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Results by year

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

Year Number of Results
1781 37
1782 18
1783 22
1784 27
1785 43
1786 60
1787 43
1788 33
1789 32
1790 44
1791 19
1792 33
1793 17
1794 18
1795 13
1796 15
1797 59
1798 15
1799 291
1800 377
1801 360
1802 283
1803 269
1804 289
1805 314
1806 282
1807 295
1808 289
1809 265
1810 267
1811 322
1812 238
1813 265
1814 285
1815 222
1816 315
1817 288
1818 303
1819 225
1820 213
1821 270
1822 247
1823 291
1824 269
1825 262
1826 385
1827 326
1828 467
1829 645
1830 569
1831 627
1832 313
1833 293
1834 287
1835 305
1836 271
1837 350
1838 484
1839 546
1840 695
1841 1154
1842 1488
1843 1118
1844 1248
1845 1278
1846 1406
1847 1367
1848 1204
1849 1208
1850 1126
1851 1228
1852 1310
1853 1559
1854 1306
1855 1587
1856 1587
1857 1488
1858 1542
1859 1562
1860 1632
1861 1275
1862 1112
1863 995
1864 1139
1865 1151
1866 1477
1867 1723
1868 1813
1869 1909
1870 1809
1871 2238
1872 2242
1873 2313
1874 2508
1875 2402
1876 2095
1877 2180
1878 2454
1879 2399
1880 2646
1881 3149
1882 2743
1883 3127
1884 3050
1885 3338
1886 3291
1887 3965
1888 4002
1889 4196
1890 4025
1891 3607
1892 4081
1893 4370
1894 3801
1895 4129
1896 4413
1897 4689
1898 4632
1899 4169
1900 3786
1901 3887
1902 3968
1903 3910
1904 4060
1905 4067
1906 3872
1907 4323
1908 4459
1909 4687
1910 4799
1911 5007
1912 4906
1913 5107
1914 5135
1915 4641
1916 4543
1917 4281
1918 4567
1919 4619
1920 4960
1921 4628
1922 4123
1923 4432
1924 4851
1925 4990
1926 5342
1927 5887
1928 5479
1929 5741
1930 5630
1931 5496
1932 5548
1933 5610
1934 5508
1935 5661
1936 5384
1937 5308
1938 5765
1939 5541
1940 4998
1941 4838
1942 4775
1943 4517
1944 4745
1945 20422
1946 53739
1947 64968
1948 70729
1949 62806
1950 85750
1951 103810
1952 108147
1953 108914
1954 105913
1955 108541
1956 107005
1957 111515
1958 109459
1959 109988
1960 112210
1961 120166
1962 125670
1963 141520
1964 162087
1965 176642
1966 179758
1967 191503
1968 207847
1969 215079
1970 218981
1971 222888
1972 227524
1973 230656
1974 234529
1975 248261
1976 250329
1977 249844
1978 258199
1979 265491
1980 267141
1981 271479
1982 283056
1983 294718
1984 302632
1985 318868
1986 331327
1987 347347
1988 363848
1989 377919
1990 383046
1991 380888
1992 382595
1993 390300
1994 401887
1995 411159
1996 421220
1997 418965
1998 436712
1999 453910
2000 491085
2001 503466
2002 521316
2003 548916
2004 591997
2005 650691
2006 697812
2007 734002
2008 781426
2009 821658
2010 884839
2011 960842
2012 1026977
2013 1077953
2014 1132104
2015 1174445
2016 1208666
2017 1232146
2018 1276605
2019 1337969
2020 1535064
2021 1679216
2022 1681431
2023 1596744
2024 1640278
2025 1783025
2026 767962
2027 34
2028 5

