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Table representation of search results timeline featuring number of search results per year.

Year Number of Results
1952 4
1953 2
1954 1
1955 1
1956 1
1957 4
1958 12
1959 16
1960 40
1961 82
1962 88
1963 140
1964 174
1965 44
1966 28
1967 64
1968 120
1969 204
1970 277
1971 320
1972 359
1973 349
1974 482
1975 628
1976 723
1977 706
1978 859
1979 927
1980 1244
1981 1329
1982 1738
1983 2114
1984 2528
1985 2899
1986 3116
1987 3391
1988 3996
1989 4534
1990 5203
1991 5785
1992 6372
1993 7365
1994 7956
1995 8796
1996 8962
1997 9085
1998 9608
1999 10130
2000 10832
2001 11147
2002 11579
2003 12260
2004 12787
2005 13435
2006 14091
2007 14509
2008 14899
2009 14809
2010 15883
2011 17000
2012 17242
2013 17237
2014 16944
2015 16691
2016 15908
2017 15565
2018 15498
2019 13415
2020 5421
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376,783 results
Results by year
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Page 1
Helix12-Stabilization Antagonist of Vitamin D Receptor.
Kato A, Itoh T, Anami Y, Egawa D, Yamamoto K. Kato A, et al. Bioconjug Chem. 2016 Jul 20;27(7):1750-61. doi: 10.1021/acs.bioconjchem.6b00246. Epub 2016 Jun 27. Bioconjug Chem. 2016. PMID: 27294600
To develop strong vitamin D receptor (VDR) antagonists and reveal their antagonistic mechanism, we designed and synthesized vitamin D analogues with bulky side chains based on the "active antagonist" concept in which antagonist prevents helix 12 (H12) …
To develop strong vitamin D receptor (VDR) antagonists and reveal their antagonistic mechanism, we designed and synthesized vi …
mGlu2/3 receptor antagonists.
Chaki S. Chaki S. Adv Pharmacol. 2019;86:97-120. doi: 10.1016/bs.apha.2019.03.004. Epub 2019 Apr 24. Adv Pharmacol. 2019. PMID: 31378257 Review.
Both orthosteric and allosteric antagonists of mGlu2/3 receptors have been synthesized, and their therapeutic potential has been examined. ...In this chapter, the general pharmacology of mGlu2/3 receptor antagonists and their therapeutic potential are …
Both orthosteric and allosteric antagonists of mGlu2/3 receptors have been synthesized, and their therapeutic potential has be …
Discovery of a Potent Steroidal Glucocorticoid Receptor Antagonist with Enhanced Selectivity against the Progesterone and Androgen Receptors (OP-3633).
Du X, Eksterowicz J, Zhou H, Rew Y, Zhu L, Yan X, Medina JC, Huang T, Chen X, Sutimantanapi D, Jahchan N, Kong W, Sun J, Zavorotinskaya T, Ye Q, Fantin VR, Sun D. Du X, et al. J Med Chem. 2019 Jul 25;62(14):6751-6764. doi: 10.1021/acs.jmedchem.9b00711. Epub 2019 Jul 5. J Med Chem. 2019. PMID: 31274313
Addition of a methyl group at the C10 position of the steroid has a significant impact on progesterone receptor (PR) and androgen receptor (AR) activity. Within this series, OP-3633 (15) emerged as a glucocorticoid receptor (GR) antagonist with increas …
Addition of a methyl group at the C10 position of the steroid has a significant impact on progesterone receptor (PR) and androgen …
GPCRs: Glucagon receptor antagonist binding site identified.
Crunkhorn S. Crunkhorn S. Nat Rev Drug Discov. 2016 Jun 1;15(6):384. doi: 10.1038/nrd.2016.100. Nat Rev Drug Discov. 2016. PMID: 27245394 No abstract available.
mGlu2/3 Receptor Antagonists as Novel Antidepressants.
