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

Year Number of Results
1945 2
1946 9
1947 4
1948 11
1949 3
1950 6
1951 13
1952 14
1953 11
1954 12
1955 12
1956 20
1957 20
1958 20
1959 48
1960 47
1961 48
1962 50
1963 437
1964 816
1965 378
1966 17
1967 30
1968 34
1969 61
1970 54
1971 45
1972 46
1973 46
1974 153
1975 179
1976 164
1977 150
1978 156
1979 125
1980 144
1981 118
1982 98
1983 107
1984 113
1985 126
1986 107
1987 151
1988 144
1989 186
1990 175
1991 133
1992 162
1993 151
1994 168
1995 2107
1996 4954
1997 5387
1998 6083
1999 6377
2000 6991
2001 8041
2002 8042
2003 8402
2004 7420
2005 6703
2006 6630
2007 6459
2008 6405
2009 6002
2010 5338
2011 5291
2012 5012
2013 4705
2014 4251
2015 3724
2016 3449
2017 3365
2018 3040
2019 1387
2020 32
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130,572 results
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Page 1
Substrate-selective inhibitors that reprogram the activity of insulin-degrading enzyme.
Maianti JP, et al. Nat Chem Biol 2019. PMID 31086331 Free PMC article.
The metalloprotease insulin-degrading enzyme (IDE) modulates blood glucose levels by cleaving insulin, a hormone that promotes glucose clearance. ...IDE inhibitors to treat diabetes, therefore, should prevent IDE-mediated insulin degradation, but not glucagon degradation, in contrast with traditional modes of enzyme inhibition. ...
The metalloprotease insulin-degrading enzyme (IDE) modulates blood glucose levels by cleaving insulin, a hormone that promotes glucos …
Targeted protein degradation: expanding the toolbox
Schapira M, et al. Nat Rev Drug Discov 2019. PMID 31666732
Proteolysis-targeting chimeras (PROTACs) and related molecules that induce targeted protein degradation by the ubiquitin-proteasome system represent a new therapeutic modality and are the focus of great interest, owing to potential advantages over traditional occupancy-based inhibitors with respect to dosing, side effects, drug resistance and modulating 'undruggable' targets. ...
Proteolysis-targeting chimeras (PROTACs) and related molecules that induce targeted protein degradation by the ubiquitin-proteasome system r …
Multi-target-directed-ligands acting as enzyme inhibitors and receptor ligands.
Rodríguez-Soacha DA, et al. Eur J Med Chem 2019 - Review. PMID 31401465
In particular, latest findings in the field of MTDL design targeting both an enzyme and a receptor are presented for different diseases such as Alzheimer's disease (AD), depression, addiction, glaucoma, non-alcoholic steatohepatitis and pain and inflammation. ...
In particular, latest findings in the field of MTDL design targeting both an enzyme and a receptor are presented for different diseas …
Gut microbiome-derived phenyl sulfate contributes to albuminuria in diabetic kidney disease
Kikuchi K, et al. Nat Commun 2019. PMID 31015435 Free PMC article.
Inhibition of tyrosine phenol-lyase, a bacterial enzyme responsible for the synthesis of phenol from dietary tyrosine before it is metabolized into phenyl sulfate in the liver, reduces albuminuria in diabetic mice. ...
Inhibition of tyrosine phenol-lyase, a bacterial enzyme responsible for the synthesis of phenol from dietary tyrosine before it is me …
Development of human cGAS-specific small-molecule inhibitors for repression of dsDNA-triggered interferon expression.
Lama L, et al. Nat Commun 2019. PMID 31113940 Free PMC article.
Therefore, inhibition of the enzyme cGAS may act anti-inflammatory. Here we report the discovery of human-cGAS-specific small-molecule inhibitors by high-throughput screening and the targeted medicinal chemistry optimization for two molecular scaffolds. ...These novel cGAS inhibitors with cell-based activity will serve as probes into cGAS-dependent innate immune pathways and warrant future pharmacological studies for treatment of cGAS-dependent inflammatory diseases....
Therefore, inhibition of the enzyme cGAS may act anti-inflammatory. Here we report the discovery of human-cGAS-specific small-molecul …
Natural Tyrosinase Inhibitors: Role of Herbals in the Treatment of Hyperpigmentary Disorders.
Zaidi KU, et al. Mini Rev Med Chem 2019 - Review. PMID 31244414
Tyrosinase inhibitors are molecules that interrelate in some way with the enzyme to prevent it from working in the normal manner. Past many decades witnessed the quest for the development of natural tyrosinase inhibitors due to imperative role played by tyrosinase in the process of melanogenesis and fungi or fruit enzymatic browning. ...
Tyrosinase inhibitors are molecules that interrelate in some way with the enzyme to prevent it from working in the normal mann …
An l-glutaminase enzyme reactor based on porous bamboo sticks and its application in enzyme inhibitors screening.
Qiao J, et al. Talanta 2019. PMID 31450397
Inspired by the porous and fibrous structure of commercially available bamboo, herein we created an l-glutaminase enzyme reactor based on bamboo sticks. The enzyme was immobilized onto the bamboo sticks through a glutaraldehyde modification to achieve covalent bonding. The enzymatic hydrolysis efficiency of the prepared l-glutaminase@bamboo sticks based porous enzyme reactor was evaluated by chiral ligand exchange capillary electrochromatography using l-glutamine as the substrate. l-glutaminase@bamboo exhibited improved enzymatic hydrolysis performances, including high hydrolysis efficiency (maximum rate V(max): two fold higher than the free enzyme), prolonged stability (14 days) and good reusability. l-Glutaminase@bamboo sticks also expanded application capability in pharmaceutical industry in enzyme inhibitor screening. ...
Inspired by the porous and fibrous structure of commercially available bamboo, herein we created an l-glutaminase enzyme reactor base …
130,572 results
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