The C3a receptor antagonist SB 290157 has agonist activity.
- Marie-Claude Mathieu, N. Sawyer, A. Therien
- BiologyImmunology Letters
- 15 September 2005
The structural basis for the selectivity of benzotriazole inhibitors of PTP1B.
- G. Scapin, Sangita Patel, E. Asante-Appiah
- Chemistry, BiologyBiochemistry
- 10 September 2003
Protein tyrosine phosphatase 1B (PTP1B) has been implicated in the regulation of the insulin signaling pathway and represents an attractive target for the design of inhibitors in the treatment of…
Structure based design of a series of potent and selective non peptidic PTP-1B inhibitors.
- C. Lau, C. Bayly, Giovana Scapin
- ChemistryBioorganic & Medicinal Chemistry Letters
- 23 February 2004
The discovery of MK-0674, an orally bioavailable cathepsin K inhibitor.
- Elise Isabel, K. Bateman, W. Black
- Biology, ChemistryBioorganic & Medicinal Chemistry Letters
- 1 February 2010
Conformation-assisted Inhibition of Protein-tyrosine Phosphatase-1B Elicits Inhibitor Selectivity over T-cell Protein-tyrosine Phosphatase*
- E. Asante-Appiah, Sangita Patel, G. Scapin
- Biology, ChemistryJournal of Biological Chemistry
- 24 March 2006
This work has successfully exploited the conservative Leu119 to Val substitution between the two enzymes to synthesize a PTP-1B inhibitor that is an order of magnitude more selective over TCPTP.
Cyclooxygenase-2 inhibitors. Synthesis and pharmacological activities of 5-methanesulfonamido-1-indanone derivatives.
- C. Li, W. Black, J. Mancini
- Chemistry, BiologyJournal of Medicinal Chemistry
- 8 December 1995
6-[(2,4-difluorophenyl)-thio]-5-methanesulfonamido-1-indanone++ + (20) (L-745,337) is identified as a potent, selective, and orally active COX-2 inhibitor and seems less ulcergenic than 2 in rats.
Rapid inhibition of the c-jun proto-oncogene expression in avian oviduct by estrogen.
- C. Lau, M. Subramaniam, K. Rasmussen, T. Spelsberg
- BiologyEndocrinology
- 1 November 1990
This paper demonstrates that the steady state c-jun mRNA level in the avian oviduct is markedly decreased to 50% of control values within 30 minutes after estrogen injection into the animals, which is the first demonstration of a steroid effect on c-Jun expression in any animal system.
Pyridazinones as selective cyclooxygenase-2 inhibitors.
- C. Li, C. Brideau, P. Prasit
- Biology, ChemistryBioorganic & Medicinal Chemistry Letters
- 1 February 2003
L-656,224 (7-chloro-2-[(4-methoxyphenyl)methyl]-3- methyl-5-propyl-4-benzofuranol): a novel, selective, orally active 5-lipoxygenase inhibitor.
- P. Belanger, A. Maycock, C. Lau
- Biology, ChemistryCanadian Journal of Physiology and Pharmacology
- 1 December 1987
The compound showed oral activity against hyperalgesia induced in the rat paw by injection of yeast or platelet-activating factor, and bronchoconstriction induced by an aerosol of Ascaris in squirrel monkeys, suggesting a role for 5-lipoxygenase inhibitors in the treatment of asthma and peripheral pain.
Development of 2,3-dihydro-6-(3-phenoxypropyl)-2-(2-phenylethyl)-5-benzofuranol (L-670,630) as a potent and orally active inhibitor of 5-lipoxygenase.
- C. Lau, P. Belanger, D. Denis
- ChemistryJournal of Medicinal Chemistry
- 3 April 1992
The series with no substituent at position 3 was the most potent and among the compounds in that series 2,3-dihydro-6-(3-phenoxypropyl)-2-phenylethyl)-5-benzofuranol (46, L-670,630) was chosen for further development.
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