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Novel small molecule inhibitors of the OLIG2 transcription factor: promising new therapeutics for glioblastoma.
Alton G, Kesari S. Alton G, et al. Future Oncol. 2016;12(8):1001-4. doi: 10.2217/fon-2015-0078. Epub 2016 Feb 12. Future Oncol. 2016. PMID: 26867754 No abstract available.
Therapeutic modulation of inflammatory gene transcription by kinase inhibitors.
Alton G, Schwamborn K, Satoh Y, Westwick JK. Alton G, et al. Expert Opin Biol Ther. 2002 Aug;2(6):621-32. doi: 10.1517/14712598.2.6.621. Expert Opin Biol Ther. 2002. PMID: 12171506 Review.
Targeting the unactivated conformations of protein kinases for small molecule drug discovery.
Alton GR, Lunney EA. Alton GR, et al. Expert Opin Drug Discov. 2008 Jun;3(6):595-605. doi: 10.1517/17460441.3.6.595. Expert Opin Drug Discov. 2008. PMID: 23506143
Cytoreductive antitumor activity of PF-2341066, a novel inhibitor of anaplastic lymphoma kinase and c-Met, in experimental models of anaplastic large-cell lymphoma.
Christensen JG, Zou HY, Arango ME, Li Q, Lee JH, McDonnell SR, Yamazaki S, Alton GR, Mroczkowski B, Los G. Christensen JG, et al. Among authors: alton gr. Mol Cancer Ther. 2007 Dec;6(12 Pt 1):3314-22. doi: 10.1158/1535-7163.MCT-07-0365. Mol Cancer Ther. 2007. PMID: 18089725
PF-2341066 potently inhibited cell proliferation, which was associated with G(1)-S-phase cell cycle arrest and induction of apoptosis in ALK-positive ALCL cells (IC(50) values, approximately 30 nmol/L) but not ALK-negative lymphoma cells. ...
PF-2341066 potently inhibited cell proliferation, which was associated with G(1)-S-phase cell cycle arrest and induction of apoptosis …
Study of the PDK1/AKT signaling pathway using selective PDK1 inhibitors, HCS, and enhanced biochemical assays.
Hofler A, Nichols T, Grant S, Lingardo L, Esposito EA, Gridley S, Murphy ST, Kath JC, Cronin CN, Kraus M, Alton G, Xie Z, Sutton S, Gehring M, Ermolieff J. Hofler A, et al. Among authors: alton g. Anal Biochem. 2011 Jul 15;414(2):179-86. doi: 10.1016/j.ab.2011.03.013. Epub 2011 Mar 12. Anal Biochem. 2011. PMID: 21402045
Discovery of novel, potent, and selective inhibitors of 3-phosphoinositide-dependent kinase (PDK1).
Murphy ST, Alton G, Bailey S, Baxi SM, Burke BJ, Chappie TA, Ermolieff J, Ferre R, Greasley S, Hickey M, Humphrey J, Kablaoui N, Kath J, Kazmirski S, Kraus M, Kupchinsky S, Li J, Lingardo L, Marx MA, Richter D, Tanis SP, Tran K, Vernier W, Xie Z, Yin MJ, Yu XH. Murphy ST, et al. Among authors: alton g. J Med Chem. 2011 Dec 22;54(24):8490-500. doi: 10.1021/jm201019k. Epub 2011 Nov 23. J Med Chem. 2011. PMID: 22040023
Structure based drug design of crizotinib (PF-02341066), a potent and selective dual inhibitor of mesenchymal-epithelial transition factor (c-MET) kinase and anaplastic lymphoma kinase (ALK).
Cui JJ, Tran-Dubé M, Shen H, Nambu M, Kung PP, Pairish M, Jia L, Meng J, Funk L, Botrous I, McTigue M, Grodsky N, Ryan K, Padrique E, Alton G, Timofeevski S, Yamazaki S, Li Q, Zou H, Christensen J, Mroczkowski B, Bender S, Kania RS, Edwards MP. Cui JJ, et al. Among authors: alton g. J Med Chem. 2011 Sep 22;54(18):6342-63. doi: 10.1021/jm2007613. Epub 2011 Aug 18. J Med Chem. 2011. PMID: 21812414
Novel isoquinolone PDK1 inhibitors discovered through fragment-based lead discovery.
Johnson MC, Hu Q, Lingardo L, Ferre RA, Greasley S, Yan J, Kath J, Chen P, Ermolieff J, Alton G. Johnson MC, et al. Among authors: alton g. J Comput Aided Mol Des. 2011 Jul;25(7):689-98. doi: 10.1007/s10822-011-9456-7. Epub 2011 Jul 22. J Comput Aided Mol Des. 2011. PMID: 21779981
Identification of novel pyrrolopyrazoles as protein kinase C β II inhibitors.
Li H, Hong Y, Nukui S, Lou J, Johnson S, Scales S, Botrous I, Tompkins E, Yin C, Zhou R, He M, Jensen J, Bouzida D, Alton G, Lafontaine J, Grant S. Li H, et al. Among authors: alton g. Bioorg Med Chem Lett. 2011 Jan 1;21(1):584-7. doi: 10.1016/j.bmcl.2010.10.032. Epub 2010 Oct 13. Bioorg Med Chem Lett. 2011. PMID: 21084194
Characterization of the CHK1 allosteric inhibitor binding site.
Vanderpool D, Johnson TO, Ping C, Bergqvist S, Alton G, Phonephaly S, Rui E, Luo C, Deng YL, Grant S, Quenzer T, Margosiak S, Register J, Brown E, Ermolieff J. Vanderpool D, et al. Among authors: alton g. Biochemistry. 2009 Oct 20;48(41):9823-30. doi: 10.1021/bi900258v. Biochemistry. 2009. PMID: 19743875
Checkpoint kinase 1 (CHK1) is a key element in the DNA damage response pathway and plays a crucial role in the S-G(2)-phase checkpoint. ...
Checkpoint kinase 1 (CHK1) is a key element in the DNA damage response pathway and plays a crucial role in the S-G(2)-phase checkpoin …
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