Chaki S. Chaki S. Trends Pharmacol Sci. 2017 Jun;38(6):569-580. doi: 10.1016/j.tips.2017.03.008. Epub 2017 Apr 13. Trends Pharmacol Sci. 2017. PMID: 28413097 Review.
Furthermore, these findings have indicated the similarities of the antidepressant effects and of the mechanisms underlying these effects between mGlu2/3 receptor antagonists and ketamine. Based on the results obtained hitherto, here I discuss the potential for mGlu2 …
Furthermore, these findings have indicated the similarities of the antidepressant effects and of the mechanisms underlying these effects bet …
Estrogen Receptor Covalent Antagonists: The Best Is Yet to Come.
Furman C, Hao MH, Prajapati S, Reynolds D, Rimkunas V, Zheng GZ, Zhu P, Korpal M. Furman C, et al. Cancer Res. 2019 Apr 15;79(8):1740-1745. doi: 10.1158/0008-5472.CAN-18-3634. Epub 2019 Apr 5. Cancer Res. 2019. PMID: 30952631 Free article. Review.
The development of tamoxifen and subsequent estrogen receptor alpha (ERα) antagonists represents a tremendous therapeutic breakthrough in the treatment of breast cancer. Despite the ability of ERα antagonists to increase survival rates, resistance to these th …
The development of tamoxifen and subsequent estrogen receptor alpha (ERα) antagonists represents a tremendous therapeutic brea …
Clinical significance of chemokine receptor antagonists.
Miao M, De Clercq E, Li G. Miao M, et al. Expert Opin Drug Metab Toxicol. 2020 Jan;16(1):11-30. doi: 10.1080/17425255.2020.1711884. Epub 2020 Jan 17. Expert Opin Drug Metab Toxicol. 2020. PMID: 31903790 Review.
Introduction: Chemokine receptors are important therapeutic targets for the treatment of many human diseases. This study will provide an overview of approved chemokine receptor antagonists and promising candidates in advanced clinical trials.Areas covered: We …
Introduction: Chemokine receptors are important therapeutic targets for the treatment of many human diseases. This study will provide …
Serotonin-1A receptor stimulation mediates effects of a metabotropic glutamate 2/3 receptor antagonist, 2S-2-amino-2-(1S,2S-2-carboxycycloprop-1-yl)-3-(xanth-9-yl)propanoic acid (LY341495), and an N-methyl-D-aspartate receptor antagonist, ketamine, in the novelty-suppressed feeding test.
Fukumoto K, Iijima M, Chaki S. Fukumoto K, et al. Psychopharmacology (Berl). 2014 Jun;231(11):2291-8. doi: 10.1007/s00213-013-3378-0. Epub 2014 Jan 9. Psychopharmacology (Berl). 2014. PMID: 24402133
RATIONALE: α-Amino-3-hydroxy-5-methyl-4-isoxazole propionic acid (AMPA) receptor stimulation has been proposed to be a common neural mechanism of metabotropic glutamate 2/3 (mGlu2/3) receptor antagonists and an N-methyl-D-aspartate receptor antagoni
RATIONALE: α-Amino-3-hydroxy-5-methyl-4-isoxazole propionic acid (AMPA) receptor stimulation has been proposed to be a common neural …
[Can an antagonist for prostaglandin receptor be an alternative of aspirin?].
Aoki T. Aoki T. Nihon Yakurigaku Zasshi. 2016 Apr;147(4):253. doi: 10.1254/fpj.147.253. Nihon Yakurigaku Zasshi. 2016. PMID: 27063910 Japanese. No abstract available.
THuNDRous news for human dopamine researchers: A selective dopamine D1 receptor antagonist will soon be available for clinical research.
Nutt D, Robbins T, Hayes A. Nutt D, et al. J Psychopharmacol. 2018 Nov;32(11):1153-1154. doi: 10.1177/0269881118799380. Epub 2018 Oct 24. J Psychopharmacol. 2018. PMID: 30354927 No abstract available.
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