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38,272,147 results

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Page 1
Turning-ON Proteasomes.
Krahn JH, Kaschani F, Kaiser M. Krahn JH, et al. Cell Chem Biol. 2017 Jun 22;24(6):653-655. doi: 10.1016/j.chembiol.2017.06.005. Cell Chem Biol. 2017. PMID: 28644955 Free article.
While proteasome inhibitors are now well-established research tools and chemotherapeutics, proteasome activators are much less explored. ...
While proteasome inhibitors are now well-established research tools and chemotherapeutics, proteasome activators are much less …
Small-molecule inhibitors of proteasome activity.
Gaczynska M, Osmulski PA. Gaczynska M, et al. Methods Mol Biol. 2005;301:3-22. doi: 10.1385/1-59259-895-1:003. Methods Mol Biol. 2005. PMID: 15917622 Review.
Besides being candidates for drugs against cancer, autoimmune diseases, inflammation, or stroke, specific proteasome inhibitors are indispensable tools for biochemical and cell biology investigations of the proteasome and proteasome-ubiquitin system. ...In this chap …
Besides being candidates for drugs against cancer, autoimmune diseases, inflammation, or stroke, specific proteasome inhibitors …
Proteasome regulators: activators and inhibitors.
Huang L, Chen CH. Huang L, et al. Curr Med Chem. 2009;16(8):931-9. doi: 10.2174/092986709787581860. Curr Med Chem. 2009. PMID: 19275603 Free PMC article. Review.
Due to the importance of the proteasome in cellular functions, inhibition or activation of the proteasome could become a useful therapeutic strategy for a variety of diseases. Many proteasome inhibitors have been identified and can be classified into two groups acco …
Due to the importance of the proteasome in cellular functions, inhibition or activation of the proteasome could become a useful therapeutic …
Structural Insights into Salinosporamide a Mediated Inhibition of the Human 20S Proteasome.
Sülzen H, Fajtova P, O'Donoghue AJ, Silhan J, Boura E. Sülzen H, et al. Molecules. 2025 Mar 20;30(6):1386. doi: 10.3390/molecules30061386. Molecules. 2025. PMID: 40142161 Free PMC article.
Marizomib (MZB), also known as salinosporamide A, is a natural gamma-lactam-beta-lactone compound derived from Salinispora tropica and is a potent 20S proteasome covalent inhibitor with demonstrated anticancer properties. Its broad-spectrum inhibition of all three p …
Marizomib (MZB), also known as salinosporamide A, is a natural gamma-lactam-beta-lactone compound derived from Salinispora tropica and is a …
Tripeptide analogues of MG132 as protease inhibitors.
Pehere AD, Nguyen S, Garlick SK, Wilson DW, Hudson I, Sykes MJ, Morton JD, Abell AD. Pehere AD, et al. Bioorg Med Chem. 2019 Jan 15;27(2):436-441. doi: 10.1016/j.bmc.2018.12.022. Epub 2018 Dec 14. Bioorg Med Chem. 2019. PMID: 30581047
The 26S proteasome and calpain are linked to a number of important human diseases. Here, we report a series of analogues of the prototypical tripeptide aldehyde inhibitor MG132 that show a unique combination of high activity and selectivity for calpains over proteasome. .. …
The 26S proteasome and calpain are linked to a number of important human diseases. Here, we report a series of analogues of the proto …
The development and pharmacology of proteasome inhibitors for the management and treatment of cancer.
Ruggeri B, Miknyoczki S, Dorsey B, Hui AM. Ruggeri B, et al. Adv Pharmacol. 2009;57:91-135. doi: 10.1016/S1054-3589(08)57003-7. Epub 2009 Nov 27. Adv Pharmacol. 2009. PMID: 20230760 Review.
The sensitivity of transformed cells to proteasome inhibitors and the successful design of treatment protocols with tolerable, albeit narrow, therapeutic indices have made proteasome inhibition a viable strategy for cancer treatment. ...These agents may expand the c …
The sensitivity of transformed cells to proteasome inhibitors and the successful design of treatment protocols with tolerable, …
Evaluation of antibacterial effect of a cationic porphyrin derivative on Pseudomonas aeruginosa in photodynamic therapy.
Ji H, Dong T, Liang G, Xu H, Wang C, Liu T, Hong G. Ji H, et al. Photodiagnosis Photodyn Ther. 2023 Dec;44:103857. doi: 10.1016/j.pdpdt.2023.103857. Epub 2023 Oct 27. Photodiagnosis Photodyn Ther. 2023. PMID: 37890810 Free article.
BACKGROUND: Pseudomonas aeruginosa is a gram-negative bacterium without spores, and it is one of the pathogens that easily cause secondary infectious diseases when human immune function is low. The purpose of this study is to explore the inhibitory effect of …
BACKGROUND: Pseudomonas aeruginosa is a gram-negative bacterium without spores, and it is one of the pathogens that easily cause secondary i …
Substituted quinolines as noncovalent proteasome inhibitors.
McDaniel TJ, Lansdell TA, Dissanayake AA, Azevedo LM, Claes J, Odom AL, Tepe JJ. McDaniel TJ, et al. Bioorg Med Chem. 2016 Jun 1;24(11):2441-2450. doi: 10.1016/j.bmc.2016.04.005. Epub 2016 Apr 2. Bioorg Med Chem. 2016. PMID: 27112450 Free PMC article.
Screening of a library of diverse heterocyclic scaffolds identified substituted quinolines as inhibitors of the human proteasome. The heterocyclic library was prepared via a novel titanium-catalyzed multicomponent coupling reaction, which rendered a diverse set of i …
Screening of a library of diverse heterocyclic scaffolds identified substituted quinolines as inhibitors of the human proteaso …
Cationic porphyrins are reversible proteasome inhibitors.
Santoro AM, Lo Giudice MC, D'Urso A, Lauceri R, Purrello R, Milardi D. Santoro AM, et al. J Am Chem Soc. 2012 Jun 27;134(25):10451-7. doi: 10.1021/ja300781u. Epub 2012 Jun 6. J Am Chem Soc. 2012. PMID: 22642538 Free article.
The relevance of electrostatics in driving porphyin-proteasome interactions has been confirmed by the observation that the inhibitory efficiency of the cationic macrocycles decreases with the number of positive substituents. We have also investigated various metalloporp …
The relevance of electrostatics in driving porphyin-proteasome interactions has been confirmed by the observation that the inhibitory effici …
Rational design of drug-like compounds targeting Mycobacterium marinum MelF protein.
Dharra R, Talwar S, Singh Y, Gupta R, Cirillo JD, Pandey AK, Kulharia M, Mehta PK. Dharra R, et al. PLoS One. 2017 Sep 5;12(9):e0183060. doi: 10.1371/journal.pone.0183060. eCollection 2017. PLoS One. 2017. PMID: 28873466 Free PMC article.
After establishing the flavin dependent oxidoreductase activity of MelF (~ 84 kDa), the inhibitors were screened for the inhibition of enzyme activity of whole cell lysate (WCL) and the purified MelF. Amongst these, 16 compounds could significantly inhibit the en …
After establishing the flavin dependent oxidoreductase activity of MelF (~ 84 kDa), the inhibitors were screened for the inhibition of en …
38,272,147 results
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