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Inhibitory effect of novel somatostatin peptide analogues on human cancer cell growth based on the selective inhibition of DNA polymerase β.
Kuriyama I, Miyazaki A, Tsuda Y, Yoshida H, Mizushina Y. Kuriyama I, et al. Among authors: miyazaki a. Bioorg Med Chem. 2013 Jan 15;21(2):403-11. doi: 10.1016/j.bmc.2012.11.024. Epub 2012 Nov 29. Bioorg Med Chem. 2013. PMID: 23266186
The present study was designed to investigate the anticancer activity of novel nine small peptides (compounds 1-9) derived from TT-232, a somatostatin structural analogue, by analyzing the inhibition of mammalian DNA polymerase (pol) and human cancer cell growth. ...From t …
The present study was designed to investigate the anticancer activity of novel nine small peptides (compounds 1-9) derived from TT-232, a
PET probe detecting non-small cell lung cancer susceptible to epidermal growth factor receptor tyrosine kinase inhibitor therapy.
Makino A, Miyazaki A, Tomoike A, Kimura H, Arimitsu K, Hirata M, Ohmomo Y, Nishii R, Okazawa H, Kiyono Y, Ono M, Saji H. Makino A, et al. Among authors: miyazaki a. Bioorg Med Chem. 2018 May 1;26(8):1609-1613. doi: 10.1016/j.bmc.2018.02.007. Epub 2018 Feb 8. Bioorg Med Chem. 2018. PMID: 29478801
Inhibitory effect of somatostatin Peptide analogues on DNA polymerase activity and human cancer cell proliferation.
Kuriyama I, Miyazaki A, Tsuda Y, Yokoi T, Okada Y, Takeuchi T, Sugawara F, Yoshida H, Mizushina Y. Kuriyama I, et al. Among authors: miyazaki a. Anticancer Res. 2010 Dec;30(12):4841-9. Anticancer Res. 2010. PMID: 21187461
BACKGROUND AND OBJECTIVES: It was previously reported that ten small peptides derived from TT-232, somatostatin structural analogue (compounds 1-10), synthesised by a solution-phase method, exhibited potent antitumour activity on human epithelial tumour (A431) cells. ...RE …
BACKGROUND AND OBJECTIVES: It was previously reported that ten small peptides derived from TT-232, somatostatin structural analogue (compoun …
Synthesis of somatostatin analogues containing C-terminal adamantane and their antiproliferative properties.
Miyazaki A, Tsuda Y, Fukushima S, Yokoi T, Vántus T, Bökönyi G, Szabó E, Horváth A, Kéri G, Okada Y. Miyazaki A, et al. J Med Chem. 2008 Aug 28;51(16):5121-4. doi: 10.1021/jm701599w. Epub 2008 Aug 5. J Med Chem. 2008. PMID: 18680358
On the basis of the structure of somatostatin analogue TT-232 (1), which exhibited a highly potent antitumor activity, we synthesized small linear peptide derivatives and evaluated their antitumor and apoptotic activity. Of them, Boc-Tyr-D-Trp-1-adamantylamide (5) had the …
On the basis of the structure of somatostatin analogue TT-232 (1), which exhibited a highly potent antitumor activity, we synthesized …
New cyclic somatostatin analogues containing a pyrazinone ring: importance of Tyr for antiproliferative activity.
Miyazaki A, Tsuda Y, Fukushima S, Yokoi T, Vántus T, Bökönyi G, Szabó E, Horváth A, Kéri G, Okada Y. Miyazaki A, et al. Bioorg Med Chem Lett. 2008 Dec 1;18(23):6199-201. doi: 10.1016/j.bmcl.2008.10.001. Epub 2008 Oct 5. Bioorg Med Chem Lett. 2008. PMID: 18930401
Novel somatostatin analogues containing a pyrazinone ring, compounds 1 and 2, exhibited good antiproliferative activity on A431 tumor cells. ...
Novel somatostatin analogues containing a pyrazinone ring, compounds 1 and 2, exhibited good antiproliferative activity on A431 tumor …
Synthesis of opioidmimetics, 3-[H-Dmt-NH(CH(2))(m)]-6-[H-Dmt-NH(CH(2))(n)]-2(1H)-pyrazinones, and studies on structure-activity relationships.
Shiotani K, Miyazaki A, Li T, Tsuda Y, Yokoi T, Ambo A, Sasaki Y, Bryant SD, Jinsmaa Y, Lazarus LH, Okada Y. Shiotani K, et al. Among authors: miyazaki a. Med Chem. 2007 Nov;3(6):583-98. doi: 10.2174/157340607782360272. Med Chem. 2007. PMID: 18045209
The data verify that a specific length of aliphatic linker is required between the Dmt pharmacophore and the pyrazinone ring to produce unique mu-opioid receptor ligands....
