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Shawn M OConnell

Explore the profile of Shawn M OConnell including associated specialties, affiliations and a list of published articles. Areas
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Articles 7
Citations 122
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Recent Articles
1.
Bennett M, Wu Y, Boloor A, Matuszkiewicz J, OConnell S, Shi L, et al.
Bioorg Med Chem Lett . 2018 Apr; 28(10):1811-1816. PMID: 29657099
The bromodomain and extra-terminal (BET) family of epigenetic proteins has attracted considerable attention in drug discovery given its involvement in regulating gene transcription. Screening a focused small molecule library based...
2.
Nie Z, Shi L, Lai C, OConnell S, Xu J, Stansfield R, et al.
Bioorg Med Chem Lett . 2018 Apr; 28(9):1490-1494. PMID: 29627262
Histone lysine demethylases (KDMs) play a key role in epigenetic regulation and KDM5A and KDM5B have been identified as potential anti-cancer drug targets. Using structural information from known KDM4 and...
3.
Chen Y, Bonaldi T, Cuomo A, Del Rosario J, Hosfield D, Kanouni T, et al.
ACS Med Chem Lett . 2017 Aug; 8(8):869-874. PMID: 28835804
Histone lysine demethylases (KDMs) play a vital role in the regulation of chromatin-related processes. Herein, we describe our discovery of a series of potent KDM4 inhibitors that are both cell...
4.
Micel L, Tentler J, Tan A, Selby H, Brunkow K, Robertson K, et al.
Mol Cancer Ther . 2014 Nov; 14(2):317-25. PMID: 25376610
The goal of this study was to investigate the activity of the selective MEK1/2 inhibitor TAK-733 in both melanoma cell lines and patient-derived melanoma xenograft models. In vitro cell proliferation...
5.
Adams M, Wallace M, Kanouni T, Scorah N, OConnell S, Miyake H, et al.
Bioorg Med Chem Lett . 2012 Mar; 22(7):2411-4. PMID: 22406151
The structure-based design, synthesis, and biological evaluation of two novel series of potent and selective MEK kinase inhibitors are described herein. The elaboration of a lead pyrrole derivative to a...
6.
Dong Q, Dougan D, Gong X, Halkowycz P, Jin B, Kanouni T, et al.
Bioorg Med Chem Lett . 2011 Feb; 21(5):1315-9. PMID: 21310613
A novel 5-phenylamino-8-methylpyrido[2,3-d]pyrimidine-4,7(3H,8H)-dione series of MEK inhibitors has been developed using structure-based drug design. Lead optimization of this series led to the discovery of TAK-733. This was advanced to Phase...
7.
Wallace M, Adams M, Kanouni T, Mol C, Dougan D, Feher V, et al.
Bioorg Med Chem Lett . 2010 Jul; 20(14):4156-8. PMID: 20621728
A novel series of pyrrole inhibitors of MEK kinase has been developed using structure-based drug design. Optimization of the series led to the identification of potent inhibitors with good pharmaceutical...