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Structure based design of 4-(3-aminomethylphenyl)piperidinyl-1-amides: novel, potent, selective, and orally bioavailable inhibitors of βII tryptase

Autor: Michael Gardyan, Mathew Rose M, Jane Davidson, Joseph Romano, Alain Dupuy, Aldous Suzanne C, Jennifer Kwong, Sam S. Rebello, Jennifer Cairns, Odessa Giardino, Yongyi Luo, Sébastien Maignan, Andrew David Morley, Clive Mccarthy, Joseph T. Tsay, Darren Engers, Guyan Liang, Houille Olivier, Julian Levell, Pribish James R, Jean-Pierre Guilloteau, Garry Fenton, Simon Watson, Trevor K.P. Harrison, Peter C. Astles, Liduo Shen, Mark Czekaj, Gregory H. Merriman, Keith Sides, Pauls Henry W, Keith Smith, Jie Wang, Heng-Keang Lim, Paul R. Eastwood, Brian Whiteley

Publikováno v: Bioorganic & Medicinal Chemistry. 13:2859-2872

Tryptase is a serine protease found almost exclusively in mast cells. It has trypsin-like specificity, favoring cleavage of substrates with an arginine (or lysine) at the P1 position, and has optimal catalytic activity at neutral pH. Current evidence

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::abef3005a193e13656a4c8e845e1b9b8
https://doi.org/10.1016/j.bmc.2005.02.014

Dimerization of β-tryptase inhibitors, does it work for both basic and neutral P1 groups?

Autor: Xin Chen, Eric W. MacMillan, Guyan Liang, Isabelle Morize, Yong Gong, Yong Mi Choi-Sledeski, Joseph T. Tsay, David J. Aldous, Berndt Kulitzscher, Jennifer Cairns, Keith Sides, Pauls Henry W

Publikováno v: Bioorganicmedicinal chemistry letters. 22(9)

The tetrameric folding of β-tryptase and the pair-wise distribution of its substrate binding sites offer a unique opportunity for development of inhibitors that span two adjacent binding sites. A series of dimeric inhibitors with two basic P1 moieti

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::31394b151f2999474eaac65e9c8c912d
https://pubmed.ncbi.nlm.nih.gov/22483389

