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14 results

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Page 1
AT7867 is a potent and oral inhibitor of AKT and p70 S6 kinase that induces pharmacodynamic changes and inhibits human tumor xenograft growth.
Grimshaw KM, Hunter LJ, Yap TA, Heaton SP, Walton MI, Woodhead SJ, Fazal L, Reule M, Davies TG, Seavers LC, Lock V, Lyons JF, Thompson NT, Workman P, Garrett MD. Grimshaw KM, et al. Among authors: heaton sp. Mol Cancer Ther. 2010 May;9(5):1100-10. doi: 10.1158/1535-7163.MCT-09-0986. Epub 2010 Apr 27. Mol Cancer Ther. 2010. PMID: 20423992 Free PMC article.
Preclinical pharmacology, antitumor activity, and development of pharmacodynamic markers for the novel, potent AKT inhibitor CCT128930.
Yap TA, Walton MI, Hunter LJ, Valenti M, de Haven Brandon A, Eve PD, Ruddle R, Heaton SP, Henley A, Pickard L, Vijayaraghavan G, Caldwell JJ, Thompson NT, Aherne W, Raynaud FI, Eccles SA, Workman P, Collins I, Garrett MD. Yap TA, et al. Among authors: heaton sp. Mol Cancer Ther. 2011 Feb;10(2):360-71. doi: 10.1158/1535-7163.MCT-10-0760. Epub 2010 Dec 29. Mol Cancer Ther. 2011. PMID: 21191045 Free PMC article.
AT13148 is a novel, oral multi-AGC kinase inhibitor with potent pharmacodynamic and antitumor activity.
Yap TA, Walton MI, Grimshaw KM, Te Poele RH, Eve PD, Valenti MR, de Haven Brandon AK, Martins V, Zetterlund A, Heaton SP, Heinzmann K, Jones PS, Feltell RE, Reule M, Woodhead SJ, Davies TG, Lyons JF, Raynaud FI, Eccles SA, Workman P, Thompson NT, Garrett MD. Yap TA, et al. Among authors: heaton sp. Clin Cancer Res. 2012 Jul 15;18(14):3912-23. doi: 10.1158/1078-0432.CCR-11-3313. Epub 2012 Jul 10. Clin Cancer Res. 2012. PMID: 22781553
Interrogating two schedules of the AKT inhibitor MK-2206 in patients with advanced solid tumors incorporating novel pharmacodynamic and functional imaging biomarkers.
Yap TA, Yan L, Patnaik A, Tunariu N, Biondo A, Fearen I, Papadopoulos KP, Olmos D, Baird R, Delgado L, Tetteh E, Beckman RA, Lupinacci L, Riisnaes R, Decordova S, Heaton SP, Swales K, deSouza NM, Leach MO, Garrett MD, Sullivan DM, de Bono JS, Tolcher AW. Yap TA, et al. Among authors: heaton sp. Clin Cancer Res. 2014 Nov 15;20(22):5672-85. doi: 10.1158/1078-0432.CCR-14-0868. Epub 2014 Sep 19. Clin Cancer Res. 2014. PMID: 25239610 Free PMC article. Clinical Trial.
First-in-man clinical trial of the oral pan-AKT inhibitor MK-2206 in patients with advanced solid tumors.
Yap TA, Yan L, Patnaik A, Fearen I, Olmos D, Papadopoulos K, Baird RD, Delgado L, Taylor A, Lupinacci L, Riisnaes R, Pope LL, Heaton SP, Thomas G, Garrett MD, Sullivan DM, de Bono JS, Tolcher AW. Yap TA, et al. Among authors: heaton sp. J Clin Oncol. 2011 Dec 10;29(35):4688-95. doi: 10.1200/JCO.2011.35.5263. Epub 2011 Oct 24. J Clin Oncol. 2011. PMID: 22025163 Clinical Trial.
AZD1152, a selective inhibitor of Aurora B kinase, inhibits human tumor xenograft growth by inducing apoptosis.
Wilkinson RW, Odedra R, Heaton SP, Wedge SR, Keen NJ, Crafter C, Foster JR, Brady MC, Bigley A, Brown E, Byth KF, Barrass NC, Mundt KE, Foote KM, Heron NM, Jung FH, Mortlock AA, Boyle FT, Green S. Wilkinson RW, et al. Among authors: heaton sp. Clin Cancer Res. 2007 Jun 15;13(12):3682-8. doi: 10.1158/1078-0432.CCR-06-2979. Clin Cancer Res. 2007. PMID: 17575233
Synthesis and SAR of 1-acetanilide-4-aminopyrazole-substituted quinazolines: selective inhibitors of Aurora B kinase with potent anti-tumor activity.
Foote KM, Mortlock AA, Heron NM, Jung FH, Hill GB, Pasquet G, Brady MC, Green S, Heaton SP, Kearney S, Keen NJ, Odedra R, Wedge SR, Wilkinson RW. Foote KM, et al. Among authors: heaton sp. Bioorg Med Chem Lett. 2008 Mar 15;18(6):1904-9. doi: 10.1016/j.bmcl.2008.02.002. Epub 2008 Feb 7. Bioorg Med Chem Lett. 2008. PMID: 18294849
14 results