About: PT150 is a modulator of glucocorticoid and androgen receptors with antiviral activity against SARS-CoV-2

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About: PT150 is a modulator of glucocorticoid and androgen receptors with antiviral activity against SARS-CoV-2 Goto Sponge NotDistinct Permalink

An Entity of Type : schema:ScholarlyArticle, within Data Space : covidontheweb.inria.fr associated with source document(s)

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type	Academic Article research paper schema:ScholarlyArticle
isDefinedBy	Covid-on-the-Web dataset
title	PT150 is a modulator of glucocorticoid and androgen receptors with antiviral activity against SARS-CoV-2
Creator	Westover, Jonna Arment, Anthony Chakravarty, Dimple Gregg, John Jacobson, Ira »more»
source	BioRxiv
abstract	PT150 is a clinical stage molecule, taken orally, with a strong safety profile having completed Phase 1 and Phase 2 clinical trials for its original use as an anti-depressant. It has an active IND for COVID-19. Antiviral activities have been found for PT150 and other members of its class in a variety of virus families; thus, it was now tested against SARS-CoV-2 in human bronchial epithelial lining cells and showed effective 90% inhibitory antiviral concentration (EC90) of 5.55 μM. PT150 is a member of an extended platform of novel glucocorticoid receptor (GR) and androgen receptor (AR) binding molecules. In vivo, their predominant net effect is one of systemic glucocorticoid antagonism, but they also show direct downregulation of AR and minor GR agonism at the cellular level. We hypothesize that anti-SARS-CoV-2 activity depends in part on this AR downregulation through diminished TMPRSS2 expression and modulation of ACE2 activity. Given that hypercortisolemia is now suggested to be a significant co-factor for COVID-19 progression, we also postulate an additive role for its potent immunomodulatory effects through systemic antagonism of cortisol.
has issue date	2020-07-13(xsd:dateTime)
bibo:doi	10.1101/2020.07.12.199505
has license	biorxiv
sha1sum (hex)	58d93687e89aa90228176d0461a87b9e5e097243
schema:url	https://doi.org/10.1101/2020.07.12.199505
resource representing a document's title	PT150 is a modulator of glucocorticoid and androgen receptors with antiviral activity against SARS-CoV-2
schema:publication	bioRxiv
resource representing a document's body	covid:58d93687e89aa90228176d0461a87b9e5e097243#body_text
is schema:about of	named entity 'activities' named entity 'virus' named entity 'activity' named entity 'GLUCOCORTICOID RECEPTOR' named entity 'HAVE' »more»

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