Pharmacokinetics


Last updated: 2021 Aug 23
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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