PyrGF and GSTLN peptides enhance pravastatin's inhibition of 3-hydroxy-3-methyl-glutaryl coenzyme

Silva, Jaff Ribeiro da; Silva, Mariana Barros de Cerqueira e; Philadelpho, Biane Oliveira; Souza, Victória Cruz de; Santos, Johnnie; Castilho, Marcelo Santos; Ferreira, Ederlan de Souza; Cilli, Eduardo Maffud

doi:10.1016/j.fbio.2021.101451

Cited by 5 publications

(3 citation statements)

References 37 publications

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“…generated the Pyr-GF and GSTLN peptides, analogues of QGF and GCTLN, respectively, showing higher HMG-CoAR activity inhibition in vitro than the original peptides with a dose-dependent inhibitory effect (Figure 3) (47). In particular, Pyr-GF binds to the active site of the enzyme, while GSTLN peptide interacts with the NADPH binding site.…”

Section: Cowpeamentioning

confidence: 99%

“…In this sense, Alsina et al concluded that residues with positive charges in the active site pocket of the enzyme, such as lysine (Lys) and arginine (Arg), may be involved in the interactions with the C-terminus of these peptides (48). Given that GSTLN/GCTLN binds to the S-domain and pravastatin binds to the L-domain of the enzyme, the combined use could increase the HMG-CoAR activity inhibition by a synergistic effect (47).…”

Section: Cowpeamentioning

confidence: 99%

“…Several authors have considered low MW, the presence of proline, a negative group in the C-terminal portion, and/or a hydrophobic group N-terminal important characteristics for the interaction peptide-enzyme and therefore for the enzyme inhibition (47,63,78). On the other hand, there are contrasting opinions on the importance of hydrophobicity (Ho) in enzyme inhibition (63,85,86).…”

Section: Analysis Of the Physicochemical Characteristics Of The Hmg-c...mentioning

confidence: 99%

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Food-derived peptides with inhibitory capacity for HMG-CoA reductase activity: a potential nutraceutical for hypercholesterolemia

Sánchez,

López,

España

et al. 2024

Food Science and Human Wellness

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Cardiovascular diseases (CVDs) are the leading global cause of mortality and disease burden. Statins are the most prescribed lipid-lowering drugs to treat hypercholesterolemia and prevent CVDs. The biochemical mechanism of statins consists of competitive inhibition of the 3-hydroxy-3-methylglutaryl-CoA reductase enzyme (HMG-CoAR), the limiting enzyme in cholesterol biosynthesis. Due to statin intolerance in some patient groups, the search for new inhibitors is a field of great interest. This review focusses on the studies reporting the inhibitory effect of protein hydrolysates and biopeptides on the HMG-CoAR enzyme activity. The analysis of the action mechanism and physicochemical characteristics of the HMG-CoAR inhibitory peptides revealed that the molecular weight, amino acid composition, charge, and polarity are key aspects of the interaction with the HMG-CoAR enzyme. In conclusion, this review reveals the potential of using food peptides as new cholesterol-lowering agents and opens a new interesting field of research. However, clinical approaches are mandatory to confirm their therapeutic hypercholesterolemic effect.

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Section: Cowpeamentioning

confidence: 99%

Section: Cowpeamentioning

confidence: 99%