Contents, Vol. 94, 1991

Autor: Graham S. LeGros, Hiroshi Yamakawa, K. Takatsu, Ratko Djukanovic, P.G. Holt, J. Bujanowski-Weber, P. Oehme, S. Bianchj, William Roche, I. Knöller, G. Delespesse, Toru Ando, Reinhold Penner, D. Macchia, R. Djukanovic, George W. Ward, Thomas Bieber, T. Furitsu, Makoto Dohi, Susan M. MacDonald, Martin D. Chapman, F. Chavarria, R. Robert Schellenberg, Michiko Haida, Makoto Nogami, John R. Brashler, J. Brom, Pascal Chanez, A. Ciccarelli, T.D. Whalley, M.J. Carmona, E. Saito, Mamoru Ito, H. Behrendt, W. Zachgo, Gabriele Zwadlo-Klarwasser, Philip J. Thompson, Sylvia Miescher, N.P. Siemensma, A. de Paulis, G. Schultze-Werninghaus, J.-P. Kinet, B.D. Gomperts, Takeo Juji, Ikuo Akutsu, Richard J. Simpson, S. Wilson, T.H. Lee, Suhad El-Lati, Bernhard Przybilla, J. Oliver, Sesha Reddigari, Monique Vogel, Koki Takahashi, Thomas Iff, L. Mugnai, E. Neher, Nathalie Paul-Eugène, Ph. Lassalle, Takeshi Fukuda, Dean D. Metcalfe, V. Lagente, C.E. O’Neil, Go Matsuzaki, C. McMenamin, Jordan N. Fink, G. Burow, Ch. Lemmermann, Ch. Schweiger, H. Wagner, K. Kurihara, D.R. Springall, Karin Pettenburger, A. Capron, H.Y.A. Lau, R. Wahl, G.J. Gleich, K. Rother, Shigeru Takafuji, W.R. Roche, Kurt Blaser, F. Gambassi, A. Pistelli, M. Bubak, Andrew F. Walls, Jeffrey M. Drazen, S.J. Lane, Johann-Christian Virchow, Akio Mori, J.M. Polak, Dietrich Kraft, Hans L. Spiegelberg, L. Lipponer, Friederike von zur Mühlen, R. zur Strassen, Rihoux Jean-Pierre, Susanne Spitzauer, Werner J. Pichler, Karen Britten, M. Schon-Hegrad, Barbara K. Stout, John Wilson, Hirokazu Okudaira, Otto Scheiner, Mitsuko Kondo, Akira Ishii, Richard Sporik, Daniel Weinreich, M. Keating, W. Dorsch, Manel Jordana, Ch.H. Heusser, Ingrid Enander, Massimo Triggiani, T. Ishizaka, Colin J. Sanderson, Dieter Vieluf, Stephanie A. Shore, J. Anrather, S. Terrados, Claus Bachert, Rosa M. Ten, E.W. Rauterberg, E. Masini, H. Rumpold, Jean Yves Lacoste, T.H.W. Lillie, K. Ohno, Alison M. Campbell, E. Gutierrez, F.L. Pearce, Stephan C. Bischoff, R. Suau, Miguel Blanca, P.H. Howarth, P.K. Jeffery, Robert L. Barker, E. Perez, M. Pfenning, Marshall Plaut, Piotr Kuna, T. Abe, H. Rotermund, Michael A. Lett-Brown, Herbert G. Johnson, Thomas Brunner, C. Ra, U. Ganzer, N. Hyslop, Kazuhiko Akiyoshi, Alain L. de Weck, J. Bews, A. Hartnell, J. Dry, K. Nosbüsch, Rafeul Alam, G. Le Gros, V. Brinkmann, Jacqueline M. Langdon, B. Thomas, P. Heap, Corinne Petit-Frère, A.G. Fernández, Wolfgang Schmutzler, Gianni Marone, Matsunobu Suko, R.W. Gristwood, D. Kraft, G.M. Walsh, A.G. Palma-Carlos, B. Bradley, N.S. Sakaguchi, J.M. Vega, O.