff B.E., Carson M., DeLucas L.J., and Chattopadhyay D. Acta Crystallogr., Sect. D: Biol. Crystallogr. 56 (2000) 1395