Pharmacokinetics


Last updated: 2021 Aug 23
Total hit(s): 4
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Original Article
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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) nameZhao MM, Yang WL et al.
Journal Signal Transduct Target Ther
Impact factor
- n/a -
Citation count: 73
Date of Entry 2021 Aug 23


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) nameZhao MM, Yang WL et al.
Journal Signal Transduct Target Ther
Impact factor
- n/a -
Citation count: 73
Date of Entry 2021 Aug 23


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) nameZhang L, Lin D et al.
Journal Science
Impact factor
20.57
Citation count: 1159


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) nameZhang L, Lin D et al.
Journal Science
Impact factor
20.57
Citation count: 1159