LitCovid-sentences  

PMC:7796052 / 4511-6254 JSONTXT 3 Projects

Annnotations TAB TSV DIC JSON TextAE Lectin_function

Id Subject Object Predicate Lexical cue
T29 0-151 Sentence denotes The virtual screening process permitted the identification of a small set of drugs as prospective nonselective BK ligands, as described elsewhere [24].
T30 152-320 Sentence denotes Specifically, the DrugBank database, containing a total of 1703 molecules, was screened for compounds that fulfilled a common pharmacophore for the B1 and B2 receptors.
T31 321-458 Sentence denotes The study identified eight drugs including raloxifene, sildenafil, cefepime, cefpirome, imatinib, ponatinib, abemaciclib and entrectinib.
T32 459-641 Sentence denotes Subsequently, the eight compounds were purchased and tested for their capacity to displace a reference ligand in any of the two bradykinin receptors B1 and B2, respectively at 20 µM.
T33 642-820 Sentence denotes Three of the compounds including raloxifene, sildenafil and cefepime displaced the reference ligand from B2, which represents a 40% success rate as found in similar studies [29].
T34 821-913 Sentence denotes However, none of the compounds exhibited affinity for the B1 receptor at this concentration.
T35 914-1019 Sentence denotes This might be due to the steric hindrance that was not properly included in the virtual screening search.
T36 1020-1156 Sentence denotes Raloxifene, the most potent antagonist identified was further investigated in a functional study in vitro, exhibiting an IC50 of ~16 µM.
T37 1157-1250 Sentence denotes Moreover, the compound showed a weak partial agonist profile with a maximal activity of ~20%.
T38 1251-1416 Sentence denotes Ralixofene is a selective estrogen receptor modulator, exerting estrogen agonist action in some target tissues while acting as an estrogen antagonist in others [30].
T39 1417-1556 Sentence denotes The compound was approved a few years ago for the treatment of osteoporosis in postmenopausal women, as well as for cancer chemoprotection.
T40 1557-1743 Sentence denotes The discovery of a new pharmacodynamic profile of relixofene as a BK partial agonist opens an opportunity for its repurposing as a therapeutic agent for the treatment of severe Covid-19.