-H. Wilhelms, R. Wiewrodt, A. Brini, Stephen R. Durham, M. Lupini, M.A. Reed, Thierry Maisonnet, A. Witzel, Peter J. Barnes, Ch. Brander, Lawrence M. Lichtenstein, A. Koffer, Y. Delneste, Laura Palma-Carlos, Jennifer Cairns, T. Brunnee, Elliott Homer, Diana J. Quint, F. Bettens, Monique Capron, Sohei Makino, Luanda Beck, T. Imai, Takayuki Ohtoshi, A. Akasawa, Lore Koller, Yoji Iikura, Naohiro Watanabe, Ahuva Nissim, J.W. Coleman, A. Ohgimi, D. Befus, J.R. Wilkinson, H. Küster, T. Katsunuma, Ch. Ebner, K.J. Turner, M.P. Piccinni, F. Ledermann, Michael Breitenbach, Bradley J. Undem, A.B. Kay, John E. Salvaggio, Carvalho de Sousa, S.T. Holgate, B. Girn, P. Berga, S. Bent, Gerald J. Gleich, Arnold S. Kirshenbaum, P.B. Boulos, Yoshitaka Ino, M. Breitenbach, R. Rathsack, May Azzawi, Sun Ying, Philippe Godard, J.H. Widdicombe, Rudolf Valenta, Christopher Corrigan, S. Romagnani, D.M. Kemeny, Bernard Dugas, Samuel B. Lehrer, Y. Churcher, John Gordon, C. Brom, F. Leynadier, Gert Kunkel, Gerard Cox, B.F. Weber, D. Diaz-Sanchez, Shinji Motojima, J.W. Wilson, Pieter L.B. Bruijnzeel, P.F. Mannaioni, K. Britten, Allen P. Kaplan, Yutaka Morita, K. Ishida, Erika Jensen-Jarolim, Jack Gauldie, Fiona R. Lake, S. Raspanti, Andrew Grant, R. Fadel, S. Dunnette, Jean Bousquet, Ivan Aebischer, Thomas A.E. Platts-Mills, T. Wyss, Richard D. O’Connor, Larry D. Ward, A.G. Morris, Clemens A. Dahinden, Toshifumi Yuuki, P. Parronchi, Hiroyuki Mochizuki, Gail M. McNutt, D.C. Reason, Martin Krieger, Lawrence E. Gelber, Naoki Inagaki, E. Kilchherr, Elisabeth Boichot, Qiu Gang, F. Gabl, Alec H. Sehon, J.V. Collins, Shiro Kasuya, J. Blomgren, Bernadette Pignol, Motohiro Ebisawa, N. Sakaguchi, Jacalyn H. Pierce, U. Blank, Fu-Tong Liu, Robert A. Seder, R. Hilger, Richard P. Bransford, M. Linssen, Jörg Kleine-Tebbe, P.D. Pare, Kazuhiko Yamamoto, Jean Michel Mencia-Huerta, Michael K. Bach, Pierre Braquet, J. Salvaggio, Reuben J.M. Falkoff, R. Merget, J. Hards, B.J. Holt, D. Strickland, P.E.R. Tatham, A.B. Tonnel, H. Saito, François-B. Michel, K. Akimoto, Jerry Dolovich, Brian M. Greenlee, Carl G. A. Persson, Anne Kagey-Sobotka, Tim R. Mosmann, Zelig Eshhar, N. Wallen, Maria Baeza, A.J. Wardlaw, Peter H. Howarth, Robin N. Poston, W. König, R.C. Benyon, M. Lopez, D. Mijic, E. Jarolim, William E. Paul, John P. Caulfield, B. Kunz, Milton A. Martins, Yasushi Okumura, J. Knöller, R. Ciriilo, K. Nieber, Geoffrey A. Stewart, Allen C. Myers, Zami Ben-Sasson, U. Hauser, M. G. Di Bello, Michael Duchêne, C. Baumgarten, C.J. Sanderson, Koji Ito, R. Valenta, M.-H. Jouvin, Menachem Rottem, F. Carswell, A. Miranda, K.R. Tainsh, Kimm J. Hamann, Judah A. Denburg, K. Wagner, Martin K. Church, Qutayba Hamid, O. Mejan, Johannes Ring, J. Fernandez, L. Juhlin, Kiyoshi Takatsu, Martin E. Sanders, Peter W. Heymann, C.E. Reed, P. Wentz-Murtha, Fred D. Finkelman, J. Llupiá, Helmut Rumpold, Stephen T. Holgate, Conceição B. Santos, G.M. Hänsch, W.L. Liu, Christoph Walker, M. Ricci, Ph. Gosset, E. Maggi, J. Wilson, R. Moqbel, Beda M. Stadler

