Screening of a novel free fatty acid receptor 1 (FFAR1) agonist peptide by phage display and machine learning based-amino acid substitution

Yoshioka, Keitaro; Yamashita, Haruki; Shimizu, Kazunori; Shimomura, Sayako; Shibata, Takahiro; Miyazaki, Jun‐ichi; Honda, Hiroyuki

doi:10.1016/j.bbrc.2021.02.142

Cited by 3 publications

(2 citation statements)

References 21 publications

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“…In our group, bioactive peptide screening using a peptide array was performed. − It was confirmed that peptide activity could be improved via AA residue substitution. A cyclic peptide library was recently established and applied for the assay of NGR cyclic cell adhesion peptides .…”

Section: Introductionmentioning

confidence: 93%

Agonist/Antagonist Activity of Oxytocin Variants Obtained from Free Cyclic Peptide Libraries Generated via Amino Acid Substitution

et al. 2021

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We established a method for synthesizing a free cyclic peptide library via peptide array synthesis to demonstrate the sequence activity of cyclic peptides. Variants of the cyclic nonapeptide oxytocin (OXT) were synthesized via residue substitution. Natural amino acids (AAs) were classified into eight groups based on their physical properties and the size of their side chains, and a representative AA from each group was selected for residue substitution. All OXT variants were systematically evaluated for agonist/ antagonist activity. Consequently, no improvement in agonist activity was observed, although substitution of the P4 and P8 residues resulted in decreased activity due to AA substitution. A few OXT variants exhibited antagonistic activity. In particular, the variants with P2 Leu residue substitution (Y2L) and Phe substitutions at residues 4 (Q4F), 5 (N5F), and 7 (P7F) showed high antagonistic activity. Variant Y2W was found to have the highest inhibitory effect, with a dissociation constant of 44 nM, which was comparable to that of the commercial antagonist atosiban (21 nM). Therefore, a free cyclic peptide library constructed via substitution with a natural AA residue was confirmed to be a powerful tool for bioactive peptide screening.

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Section: Introductionmentioning

confidence: 93%

Agonist/Antagonist Activity of Oxytocin Variants Obtained from Free Cyclic Peptide Libraries Generated via Amino Acid Substitution

et al. 2021

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“…The functions of various peptides can be assayed. By using the technology, we developed various bioactive peptides, including a peptide inhibitor of amylase activity (Ochiai et al, 2012;Yamashita et al, 2020), cell death-inducing intracellular peptides (Kozaki et al, 2017(Kozaki et al, , 2020Matsumoto et al, 2015), and a peptide ligand to the free fatty acid receptor 1 (FFAR1) (Yoshioka et al, 2021).…”

Section: Introductionmentioning

confidence: 99%

Screening of anti‐atrophic peptides by using photo‐cleavable peptide array and 96‐well scale contractile human skeletal muscle atrophy models

Yamamoto

Ohsumi

Nagashima

et al. 2022

Biotech & Bioengineering

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Skeletal muscle atrophy is characterized by decreases in protein content, myofiber diameter, and contractile force generation. As muscle atrophy worsens the quality of life, the development of anti‐atrophic substances is desirable. In this study, we aimed to demonstrate a screening process for anti‐atrophic peptides using photo‐cleavable peptide array technology and human contractile atrophic muscle models. We developed a 96‐well system and established a screening process with less variability. Dexamethasone‐induced human atrophic tissue was constructed in the system. Eight peptides were selected from the literature and used for the screening of peptides for preventing the decrease of the contractile forces of tissues. The peptide QIGFIW, which showed preventive activity, was selected as the seed sequence. As a result of amino acid substitution, we obtained QIGFIQ as a peptide with higher anti‐atrophic activity. These results indicate that the combinatorial use of the photo‐cleavable peptide array technology and 96‐well screening system could comprise a powerful approach to obtaining anti‐atrophic peptides, and suggest that the 96‐well screening system and atrophic model represent a practical and powerful tool for the development of drugs/functional food ingredients.

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Screening of Anti-Atrophic Peptides by Using Photo-Cleavable Peptide Array and 96-Well Scale Contractile Human Skeletal Muscle Atrophy Models

Yamamoto¹,

Ohsumi²,

Nagashima³

et al. 2022

SSRN Journal

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Screening of a novel free fatty acid receptor 1 (FFAR1) agonist peptide by phage display and machine learning based-amino acid substitution

Cited by 3 publications

References 21 publications

Agonist/Antagonist Activity of Oxytocin Variants Obtained from Free Cyclic Peptide Libraries Generated via Amino Acid Substitution

Agonist/Antagonist Activity of Oxytocin Variants Obtained from Free Cyclic Peptide Libraries Generated via Amino Acid Substitution

Screening of anti‐atrophic peptides by using photo‐cleavable peptide array and 96‐well scale contractile human skeletal muscle atrophy models

Screening of Anti-Atrophic Peptides by Using Photo-Cleavable Peptide Array and 96-Well Scale Contractile Human Skeletal Muscle Atrophy Models

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