Application of conformationally restricted peptidomimetics to modeling the bound conformation of peptide antagonists with the IL-1 receptor

Letters in Peptide Science - Tập 5 - Trang 93-100 - 1998
Gary A. Flynn1, Ann L. Akeson2, Ram Dharanipragada2, Michael J. Genin2, J. Antony Malikayil2, Richard Pottorf2, Jeffery S. Sabol2, Herman Schreuder2, Ron Tomlinson2, Phil Waid2, Ron Barrett3, Jeff Jacobs3, Steve Yanofsky3
1Selectide Corporation, Tucson, U.S.A.
2Hoechst Marion Roussel Inc., Cincinnati, U.S.A.
3Affymax Research Institute, Palo Alto, U.S.A.

Tóm tắt

A collection of complementary peptide caricatures that closely mimic low-energy (presumably highly populated) conformations of amino acids of interest would constitute a valuable tool set to study the interactions of small peptide ligands with their biological targets. Our general strategy for the design, synthesis and application of peptidomimetics is presented. An illustration of how structural information from mimetics combined with cutting edge biophysical data can be used to derive a model for the bound conformation of an 11-mer peptide antagonist with the IL-1 receptor is given.

Tài liệu tham khảo

For a review see: Liskamp, R.M.J., Recl. Trav. Chim. Pays-Bas, 113 (1994) 1. Flynn, G.A., French, J.F. and Dage, R.C., In Laragh, J.H. and Brenner, B.M. (Eds.) Hypertension: Pathophysiology, Diagnosis and Management, 2nd ed., Raven Press, New York, NY, 1995, pp. 3099–3114. Roterman, I.K., Lambert, M.H., Gibson, K.D. and Sheraga, H.A., J. Biomol. Struct. Dyn., 7 (1989) 421. Flynn, G.A., Beight, D.W., Mehdi, S., Koehl, J.R., Giroux, E.L., French, J.F., Hake, P.W. and Dage, R.C., J. Med. Chem., 36 (1993) 2420. Flynn, G.A., Burkholder, T.P., Huber, E.W. and Bey, P., Bioorg. Med. Chem. Lett., 1 (1991) 309. Warshawsky, A.M., Flynn, G.A., Koehl, J.R. and Mehdi, S., Bioorg. Med. Chem. Lett., 6 (1996) 957. Burkholder, T.P., Huber, E.W. and Flynn, G.A., Bioorg. Med. Chem. Lett., 3 (1993) 231. Moeller, K.D. and Rothfus, S.L., et al., Tetrahedron Lett., 33 (1992) 2913. Moeller, K.D. and Hanau, C.E., Tetrahedron Lett., 33 (1992) 6041. Oinuma, H., et al., 209th ACS National Meeting, Anaheim, CA, U.S.A., April 2–6, 1995, Medi Poster 161. Simpkins, L.M., et al., 210th ACS National Meeting, Chicago, IL, U.S.A., August 20–24, 1995, Medi Poster 64. Waid, P.P., Flynn, G.A., Huber, E.W. and Sbaol, J., Tetrahedron Lett., 37 (1996) 4091. Evans, D.A., Britton, T.C., Ellman, J.A. and Dorow, R.L., J. Am. Chem. Soc., 112 (1990) 4011. Kazmierski, W.M., Urbanczyk-Lipkowska, Z. and Hruby, V.J., J. Org. Chem., 59 (1994) 1789. Dharanipragada, R., Nicolas, E., Toth, G. and Hruby, V.J., Tetrahedron Lett., 30 (1989) 6841. Borteju, L.W., Werner, K. and Hruby, V.J., Tetrahedron Lett., 33 (1992) 7491. Li, G., Patel, E. and Hruby, V.J., Tetrahedron Lett., 35 (1994) 2301. DiMaio, J. and Belleau, B., J. Chem. Soc. Perkin Trans I (1989) 1687. Liao, S. and Hruby, V.J., Tetrahedron Lett., 37 (1996) 1563. Zydowsky, T.M., Dellaria Jr., J.F. and Nellans, H.N., J. Org. Chem., 53 (1988) 5607. Kojima, Y., Yamashita, T., Washizawa, M. and Ohsuka, A., Makromol. Rapid Commun., 10 (1989) 121. Seebach, D., Boes, M., Naef, R. and Scheiaer, W.B., J. Am. Chem. Soc., 105 (1983) 5390. Hinds, M.G., Richards, N.J. and robinson, J. A., J. Chem. Soc., Chem. Commun. (1988) 1447. Genin, M.J. and Johnson, R.L., J. Am. Chem. Soc., 114 (1992) 8778. Yanofsky, S.D., Baldwin, D.N., Butler, J.H., Holden, F.R., Jacobs, J.W., Balasubramanian, Chinn, J.P., Cwirla, S.E., Peters-Bhatt, E., Whitehorse, E.A., Tate, E.H., Akeson, A., Bowlin, T.L., Dowere, W.J. and Barrett, K.W., Proc. Natl. Acad. Sci. USA, 93 (1996) 7381. Evans, R.J., Bray, J., Childs, J.D., Vigers, G.P.A., Brandhuber, B.J., Skalicky, J.J., Thompson, R.C. and Eisenberg, S.P., J. Biol. Chem., 270 (1995) 11477. Schreuder, H., Tardif, C., Trump-Kalimeyer, S., Sofflentini, A., Sarubbi, E., Akeson, A., Bowlin, T., Yanofsky, S. and Barrett, R.W., Nature, 386 (1997) 184. Bovey, P., Peptidomimetics and Small Molecule Design, IBC Conference, Philadelphia, PA, U.S.A., March 10–12, 1997.