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Kurt R Gregor

Explore the profile of Kurt R Gregor including associated specialties, affiliations and a list of published articles. Areas
Snapshot
Articles 5
Citations 275
Followers 0
Related Specialties
Biochemistry
Pharmacology
Chemistry
Top 10 Co-Authors
James R Burke
Mark A Pattoli
John F MacMaster
Kim W McIntyre
F Christopher Zusi
Yuping Qiu
Luisa Salter-Cid
Vojkan Susulic
Joann Strnad
Ning Li
Published In
J Pharmacol Exp Ther
J Biol Chem
J Med Chem
Bioorg Med Chem Lett
Affiliations
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Recent Articles
1.
Biologic-like In Vivo Efficacy with Small Molecule Inhibitors of TNFα Identified Using Scaffold Hopping and Structure-Based Drug Design Approaches
Xiao H, Li N, Duan J, Jiang B, Lu Z, Ngu K, et al.
J Med Chem . 2020 Dec; 63(23):15050-15071. PMID: 33261314
Scaffold hopping and structure-based drug design were employed to identify substituted 4-aminoquinolines and 4-aminonaphthyridines as potent, small molecule inhibitors of tumor necrosis factor alpha (TNFα). Structure-activity relationships in both the...
2.
Periodic, partial inhibition of IkappaB Kinase beta-mediated signaling yields therapeutic benefit in preclinical models of rheumatoid arthritis
Gillooly K, Pattoli M, Taylor T, Chen L, Cheng L, Gregor K, et al.
J Pharmacol Exp Ther . 2009 Aug; 331(2):349-60. PMID: 19652024
We have previously shown that inhibitors of IkappaB kinase beta (IKKbeta), including 4(2'-aminoethyl)amino-1,8-dimethylimidazo(1,2-a)quinoxaline (BMS-345541), are efficacious against experimental arthritis in rodents. In our efforts to identify an analog as a...
3.
Synthesis and biological evaluation of 4-amino derivatives of benzimidazoquinoxaline, benzimidazoquinoline, and benzopyrazoloquinazoline as potent IKK inhibitors
Beaulieu F, Ouellet C, Ruediger E, Belema M, Qiu Y, Yang X, et al.
Bioorg Med Chem Lett . 2007 Jan; 17(5):1233-7. PMID: 17197177
We have recently identified BMS-345541 (1) as a highly selective and potent inhibitor of IKK-2 (IC50 = 0.30 microM), which however was considerably less potent against IKK-1 (IC50 = 4.0...
4.
Collagen and aggrecan degradation is blocked in interleukin-1-treated cartilage explants by an inhibitor of IkappaB kinase through suppression of metalloproteinase expression
Pattoli M, MacMaster J, Gregor K, Burke J
J Pharmacol Exp Ther . 2005 Jul; 315(1):382-8. PMID: 16009742
It has previously been shown that BMS-345541 [4(2'-aminoethyl)amino-1,8-dimethylimidazo(1,2-a)quinoxaline], a highly-selective inhibitor of IkappaB kinase (IKK), blocks both inflammation and joint destruction in murine collagen-induced arthritis. Although this agent has been...
5.
BMS-345541 is a highly selective inhibitor of I kappa B kinase that binds at an allosteric site of the enzyme and blocks NF-kappa B-dependent transcription in mice
Burke J, Pattoli M, Gregor K, Brassil P, MacMaster J, McIntyre K, et al.
J Biol Chem . 2002 Oct; 278(3):1450-6. PMID: 12403772
The signal-inducible phosphorylation of serines 32 and 36 of I kappa B alpha is critical in regulating the subsequent ubiquitination and proteolysis of I kappa B alpha, which then releases...