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Intravenous administration of the selective toll-like receptor 7 agonist DSR-29133 leads to anti-tumor efficacy in murine solid tumor models which can be potentiated by combination with fractionated radiotherapy.
Dovedi SJ, Adlard AL, Ota Y, Murata M, Sugaru E, Koga-Yamakawa E, Eguchi K, Hirose Y, Yamamoto S, Umehara H, Honeychurch J, Cheadle EJ, Hughes G, Jewsbury PJ, Wilkinson RW, Stratford IJ, Illidge TM. Dovedi SJ, et al. Among authors: sugaru e. Oncotarget. 2016 Mar 29;7(13):17035-46. doi: 10.18632/oncotarget.7928. Oncotarget. 2016. PMID: 26959743 Free PMC article.
TLR7 tolerance is independent of the type I IFN pathway and leads to loss of anti-tumor efficacy in mice.
Koga-Yamakawa E, Murata M, Dovedi SJ, Wilkinson RW, Ota Y, Umehara H, Sugaru E, Hirose Y, Harada H, Jewsbury PJ, Yamamoto S, Robinson DT, Li CJ. Koga-Yamakawa E, et al. Among authors: sugaru e. Cancer Immunol Immunother. 2015 Oct;64(10):1229-39. doi: 10.1007/s00262-015-1730-4. Epub 2015 Jun 20. Cancer Immunol Immunother. 2015. PMID: 26091797 Free PMC article.
Discovery of 3H-imidazo[4,5-c]quinolin-4(5H)-ones as potent and selective dipeptidyl peptidase IV (DPP-4) inhibitors: use of a carboxylate prodrug to improve bioavailability.
Ikuma Y, Hochigai H, Kimura H, Nunami N, Kobayashi T, Uchiyama K, Umezome T, Sakurai Y, Sawada N, Tadano J, Sugaru E, Ono M, Hirose Y, Nakahira H. Ikuma Y, et al. Among authors: sugaru e. Bioorg Med Chem. 2015 Feb 15;23(4):779-90. doi: 10.1016/j.bmc.2014.12.051. Epub 2014 Dec 30. Bioorg Med Chem. 2015. PMID: 25596166
Chronic administration of DSP-7238, a novel, potent, specific and substrate-selective DPP IV inhibitor, improves glycaemic control and beta-cell damage in diabetic mice.
Furuta Y, Horiguchi M, Sugaru E, Ono-Kishino M, Otani M, Sakai M, Masui Y, Tsuchida A, Sato Y, Takubo K, Hochigai H, Kimura H, Nakahira H, Nakagawa T, Taiji M. Furuta Y, et al. Among authors: sugaru e. Diabetes Obes Metab. 2010 May;12(5):421-30. doi: 10.1111/j.1463-1326.2009.01180.x. Diabetes Obes Metab. 2010. PMID: 20415690
2-({6-[(3R)-3-amino-3-methylpiperidine-1-yl]-1,3-dimethyl-2,4-dioxo-1,2,3,4-tetrahydro-5H-pyrrolo[3,2-d]pyrimidine-5-yl}methyl)-4-fluorobenzonitrile (DSR-12727): a potent, orally active dipeptidyl peptidase IV inhibitor without mechanism-based inactivation of CYP3A.
Nishio Y, Kimura H, Sawada N, Sugaru E, Horiguchi M, Ono M, Furuta Y, Sakai M, Masui Y, Otani M, Hashizuka T, Honda Y, Deguchi J, Nakagawa T, Nakahira H. Nishio Y, et al. Among authors: sugaru e. Bioorg Med Chem. 2011 Sep 15;19(18):5490-9. doi: 10.1016/j.bmc.2011.07.042. Epub 2011 Aug 4. Bioorg Med Chem. 2011. PMID: 21865048
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