Affiliation: Pharmacia Corporation
- A selective IKK-2 inhibitor blocks NF-kappa B-dependent gene expression in interleukin-1 beta-stimulated synovial fibroblastsNandini Kishore
Department of Arthritis and Inflammation Pharmacology, Pharmacia Corp, St Louis, Missouri 63167, USA
J Biol Chem 278:32861-71. 2003..Thus, the effect of SC-514 on cytokine gene expression may be a combination of inhibiting I kappa B alpha phosphorylation/degradation, affecting NF-kappa B nuclear import/export as well as the phosphorylation and transactivation of p65...
- Kinetic mechanisms of IkappaB-related kinases (IKK) inducible IKK and TBK-1 differ from IKK-1/IKK-2 heterodimerQ Khai Huynh
Department of Arthritis and Inflammation Pharmacology, Discovery Research, Pharmacia Corporation, Mailzone T3M, 800 North Lindbergh Blvd, St Louis, MO 63167, USA
J Biol Chem 277:12550-8. 2002..87 microm), followed by rhIKK-i (K(IkappaBalpha) = 5.47 microm) and rhIKK-1/rhIKK-2 heterodimers (K(IkappaBalpha) = 0.12 microm). Thus this family of IkappaB kinases has very unique kinetic properties...
- IKK-i and TBK-1 are enzymatically distinct from the homologous enzyme IKK-2: comparative analysis of recombinant human IKK-i, TBK-1, and IKK-2Nandini Kishore
Department of Arthritis and Inflammation Pharmacology, Discovery Research, Pharmacia Corporation, St Louis, Missouri 63167, USA
J Biol Chem 277:13840-7. 2002..Thus, although these IKKs are structurally similar, their enzymatic properties may provide insights into their unique functions...
- Inhibition of IKK-2 by 2-[(aminocarbonyl)amino]-5-acetylenyl-3-thiophenecarboxamidesDominique Bonafoux
Department of Medicinal Chemistry, Pfizer Inc, St Louis, MO 63017, USA
Bioorg Med Chem Lett 15:2870-5. 2005....
- Discovery of novel benzothiazolesulfonamides as potent inhibitors of HIV-1 proteaseSrinivasan R Nagarajan
Pfizer Global Research and Development, Pfizer Inc, 700 Chesterfield Parkway West, Chesterfield, MO 63017, USA
Bioorg Med Chem 11:4769-77. 2003..During the course of our studies, we also developed an efficient synthesis of benzothiazole-6-sulfonic acid via a two-step procedure starting from sulfanilamide...