| Cathepsin L (CTSL) levels increased in SARS-CoV-2 infected mice's liver.Cathepsin L inhibitor, Amantadine reduced the levels of CTSL. | CTSL levels increased in the lungs of infected mice, on inhibitor treatment, no statistically significant result was observed. ✍ | 33774649 (Signal Transduct Target Ther)
PMID | 33774649 Date of Publishing: 2021 Mar 27 | Title | Cathepsin L plays a key role in SARS-CoV-2 infection in humans and humanized mice and is a promising target for new drug development | Author(s) name | Zhao MM, Yang WL et al. | Journal | Signal Transduct Target Ther | Impact factor | - n/a - Citation count: 73 | Date of Entry | 2021 Aug 23 |
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NLM format |
Zhao MM, Yang WL, Yang FY, Zhang L, Huang WJ, Hou W, Fan CF, Jin RH, Feng YM, Wang YC, Yang JK. Cathepsin L plays a key role in SARS-CoV-2 infection in humans and humanized mice and is a promising target for new drug development. Signal Transduct Target Ther. 2021 Mar 27;6(1):134. PMID:33774649 |
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| Cathepsin L (CTSL) levels increased in SARS-CoV-2 infected mice's liver.Cathepsin L inhibitor, E64d reduced the levels of CTSL. | CTSL levels increased in the lungs of mice infected with the pseudovirus, on inhibitor treatment no statistically significant result was observed. ✍ | 33774649 (Signal Transduct Target Ther)
PMID | 33774649 Date of Publishing: 2021 Mar 27 | Title | Cathepsin L plays a key role in SARS-CoV-2 infection in humans and humanized mice and is a promising target for new drug development | Author(s) name | Zhao MM, Yang WL et al. | Journal | Signal Transduct Target Ther | Impact factor | - n/a - Citation count: 73 | Date of Entry | 2021 Aug 23 |
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NLM format |
Zhao MM, Yang WL, Yang FY, Zhang L, Huang WJ, Hou W, Fan CF, Jin RH, Feng YM, Wang YC, Yang JK. Cathepsin L plays a key role in SARS-CoV-2 infection in humans and humanized mice and is a promising target for new drug development. Signal Transduct Target Ther. 2021 Mar 27;6(1):134. PMID:33774649 |
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| Compound 13a has IC50 of 2.39 ± 0.63 µ;M against SARS-CoV-2 main protease. | 13a was cleared at a rapid rate from plasma, at 24 hours it was found at 135 ng/g tissue in the lung and at 52.7 ng/ml in bronchio-alveolar lavage fluid (BALF), showing it was distributed into the tissues, thus very useful anti-coronavirus drug. ✍ | 32198291 (Science)
PMID | 32198291 Date of Publishing: 2020 Apr 24 | Title | Crystal structure of SARS-CoV-2 main protease provides a basis for design of improved -ketoamide inhibitors | Author(s) name | Zhang L, Lin D et al. | Journal | Science | Impact factor | 20.57 Citation count: 1159 |
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NLM format |
Zhang L, Lin D, Sun X, Curth U, Drosten C, Sauerhering L, Becker S, Rox K, Hilgenfeld R. Crystal structure of SARS-CoV-2 main protease provides a basis for design of improved -ketoamide inhibitors. Science. 2020 Apr 24;368(6489):409-412. PMID:32198291 |
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| Compound 13b inhibits the purified recombinant SARS-CoV-2 Mpro with IC50 = 0.67 ± 0.18 μ;M. In human Calu-3 cells infected with SARS-CoV-2 it has an EC50 of 4 to 5 μ;M. | After 24 hours, 13b was found at 33 ng/g in lung tissue.
Inhalation was tolerated well and mice did not show any adverse effects, which suggests that direct administration of the compound to the lungs would be possible. ✍ | 32198291 (Science)
PMID | 32198291 Date of Publishing: 2020 Apr 24 | Title | Crystal structure of SARS-CoV-2 main protease provides a basis for design of improved -ketoamide inhibitors | Author(s) name | Zhang L, Lin D et al. | Journal | Science | Impact factor | 20.57 Citation count: 1159 |
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NLM format |
Zhang L, Lin D, Sun X, Curth U, Drosten C, Sauerhering L, Becker S, Rox K, Hilgenfeld R. Crystal structure of SARS-CoV-2 main protease provides a basis for design of improved -ketoamide inhibitors. Science. 2020 Apr 24;368(6489):409-412. PMID:32198291 |
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