Publikováno v: International Archives of Allergy and Immunology. 94:1-8

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::29ab4b881d1f9426d48a55e3e57a2743
https://doi.org/10.1159/000235316

Biographical Sketch of Dr. Alec H. Sehon

Autor: Matsunobu Suko, R.W. Gristwood, A.G. Palma-Carlos, T.H.W. Lillie, K. Ohno, R. Wiewrodt, K. Nosbüsch, Jacqueline M. Langdon, A. Brini, Zelig Eshhar, E. Kilchherr, V. Lagente, C.E. O’Neil, T. Katsunuma, Jean Michel Mencia-Huerta, M. Lopez, Michael K. Bach, D. Mijic, E. Jarolim, F.L. Pearce, E. Perez, Beda M. Stadler, Pierre Braquet, E. Saito, Mamoru Ito, H. Behrendt, N. Wallen, Maria Baeza, A.J. Wardlaw, Ch. Lemmermann, Ch. Schweiger, Bernadette Pignol, A. de Paulis, J. Salvaggio, Reuben J.M. Falkoff, J. Hards, William E. Paul, B.J. Holt, P. Berga, R. Djukanovic, Philip J. Thompson, Sylvia Miescher, N.P. Siemensma, Graham S. LeGros, Hiroshi Yamakawa, Yoshitaka Ino, M. Breitenbach, D. Strickland, K. Wagner, Martin K. Church, B. Bradley, Gert Kunkel, Gerard Cox, John P. Caulfield, Milton A. Martins, Yasushi Okumura, Daniel Weinreich, C.E. Reed, M.A. Reed, Thierry Maisonnet, Sesha Reddigari, Monique Vogel, Philippe Godard, J.H. Widdicombe, Robert A. Seder, F. Gabl, Christopher Corrigan, S. Romagnani, J.V. Collins, Jacalyn H. Pierce, O. Mejan, J. Fernandez, Fred D. Finkelman, J. Llupiá, O.-H. Wilhelms, H. Saito, François-B. Michel, A. Witzel, Jean Bousquet, Ivan Aebischer, Lawrence E. Gelber, Naoki Inagaki, Fu-Tong Liu, Thomas A.E. Platts-Mills, T. Wyss, D.M. Kemeny, Elisabeth Boichot, T. Imai, Y. Delneste, Ch. Brander, Stephanie A. Shore, John R. Brashler, Wolfgang Schmutzler, Richard P. Bransford, Fiona R. Lake, Ingrid Enander, W. Zachgo, Gabriele Zwadlo-Klarwasser, S. Terrados, Jennifer Cairns, Rosa M. Ten, R.C. Benyon, J.W. Coleman, Bernard Dugas, Samuel B. Lehrer, Y. Churcher, Shiro Kasuya, Takayuki Ohtoshi, G. Le Gros, D. Diaz-Sanchez, A.B. Tonnel, J. Brom, Pascal Chanez, J. Blomgren, John Gordon, P. Heap, M. Linssen, Jörg Kleine-Tebbe, Manel Jordana, Ch.H. Heusser, K. Akimoto, Jerry Dolovich, T. Ishizaka, Ratko Djukanovic, I. Knöller, Thomas Bieber, Peter H. Howarth, Helmut Rumpold, H. Rumpold, Motohiro Ebisawa, Jean Yves Lacoste, Gianni Marone, P.G. Holt, Pieter L.B. Bruijnzeel, Massimo Triggiani, Karen Britten, D.C. Reason, N. Sakaguchi, N.S. Sakaguchi, Ikuo Akutsu, G. Schultze-Werninghaus, R. Valenta, U. Blank, J.M. Vega, F. Leynadier, C. Ra, Bernhard Przybilla, K. Takatsu, Robin N. Poston, Larry D. Ward, P.K. Jeffery, Stephen R. Durham, J. Bujanowski-Weber, Nathalie Paul-Eugène, J. Dry, E.W. Rauterberg, B. Kunz, Christoph Walker, Richard J. Simpson, S. Wilson, V. Brinkmann, Ph. Lassalle, G. Burow, P.D. Pare, P. Oehme, Rafeul Alam, J. Knöller, R. Ciriilo, Conceição B. Santos, W. König, S. Bianchj, Allen C. Myers, K.R. Tainsh, Thomas Iff, E. Maggi, A. Miranda, T.D. Whalley, William Roche, Kimm J. Hamann, Lawrence M. Lichtenstein, Herbert G. Johnson, Kazuhiko Akiyoshi, Allen P. Kaplan, G. Delespesse, M.J. Carmona, H.Y.A. Lau, Kazuhiko