Synthesis and investigation of the derivatives of amidinohydrazonelated aromatic compounds as furin inhibitors

Osadchuk, T. V.; Semyroz, A. V.; Shybyryn, O. V.; Kibirev, V. K.

doi:10.15407/ubj89.06.003

Cited by 1 publication

(4 citation statements)

References 26 publications

(31 reference statements)

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“… 208 These compounds were suggested to act through mixed inhibition, but their K i values were in the micromolar range. 208 …”

Section: Furin Inhibitorsmentioning

confidence: 99%

“…The C-terminal segment is more loosely bound and may dissociate readily after hydrolysis . Furin and furin-like PC enzymes are extensively investigated as drug targets. , Reported inhibitors include peptide-derived compounds, − peptidomimetic, − and nonpeptidic small-molecule compounds. ,− …”

Section: Substrate Binding Site Of Furin and The Mechanism Of Proteas...mentioning

confidence: 99%

“…A closely related series of bisamidinohydrazones were recently reported featuring a 1,3-bisphenoxypropane spacer exemplified by D7 and D8 (Figure 25). 208 These compounds were suggested to act through mixed inhibition, but their K i values were in the micromolar range. 208 Phenylpyridinylmethylpiperidines and Piperazines.…”

Section: ■ Furin Inhibitorsmentioning

confidence: 99%

“…208 These compounds were suggested to act through mixed inhibition, but their K i values were in the micromolar range. 208 Phenylpyridinylmethylpiperidines and Piperazines. A large series of substituted phenylpyridinylmethylpiperidines, phenylpyridinylmethyl piperazines, and their analogs were reported as furin inhibitors (Figures 26 and 27).…”

Section: ■ Furin Inhibitorsmentioning

confidence: 99%

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Why All the Fury over Furin?

2021

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Analysis of the SARS-CoV-2 sequence revealed a multibasic furin cleavage site at the S1/S2 boundary of the spike protein distinguishing this virus from SARS-CoV. Furin, the best-characterized member of the mammalian proprotein convertases, is an ubiquitously expressed single pass type 1 transmembrane protein. Cleavage of SARS-CoV-2 spike protein by furin promotes viral entry into lung cells. While furin knockout is embryonically lethal, its knockout in differentiated somatic cells is not, thus furin provides an exciting therapeutic target for viral pathogens including SARS-CoV-2 and bacterial infections. Several peptide-based and small-molecule inhibitors of furin have been recently reported, and select cocrystal structures have been solved, paving the way for further optimization and selection of clinical candidates. This perspective highlights furin structure, substrates, recent inhibitors, and crystal structures with emphasis on furin’s role in SARS-CoV-2 infection, where the current data strongly suggest its inhibition as a promising therapeutic intervention for SARS-CoV-2.

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“… 208 These compounds were suggested to act through mixed inhibition, but their K i values were in the micromolar range. 208 …”

Section: Furin Inhibitorsmentioning

confidence: 99%