The data verify that a specific length of aliphatic linker is required between the Dmt pharmacophore and the pyrazinone ring to produ …
Design and synthesis of opioidmimetics containing 2',6'-dimethyl-L-tyrosine and a pyrazinone-ring platform.
Shiotani K, Li T, Miyazaki A, Tsuda Y, Yokoi T, Ambo A, Sasaki Y, Bryant SD, Lazarus LH, Okada Y. Shiotani K, et al. Among authors: miyazaki a. Bioorg Med Chem Lett. 2007 Nov 1;17(21):5768-71. doi: 10.1016/j.bmcl.2007.08.058. Epub 2007 Aug 28. Bioorg Med Chem Lett. 2007. PMID: 17826995 Free PMC article.
Twelve 2',6'-dimethyl-L-tyrosine (Dmt) analogues linked to a pyrazinone platform were synthesized as 3- or 6-[H-Dmt-NH(CH(2))(n)],3- or 6-R-2(1H)-pyrazinone (n=1-4). 3-[H-Dmt-NH-(CH(2))(4)]-6-beta-phenethyl-5-methyl-2(1H)-pyrazinone 11 bound to mu-opioid receptors with hig …
Twelve 2',6'-dimethyl-L-tyrosine (Dmt) analogues linked to a pyrazinone platform were synthesized as 3- or 6-[H-Dmt-NH(CH(2))(n)],3- …
Bifunctional [2',6'-dimethyl-L-tyrosine1]endomorphin-2 analogues substituted at position 3 with alkylated phenylalanine derivatives yield potent mixed mu-agonist/delta-antagonist and dual mu-agonist/delta-agonist opioid ligands.
Li T, Shiotani K, Miyazaki A, Tsuda Y, Ambo A, Sasaki Y, Jinsmaa Y, Marczak E, Bryant SD, Lazarus LH, Okada Y. Li T, et al. Among authors: miyazaki a. J Med Chem. 2007 Jun 14;50(12):2753-66. doi: 10.1021/jm061238m. Epub 2007 May 12. J Med Chem. 2007. PMID: 17497839 Free PMC article.
(iii) There were elevated mu-bioactivity (IC50 = 0.12-14.4 nM) and abolished delta-agonism (IC50 > 10 muM in 2', 3', 4', 5', 6'), although 4' and 6' demonstrated a potent mixed mu-agonism/delta-antagonism (for 4', IC50mu = 0.12 and pA2 = 8.15; for 6', IC50mu = 0.21 nM a …
(iii) There were elevated mu-bioactivity (IC50 = 0.12-14.4 nM) and abolished delta-agonism (IC50 > 10 muM in 2', 3', 4', 5', 6'), althoug …
Transformation of mu-opioid receptor agonists into biologically potent mu-opioid receptor antagonists.
Li T, Jinsmaa Y, Nedachi M, Miyazaki A, Tsuda Y, Ambo A, Sasaki Y, Bryant SD, Marczak E, Li Q, Swartzwelder HS, Lazarus LH, Okada Y. Li T, et al. Among authors: miyazaki a. Bioorg Med Chem. 2007 Feb 1;15(3):1237-51. doi: 10.1016/j.bmc.2006.11.019. Epub 2006 Nov 14. Bioorg Med Chem. 2007. PMID: 17142049
Thus, N-allylation of Dmt containing opioid peptides or opioidmimetics continues to provide a facile means to convert selective mu-opioid agonists into potent mu-opioid antagonists....
Thus, N-allylation of Dmt containing opioid peptides or opioidmimetics continues to provide a facile means to convert selective mu-op …
Synthesis of 3,6-bis[H-Tyr/H-Dmt-NH(CH2)m,n]-2(1H)pyrazinone derivatives: function of alkyl chain length on opioid activity.
Shiotani K, Li T, Miyazaki A, Tsuda Y, Bryant SD, Ambo A, Sasaki Y, Lazarus LH, Okada Y. Shiotani K, et al. Among authors: miyazaki a. Bioorg Med Chem Lett. 2006 Nov 15;16(22):5793-6. doi: 10.1016/j.bmcl.2006.08.079. Epub 2006 Sep 1. Bioorg Med Chem Lett. 2006. PMID: 16949282 Free PMC article.
Dimeric opioid analogues linked to a pyrazinone platform, 3-[Tyr/Dmt-NH(CH2)m]-6-[Tyr/Dmt-NH(CH2)n]-2(1H)-pyrazinone (m, n=3 or 4), were synthesized. ...
Dimeric opioid analogues linked to a pyrazinone platform, 3-[Tyr/Dmt-NH(CH2)m]-6-[Tyr/Dmt-NH(CH2)n]-2(1H)-pyrazinone (m, n=3 or 4), w …
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