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

Year Number of Results
1945 1
1946 1
1947 2
1948 2
1949 6
1950 2
1951 2
1952 6
1954 3
1955 1
1956 12
1957 7
1958 5
1959 10
1960 18
1961 10
1962 15
1963 12
1964 10
1965 6
1966 6
1967 44
1968 66
1969 98
1970 78
1971 128
1972 169
1973 165
1974 164
1975 124
1976 161
1977 161
1978 225
1979 297
1980 285
1981 325
1982 353
1983 455
1984 462
1985 481
1986 519
1987 536
1988 511
1989 540
1990 461
1991 437
1992 432
1993 381
1994 383
1995 508
1996 647
1997 642
1998 647
1999 650
2000 626
2001 655
2002 645
2003 697
2004 752
2005 767
2006 791
2007 778
2008 783
2009 765
2010 792
2011 791
2012 728
2013 663
2014 586
2015 504
2016 416
2017 404
2018 352
2019 169
2020 4
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23,227 results
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Page 1
Proteases and protease inhibitors in infectious diseases.
Agbowuro AA, et al. Med Res Rev 2018 - Review. PMID 29149530
While a few of these enzymes including HIV protease and HCV NS3-4A protease have been targeted to a clinically useful level, a number are yet to yield any clinical outcomes in terms of antimicrobial therapy. ...We assess the mechanism of action and clinical performance of the protease inhibitors against infectious agents with their developmental strategies and look to the next frontiers in the use of protease inhibitors as anti-infective agents....
While a few of these enzymes including HIV protease and HCV NS3-4A protease have been targeted to a clinically useful l …
Protease inhibitors broadly effective against feline, ferret and mink coronaviruses.
Perera KD, et al. Antiviral Res 2018. PMID 30342822 Free PMC article.
We have previously reported the efficacy of a protease inhibitor in cats with FIP, demonstrating that a virally encoded 3C-like protease (3CLpro) is a valid target for antiviral drug development for coronavirus infections. In this study, we extended our previous work on coronavirus inhibitors and investigated the structure-activity relationships of a focused library of protease inhibitors for ferret and mink 3CLpro. ...
We have previously reported the efficacy of a protease inhibitor in cats with FIP, demonstrating that a virally encoded …
Strategies Towards Protease Inhibitors for Emerging Flaviviruses.
Nitsche C. Adv Exp Med Biol 2018 - Review. PMID 29845533
Among others, the flaviviral protease NS2B-NS3 is a promising drug target to inhibit viral replication. Flaviviral proteases share a high degree of structural similarity and substrate-recognition profile, which may facilitate a strategy towards development of pan-flaviviral protease inhibitors. ...Small-molecular, structurally diverse protease inhibitors have been reported to reach affinities in the lower micromolar range. ...
Among others, the flaviviral protease NS2B-NS3 is a promising drug target to inhibit viral replication. Flaviviral prot …
Distinct effects of HIV protease inhibitors and ERAD inhibitors on zygote to ookinete transition of the malaria parasite.
Goulielmaki E, et al. Mol Biochem Parasitol 2018. PMID 29305880
In this study we tested the putative effect of three HIV protease inhibitors, two general aspartyl protease inhibitors and three AAA-p97 ATPase inhibitors on the zygote to ookinete transition of the Plasmodium parasite. ...Our results highlight a potential of HIV protease inhibitors and p97 inhibitors as transmission blocking agents for the eradication of malaria....
In this study we tested the putative effect of three HIV protease inhibitors, two general aspartyl protease i
Protease Inhibitors and Cardiovascular Outcomes in Patients With HIV and Heart Failure.
Alvi RM, et al. J Am Coll Cardiol 2018. PMID 30049313 Free PMC article.
BACKGROUND: Incident heart failure (HF) is increased in persons with human immunodeficiency virus (PHIV). Protease inhibitors (PIs) are associated with adverse cardiac remodeling and vascular events; however, there are no data on the use of PIs in PHIV with HF. ...Predictors of CV mortality included PI use, CAD, PASP, and immunosuppression. Overall, PIs were associated with a 2-fold increased risk of CV mortality. ...
BACKGROUND: Incident heart failure (HF) is increased in persons with human immunodeficiency virus (PHIV). …
Novel highly selective inhibitors of ubiquitin specific protease 30 (USP30) accelerate mitophagy.
Kluge AF, et al. Bioorg Med Chem Lett 2018. PMID 29935771
USP30 is an enzyme that de-ubiquitinates mitochondrial proteins; therefore, inhibiting this enzyme could foster mitophagy. Herein, we disclose the structure-activity relationships (SAR) within a novel series of highly selective USP30 inhibitors. ...We show that MF-094 increases protein ubiquitination and accelerates mitophagy....
USP30 is an enzyme that de-ubiquitinates mitochondrial proteins; therefore, inhibiting this enzyme could foster mitophagy. Her …
Discovery and characterization of highly potent and selective allosteric USP7 inhibitors.
Gavory G, et al. Nat Chem Biol 2018. PMID 29200206
Given the importance of ubiquitin-specific protease 7 (USP7) in oncogenic pathways, identification of USP7 inhibitors has attracted considerable interest. ...In this article, we describe the identification, optimization and detailed characterization of highly potent (IC(50) < 10 nM), selective USP7 inhibitors together with their less active, enantiomeric counterparts. ...
Given the importance of ubiquitin-specific protease 7 (USP7) in oncogenic pathways, identification of USP7 in
Structures of Zika virus NS2B-NS3 protease in complex with peptidomimetic inhibitors.
Phoo WW, et al. Antiviral Res 2018. PMID 30315877
Zika virus NS2B-NS3 protease plays an essential role in viral replication by processing the viral polyprotein into individual proteins. ...These new structures of protease-inhibitor complexes will guide the design of more effective NS2B-NS3 protease inhibitors with improved potency and bioavailability....
Zika virus NS2B-NS3 protease plays an essential role in viral replication by processing the viral polyprotein into i
Hepatitis C - New drugs and treatment prospects
Zając M, et al. Eur J Med Chem 2019 - Review. PMID 30685524
In the 1990s, interferons alpha-2 were used in the treatment of HCV and in the next decade HCV therapy was based on pegylated interferon alpha-2 in combination with ribavirin. Since 2011, interferons alpha, DNA and RNA polymerase inhibitors, NS3/4A RNA protease inhibitors, NS5 RNA serine protease inhibitors, NS5B RNA polymerase inhibitors have been approved for clinical use. ...
In the 1990s, interferons alpha-2 were used in the treatment of HCV and in the next decade HCV therapy was based
DPP8/DPP9 inhibitor-induced pyroptosis for treatment of acute myeloid leukemia.
Johnson DC, et al. Nat Med 2018. PMID 29967349 Free PMC article.
In mouse myeloid cells, Dpp8/9 inhibition activates the inflammasome sensor Nlrp1b, which in turn activates pro-caspase-1 to mediate cell death(3), but the mechanism of DPP8/9 inhibitor-induced pyroptosis in human myeloid cells is not yet known. ...We further show that DPP8/9 inhibitors induce pyroptosis in the majority of human acute myeloid leukemia (AML) cell lines and primary AML samples, but not in cells from many other lineages, and that these inhibitors inhibit human AML progression in mouse models. ...
In mouse myeloid cells, Dpp8/9 inhibition activates the inflammasome sensor Nlrp1b, which in turn activates pro-
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