Peptide-Based Regulation of TNF-α-Mediated Cytotoxicity

Tumor necrosis factor alpha (TNF-α) is a pro-inflammatory cytokine associated with TNF receptor 1 (TNFR1) and TNF receptor 2 (TNFR2), which play important roles in several inflammatory diseases. There is a growing interest in developing alternative molecules that can be used as TNF blockers. In this...

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Main Authors: Betul Zehra Temur, Ahmet Can Timucin, Ahmet Emin Atik, Tanil Kocagoz, Ozge Can
Format: Article
Language:English
Published: MDPI AG 2025-04-01
Series:Biomolecules
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Online Access:https://www.mdpi.com/2218-273X/15/4/559
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author Betul Zehra Temur
Ahmet Can Timucin
Ahmet Emin Atik
Tanil Kocagoz
Ozge Can
author_facet Betul Zehra Temur
Ahmet Can Timucin
Ahmet Emin Atik
Tanil Kocagoz
Ozge Can
author_sort Betul Zehra Temur
collection DOAJ
description Tumor necrosis factor alpha (TNF-α) is a pro-inflammatory cytokine associated with TNF receptor 1 (TNFR1) and TNF receptor 2 (TNFR2), which play important roles in several inflammatory diseases. There is a growing interest in developing alternative molecules that can be used as TNF blockers. In this study, we focused on TNF-α-, TNFR1-, and TNFR2-mimicking peptides to inhibit TNF-α receptor binding in various ways. Six peptides (OB1, OB2, OB5, OB6, OB7, and OB8) were developed to bind TNFR1, TNFR2, and TNF-α. OB1 and OB2 bound to TNF-α with lower <i data-eusoft-scrollable-element="1">K</i><sub data-eusoft-scrollable-element="1">d</sub> values of 300 and 46.7 nM, respectively, compared to previously published sequences. These synthetic peptides directly and indirectly inhibited TNF-α in vitro without cytotoxicity to L929 cells, and OB1 significantly inhibited apoptosis in the presence of hTNF-α. Peptides developed in this study may prove to be useful for therapeutic inhibition of TNF-α.
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spelling doaj-art-3bcce3b1baad4dcebfd00ee48787c4342025-08-20T02:17:20ZengMDPI AGBiomolecules2218-273X2025-04-0115455910.3390/biom15040559Peptide-Based Regulation of TNF-α-Mediated CytotoxicityBetul Zehra Temur0Ahmet Can Timucin1Ahmet Emin Atik2Tanil Kocagoz3Ozge Can4Department of Medical Biotechnology, Institute of Health Sciences, Acibadem Mehmet Ali Aydinlar University, Atasehir, 34752 Istanbul, TurkeyDepartment of Molecular Biology and Genetics, Faculty of Engineering and Natural Sciences, Acibadem Mehmet Ali Aydinlar University, Atasehir, 34752 İstanbul, TurkeyTurgut Ilaclari A.S., 41400 Kocaeli, TurkeyDepartment of Medical Biotechnology, Institute of Health Sciences, Acibadem Mehmet Ali Aydinlar University, Atasehir, 34752 Istanbul, TurkeyDepartment of Biomedical Engineering, Faculty of Engineering and Natural Sciences, Acibadem Mehmet Ali Aydinlar University, Atasehir, 34752 Istanbul, TurkeyTumor necrosis factor alpha (TNF-α) is a pro-inflammatory cytokine associated with TNF receptor 1 (TNFR1) and TNF receptor 2 (TNFR2), which play important roles in several inflammatory diseases. There is a growing interest in developing alternative molecules that can be used as TNF blockers. In this study, we focused on TNF-α-, TNFR1-, and TNFR2-mimicking peptides to inhibit TNF-α receptor binding in various ways. Six peptides (OB1, OB2, OB5, OB6, OB7, and OB8) were developed to bind TNFR1, TNFR2, and TNF-α. OB1 and OB2 bound to TNF-α with lower <i data-eusoft-scrollable-element="1">K</i><sub data-eusoft-scrollable-element="1">d</sub> values of 300 and 46.7 nM, respectively, compared to previously published sequences. These synthetic peptides directly and indirectly inhibited TNF-α in vitro without cytotoxicity to L929 cells, and OB1 significantly inhibited apoptosis in the presence of hTNF-α. Peptides developed in this study may prove to be useful for therapeutic inhibition of TNF-α.https://www.mdpi.com/2218-273X/15/4/559TNF-αTNF-α receptorsTNF-α-binding peptideTNFR1-binding peptideTNFR2-binding peptideTNF-α inhibition
spellingShingle Betul Zehra Temur
Ahmet Can Timucin
Ahmet Emin Atik
Tanil Kocagoz
Ozge Can
Peptide-Based Regulation of TNF-α-Mediated Cytotoxicity
Biomolecules
TNF-α
TNF-α receptors
TNF-α-binding peptide
TNFR1-binding peptide
TNFR2-binding peptide
TNF-α inhibition
title Peptide-Based Regulation of TNF-α-Mediated Cytotoxicity
title_full Peptide-Based Regulation of TNF-α-Mediated Cytotoxicity
title_fullStr Peptide-Based Regulation of TNF-α-Mediated Cytotoxicity
title_full_unstemmed Peptide-Based Regulation of TNF-α-Mediated Cytotoxicity
title_short Peptide-Based Regulation of TNF-α-Mediated Cytotoxicity
title_sort peptide based regulation of tnf α mediated cytotoxicity
topic TNF-α
TNF-α receptors
TNF-α-binding peptide
TNFR1-binding peptide
TNFR2-binding peptide
TNF-α inhibition
url https://www.mdpi.com/2218-273X/15/4/559
work_keys_str_mv AT betulzehratemur peptidebasedregulationoftnfamediatedcytotoxicity
AT ahmetcantimucin peptidebasedregulationoftnfamediatedcytotoxicity
AT ahmeteminatik peptidebasedregulationoftnfamediatedcytotoxicity
AT tanilkocagoz peptidebasedregulationoftnfamediatedcytotoxicity
AT ozgecan peptidebasedregulationoftnfamediatedcytotoxicity