Zobrazeno 1 - 10
of 11
pro vyhledávání: '"Ermenegilda McCauley"'
Autor:
Malcolm MacCoss, John A. Schmidt, Linda A. Egger, Linus S. Lin, Jin Cao, Richard A. Mumford, Gail Van Riper, William K. Hagmann, Thomas J. Lanza, Usha Kidambi, Ermenegilda McCauley
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 12:133-136
N-(3,5-Dichlorophenylsulfonyl)-(R)-thioprolyl biarylalanine 10a has been identified as a potent and specific antagonist of the α4β1 integrin. Altering the configuration of thioproline from R to S led to a series of dual antagonists of α4β1 and α
Autor:
David A. Geller, Ermenegilda McCauley, Michael J. Tocci, Timothy R. Billiar, Malcolm MacCoss, Andreas K. Nussler, Stephan K. Grant, Kenny K. Wong, Jimmy R. Calaycay, Theresa M. Kelly, Jeffrey R. Weidner, Patrick R. Griffin, S.M. Raju, Tracey Klatt, Shrenik K. Shah, Hongbo Qi, Richard A. Mumford, Gloria C. Wolfe, Hollis R. Williams, John A. Schmidt, Nancy I. Hutchinson, Karen L. MacNaul
Publikováno v:
Journal of Biological Chemistry. 271:28212-28219
Recombinant human inducible nitric-oxide synthase (rH-iNOS) was expressed in the baculovirus system and purified by a novel immunoaffinity column. rH-iNOS and its native counterpart from cytokine-stimulated primary hepatocytes exhibited similar molec
Autor:
Linus S. Lin, Thomas J. Lanza, John A. Schmidt, Richard A. Mumford, Xinchun Tong, Laurie A. Castonguay, Theodore M. Kamenecka, Linda A. Egger, Gail Van Riper, Malcolm MacCoss, William K. Hagmann, Ermenegilda McCauley
Publikováno v:
Bioorganicmedicinal chemistry letters. 14(9)
We have designed and synthesized a series of heterocyclic bioisosteres for an anilide based on molecular modeling. Excellent potency was retained in the benzoxazole and the benzimidazole derivatives, where a hydrogen bond acceptor is appropriately po
Autor:
Linda A. Egger, Ermenegilda McCauley, George A. Doherty, Richard A. Mumford, Sharon Tong, Malcolm MacCoss, William K. Hagmann, Ginger X. Yang, Edite Borges, Linda L. Chang, Usha Kidambi, Gail Van Riper, John A. Schmidt
Publikováno v:
Bioorganicmedicinal chemistry letters. 12(11)
A series of substituted tetrahydrofuroyl-1-phenylalanine derivatives was prepared and evaluated as VLA-4 antagonists. Substitution of the alpha carbon of the tetrahydrofuran with aryl groups increased the specificity for VLA-4 versus alpha(4)beta(7)
Autor:
George A. Doherty, Richard A. Mumford, Theodore M. Kamenecka, William K. Hagmann, Sharon Tong, Ermenegilda McCauley, Gail Van Riper
Publikováno v:
Bioorganicmedicinal chemistry letters. 12(5)
A series of N-arylated phenylalanine derivatives has been synthesized and has been shown to be potent inhibitors of the integrin VLA-4. N-phenyl and N-heteroaryl derivatives with hydrogen bond acceptors in the meta position demonstrated low nanomolar
Autor:
Thomas J. Lanza, Ralph A. Stearns, Theodore M. Kamenecka, Adria Colletti, John A. Schmidt, Linda A. Egger, Plato A. Magriotis, Gail Van Riper, Kathryn A. Lyons, Malcolm MacCoss, Richard A. Mumford, Xinchun Tong, Stella H. Vincent, Ermenegilda McCauley, Stephen E. de Laszlo, Ihor E. Kopka, Judy Fenyk-Melody, Yohannes Teffera, William K. Hagmann, David N. Young, Philippe L. Durette, Linus S. Lin, Usha Kidambi
Publikováno v:
Bioorganicmedicinal chemistry letters. 12(4)
Acylated beta-amino acids are described as potent, specific and orally bioavailable antagonists of VLA-4. The initial lead was identified from a combinatorial library. Subsequent optimization using a traditional medicinal chemistry approach led to si
Autor:
Linus S, Lin, Thomas, Lanza, Ermenegilda, McCauley, Gail, Van Riper, Usha, Kidambi, Jin, Cao, Linda A, Egger, Richard A, Mumford, John A, Schmidt, Malcolm, MacCoss, William K, Hagmann
Publikováno v:
Bioorganicmedicinal chemistry letters. 12(2)
N-(3,5-Dichlorophenylsulfonyl)-(R)-thioprolyl biarylalanine 10a has been identified as a potent and specific antagonist of the alpha(4)beta(1) integrin. Altering the configuration of thioproline from R to S led to a series of dual antagonists of alph
Autor:
John W. Kozarich, Renee M. Chabin, Ermenegilda McCauley, John A. Schmidt, Sayyaparaju Madhusudanaraju, Nancy I. Hutchinson, Karen L. MacNaul, Gloria C. Wolfe, Kenny K. Wong, Jimmy R. Calaycay, Theresa M. Kelly
Publikováno v:
Biochemistry. 35(29)
Nitric oxide synthase catalyzes the pyridine nucleotide-dependent oxidation of L-arginine to nitric oxide and L-citrulline. It is a specialized cytochrome P450 monooxygenase that is sensitive to inhibition by imidazole. Steady-state kinetic studies o
Autor:
Jon D. Polishook, Russell B. Lingham, Claude Dufresne, Lin Kong, Gregory E. Koch, Isabel Martin, John G. Ondeyka, Jerrold M. Liesch, Tannis M. Jurgens, Ermenegilda McCauley, Hans T. Beck, Robert P. Borris, Carmen Cascales, Steven R. King, Otto D. Hensens, Susan L. Raghoobar, Fernando Pelaez, Michael J. Salvatore, Suzanne E. Gartner, Deborah L. Zink, Maria Teresa Diez, Michael J. Balick, Amy Hsu
Publikováno v:
Journal of natural products. 57(6)
gamma-Pyrone-3-acetic acid (L-741,494) is a novel metabolite produced by a culture of the fungal genus Xylaria. This substance is a water-soluble, competitive, irreversible inhibitor of Interleukin-1 beta Converting Enzyme that is inactive against pa
Autor:
Thomas J. Lanza, Plato A. Magriotis, Ralph A. Stearns, Malcolm MacCoss, Kathryn A. Lyons, Stella H. Vincent, Usha Kidambi, Adria Colletti, Linus S. Lin, Richard A. Mumford, Xinchun Tong, David N. Young, Stephen E. de Laszlo, Judy Fenyk-Melody, Ihor E. Kopka, John A. Schmidt, Philippe L. Durette, William K. Hagmann, Gail Van Riper, Ermenegilda McCauley, Yohannes Teffera, Theodore M. Kamenecka, Linda A. Egger
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 12:1695