Yamamoto, C. McMenamin, J. Wilson, Peter J. Barnes, Laura Palma-Carlos, A. Akasawa, G.M. Walsh, A. Capron, Toru Ando, W.R. Roche, Qiu Gang, Andrew F. Walls, Monique Capron, Sohei Makino, M. Lupini, Luanda Beck, J. Oliver, C. Baumgarten, L. Mugnai, C.J. Sanderson, Naohiro Watanabe, L. Lipponer, Alec H. Sehon, T. Furitsu, A. Ohgimi, Makoto Dohi, T. Brunnee, Elliott Homer, Diana J. Quint, A. Koffer, Friederike von zur Mühlen, R. Moqbel, Bradley J. Undem, Barbara K. Stout, Arnold S. Kirshenbaum, P.B. Boulos, Judah A. Denburg, M.-H. Jouvin, Werner J. Pichler, Shigeru Takafuji, M. Schon-Hegrad, Michael Breitenbach, G.M. Hänsch, Johannes Ring, J. Anrather, Robert L. Barker, Reinhold Penner, Otto Scheiner, L. Juhlin, Johann-Christian Virchow, Hirokazu Okudaira, E. Masini, S. Dunnette, Gerald J. Gleich, E. Gutierrez, Marshall Plaut, K. Nieber, F. Carswell, Piotr Kuna, R. Hilger, H. Küster, Clemens A. Dahinden, D. Macchia, W.L. Liu, M.P. Piccinni, Colin J. Sanderson, F. Gambassi, Jeffrey M. Drazen, Geoffrey A. Stewart, R. Wahl, G.J. Gleich, R. zur Strassen, R. Merget, M. Ricci, Menachem Rottem, John E. Salvaggio, Qutayba Hamid, Go Matsuzaki, Peter W. Heymann, Martin D. Chapman, P.E.R. Tatham, F. Chavarria, P. Wentz-Murtha, H. Wagner, S.J. Lane, Ph. Gosset, Akio Mori, K. Rother, Dietrich Kraft, Hans L. Spiegelberg, Kurt Blaser, A. Pistelli, Koki Takahashi, Kiyoshi Takatsu, D. Kraft, Martin E. Sanders, R. Suau, Stephen T. Holgate, T. Abe, Thomas Brunner, John Wilson, N. Hyslop, Alain L. de Weck, A. Hartnell, Corinne Petit-Frère, Zami Ben-Sasson, F. Bettens, Lore Koller, Yoji Iikura, U. Hauser, May Azzawi, Yutaka Morita, K. Ishida, M. G. Di Bello, Michael Duchêne, Koji Ito, Martin Krieger, D.R. Springall, Karin Pettenburger, J.M. Polak, Ahuva Nissim, Susanne Spitzauer, D. Befus, J.R. Wilkinson, Ch. Ebner, K.J. Turner, M. Bubak, F. Ledermann, Akira Ishii, Richard Sporik, M. Keating, A.B. Kay, Carvalho de Sousa, S.T. Holgate, B. Girn, S. Bent, Dieter Vieluf, Rihoux Jean-Pierre, W. Dorsch, Mitsuko Kondo, Claus Bachert, T.H. Lee, Suhad El-Lati, George W. Ward, E. Neher, R. Robert Schellenberg, Michiko Haida, Makoto Nogami, Brian M. Greenlee, Carl G. A. Persson, Anne Kagey-Sobotka, M. Pfenning, Dean D. Metcalfe, B.F. Weber, H. Rotermund, Shinji Motojima, J.W. Wilson, Tim R. Mosmann, Michael A. Lett-Brown, K. Kurihara, P.F. Mannaioni, Erika Jensen-Jarolim, Jack Gauldie, S. Raspanti, Andrew Grant, U. Ganzer, R. Fadel, R. Rathsack, Susan M. MacDonald, Toshifumi Yuuki, Sun Ying, B. Thomas, Rudolf Valenta, P. Parronchi, A. Ciccarelli, J.-P. Kinet, B.D. Gomperts, Takeo Juji, C. Brom, Hiroyuki Mochizuki, Gail M. McNutt, Alison M. Campbell, Takeshi Fukuda, K. Britten, Jordan N. Fink, J. Bews, Richard D. O’Connor, Stephan C. Bischoff, Miguel Blanca, P.H. Howarth, A.G. Morris, A.G. Fernández

Publikováno v: International Archives of Allergy and Immunology. 94:9-10

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::07efb71f8c64b25b7fbfe3c81a32f441
https://doi.org/10.1159/000235317