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Enzalutamide inhibits TMPRSS2. 13 / 13
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"Using lentivirus-pseudotyped and authentic HCoV, we report that enzalutamide reduced 229E and NL63 entry and infection in both TMPRSS2- and nonexpressing immortalized cells, suggesting a TMPRSS2-independent mechanism."
38529542
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"R1881-stimulated expression of AR-target genes FKBP5 , STEAP4 , and TMPRSS2 was inhibited by enzalutamide and UT-105 ( xref )."
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"Camostat mesilate and enzalutamide have been reported to inhibit TMPRSS2 in vitro, and at present, they are in phase 2 clinical trials (NCT04455815 and NCT04475601, respectively)."
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"Notably , unlike in LNCaP cells , in which DHT stimulated and enzalutamide reduced TMPRSS2 expression , no obvious changes in mRNA expression of TMPRSS2 were observed in H2126 and H1437 cells treated with these two agents ( Supplementary Fig. 5c-f ) ."
33558541
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"Distinct from results in LNCaP cells that DHT stimulated TMPRSS2 expression and enzalutamide reduced TMPRSS2 expression , respectively , no obvious changes in TMPRSS2 expression were observed in H2126 and H1437 cells with these two treatments ( Supplementary Fig. 5g ) ."
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"The antiandrogen enzalutamide downregulates TMPRSS2 and reduces cellular entry of SARS-CoV-2 in human lung cells.Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), the cause of the COVID-19 pandemic, is a positive-sense single-stranded RNA coronavirus highly related to SARS-CoV, which caused the 2002/2003 SARS pandemic1,2."
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"R1881-stimulated expression of AR-target genes FKBP5, STEAP4, and TMPRSS2 was inhibited by enzalutamide and UT-105 (Fig. 3G)."
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"Both RD162 and MDV3100 antagonized induction of PSA and TMPRSS2 by the synthetic androgen R1881 in parental LNCaP cells (XREF_SUPPLEMENTARY)."
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"Consistently , enzalutamide significantly decreased TMPRSS2 expression and inhibited SARS-CoV-2 infection in human prostate cancer cells ( Fig. 2 ) ."
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"On the other hand , TMPRSS2 was induced significantly upon DHT exposure and was suppressed by enzalutamide or WBM ."
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"The antiandrogen enzalutamide downregulates TMPRSS2 and reduces cellular entry of SARS-CoV-2 in human lung cells."
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"In line with this , enzalutamide ( an androgen receptor antagonist ) , estradiol , and the phytoestrogen genistein were recently reported to downregulate the expression of TMPRSS2 using RNA sequencing data derived from human prostate , breast , and endometrial cancer cell lines ."
33369210
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"Thus , an AR inhibitor , enzalutamide can reduce TMPRSS2 expression , subsequently resulting in the attenuated entry driven by SARS-CoV-2 ."
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