2021
DOI: 10.1016/j.bbagen.2020.129828
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Novel inhibitors of human glucose-6-phosphate dehydrogenase (HsG6PD) affect the activity and stability of the protein

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Cited by 6 publications
(12 citation statements)
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“…Finally, it is interesting to mention that notwithstanding the fact that CNZ-3 and CNZ-7 compounds inhibited HpG6PD, they also inhibited the HsG6PD enzyme at high levels ( Supplementary Table S1 ), as previously reported by Ramírez-Nava et al [ 21 ]. Therefore, these compounds were not used in in silico studies as they did not show selective inhibition.…”
Section: Resultssupporting
confidence: 77%
See 1 more Smart Citation
“…Finally, it is interesting to mention that notwithstanding the fact that CNZ-3 and CNZ-7 compounds inhibited HpG6PD, they also inhibited the HsG6PD enzyme at high levels ( Supplementary Table S1 ), as previously reported by Ramírez-Nava et al [ 21 ]. Therefore, these compounds were not used in in silico studies as they did not show selective inhibition.…”
Section: Resultssupporting
confidence: 77%
“…Dr. Gabriel Navarrete-Vázquez from the Pharmacy Faculty of the Autonomous University of the State of Morelos provided the chemical compounds [ 32 ]. These compounds were selected based on the previously reported chemical inhibitors of human G6PD [ 21 ], prepared at a final concentration of 400 μM in 5% dimethyl sulfoxide (DMSO) (Sigma Aldrich, St. Louis, MO, USA), incubated with 0.2 mg/mL of HpG6PD (200 ng total) at 37 °C for two hours, and the HpG6PD residual activity was measured. In addition, the HpG6PD protein was incubated with 5% DMSO and used as a control.…”
Section: Methodsmentioning
confidence: 99%
“…These results indicated that inhibitors caused a rearrangement in the tryptophan residues' microenvironment, altering the protein's 3D structure, provoking a loss of catalytic activity. This same finding was reported in a G6PD study, in which a decrease in fluorescence intensity was observed when the human G6PD protein was incubated in the presence of CNZ-3 [19].…”
Section: Intrinsic and Extrinsic Fluorescence Assayssupporting
confidence: 88%
“…These results indicate that the four compounds caused changes in molar ellipticity (ϕ) at 222 nm (α-helix) and 208 nm (β-folded), revealing an increasing amount of random coil, which could explain the loss in catalytic activity. Despite the absence of studies of inhibitors of the fused TvG6PD::6PGL protein, similar findings have been observed over the human G6PD protein, in which compounds that affected catalytic activity also affected its secondary structure [19].…”
Section: Circular Dichroismsupporting
confidence: 55%
“…Indeed, Compounds 6 and 9 are interesting bioactive compounds for the treatment of diabetes due to their antihyperglycemic effect. Further studies are needed to identify other possible targets in the body [46], in order to fully characterize its polypharmacological profile.…”
Section: Discussionmentioning
confidence: 99%