{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,6,5]],"date-time":"2026-06-05T12:40:30Z","timestamp":1780663230709,"version":"3.54.1"},"reference-count":44,"publisher":"MDPI AG","issue":"3","license":[{"start":{"date-parts":[[2024,2,24]],"date-time":"2024-02-24T00:00:00Z","timestamp":1708732800000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"funder":[{"DOI":"10.13039\/501100018542","name":"Natural Science Foundation of Sichuan Province","doi-asserted-by":"publisher","award":["2022NSFSC0579"],"award-info":[{"award-number":["2022NSFSC0579"]}],"id":[{"id":"10.13039\/501100018542","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/501100018542","name":"Natural Science Foundation of Sichuan Province","doi-asserted-by":"publisher","award":["31970423"],"award-info":[{"award-number":["31970423"]}],"id":[{"id":"10.13039\/501100018542","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/501100018542","name":"Natural Science Foundation of Sichuan Province","doi-asserted-by":"publisher","award":["32071242"],"award-info":[{"award-number":["32071242"]}],"id":[{"id":"10.13039\/501100018542","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/501100018542","name":"Natural Science Foundation of Sichuan Province","doi-asserted-by":"publisher","award":["32200379"],"award-info":[{"award-number":["32200379"]}],"id":[{"id":"10.13039\/501100018542","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/501100001809","name":"National Natural Science Foundation of Chin","doi-asserted-by":"publisher","award":["2022NSFSC0579"],"award-info":[{"award-number":["2022NSFSC0579"]}],"id":[{"id":"10.13039\/501100001809","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/501100001809","name":"National Natural Science Foundation of Chin","doi-asserted-by":"publisher","award":["31970423"],"award-info":[{"award-number":["31970423"]}],"id":[{"id":"10.13039\/501100001809","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/501100001809","name":"National Natural Science Foundation of Chin","doi-asserted-by":"publisher","award":["32071242"],"award-info":[{"award-number":["32071242"]}],"id":[{"id":"10.13039\/501100001809","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/501100001809","name":"National Natural Science Foundation of Chin","doi-asserted-by":"publisher","award":["32200379"],"award-info":[{"award-number":["32200379"]}],"id":[{"id":"10.13039\/501100001809","id-type":"DOI","asserted-by":"publisher"}]}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Toxins"],"abstract":"<jats:p>Toll-like receptor 4 (TLR4) is a crucial inflammatory signaling pathway that can serve as a potential treatment target for various disorders. A number of inhibitors have been developed for the TLR4 pathway, and although no inhibitors have been approved for clinical use, most have been screened against the TLR4-MD2 conformation. The venom gland is the organ of venomous snakes that secretes substances that are toxic to other animals. The level of gene transcription in venom glands is different from that in other tissues, includes a large number of biologically active ingredients, and is an important natural resource for the development of new drugs. We constructed a T7 phage display library using the cobra (Naja atra) venom gland from the Guangdong Snake Breeding Plant and performed three rounds of screening with TLR4 as the target, randomly selecting monoclonal phage spots for PCR followed by Sanger sequencing. The obtained sequences were subjected to length analysis, molecular docking, solubility prediction, and stability prediction, and a peptide containing 39 amino acids (NA39) was finally screened out. The BLAST results indicated that NA39 was a sequence in RPL19 (Ribosomal Protein L19). After peptide synthesis, the binding ability of NA39 to TLR4 was verified by the surface plasmon resonance (SPR) technique. In this study, a new peptide that can specifically bind TLR4 was successfully screened from the cobra venom gland cDNA library, further demonstrating the effectiveness of phage display technology in the field of drug discovery.<\/jats:p>","DOI":"10.3390\/toxins16030113","type":"journal-article","created":{"date-parts":[[2024,2,26]],"date-time":"2024-02-26T03:34:04Z","timestamp":1708918444000},"page":"113","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":3,"title":["Screening TLR4 Binding Peptide from Naja atra Venom Glands Based on Phage Display"],"prefix":"10.3390","volume":"16","author":[{"given":"Runhan","family":"Li","sequence":"first","affiliation":[{"name":"Key Laboratory of Ecology of Rare and Endangered Species and Environmental Protection, Guangxi Normal University, Ministry of Education, Guilin 541006, China"},{"name":"Chengdu Institute of Biology, Chinese Academy of Sciences, Chengdu 610041, China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Yezhong","family":"Tang","sequence":"additional","affiliation":[{"name":"Chengdu Institute of Biology, Chinese Academy of Sciences, Chengdu 610041, China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-2266-7776","authenticated-orcid":false,"given":"Zening","family":"Chen","sequence":"additional","affiliation":[{"name":"Key Laboratory of Ecology of Rare and Endangered Species and Environmental Protection, Guangxi Normal University, Ministry of Education, Guilin 541006, China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-1725-8721","authenticated-orcid":false,"given":"Yang","family":"Liu","sequence":"additional","affiliation":[{"name":"Chengdu Institute of Biology, Chinese Academy of Sciences, Chengdu 610041, China"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"1968","published-online":{"date-parts":[[2024,2,24]]},"reference":[{"key":"ref_1","doi-asserted-by":"crossref","first-page":"197","DOI":"10.1146\/annurev.immunol.20.083001.084359","article-title":"Innate immune recognition","volume":"20","author":"Janeway","year":"2002","journal-title":"Annu. Rev. Immunol."},{"key":"ref_2","doi-asserted-by":"crossref","first-page":"20","DOI":"10.1111\/j.1460-9568.2008.06321.x","article-title":"Non-stereoselective reversal of neuropathic pain by naloxone and naltrexone: Involvement of toll-like receptor 4 (TLR4)","volume":"28","author":"Hutchinson","year":"2008","journal-title":"Eur. J. Neurosci."},{"key":"ref_3","doi-asserted-by":"crossref","first-page":"51","DOI":"10.1016\/j.ejphar.2011.11.037","article-title":"Effects of intrathecal epigallocatechin gallate, an inhibitor of Toll-like receptor 4, on chronic neuropathic pain in rats","volume":"676","author":"Kuang","year":"2012","journal-title":"Eur. J. Pharmacol."},{"key":"ref_4","doi-asserted-by":"crossref","first-page":"5856","DOI":"10.1073\/pnas.0501634102","article-title":"The CNS role of Toll-like receptor 4 in innate neuroimmunity and painful neuropathy","volume":"102","author":"Tanga","year":"2005","journal-title":"Proc. Natl. Acad. Sci. USA"},{"key":"ref_5","doi-asserted-by":"crossref","first-page":"316","DOI":"10.1016\/j.expneurol.2011.09.038","article-title":"Toll-like receptors in chronic pain","volume":"234","author":"Nicotra","year":"2012","journal-title":"Exp. Neurol."},{"key":"ref_6","doi-asserted-by":"crossref","first-page":"1908","DOI":"10.1097\/j.pain.0000000000001306","article-title":"Targeting toll-like receptor-4 (TLR4)-an emerging therapeutic target for persistent pain states","volume":"159","author":"Bruno","year":"2018","journal-title":"Pain"},{"key":"ref_7","doi-asserted-by":"crossref","unstructured":"Heine, H., and Zamyatina, A. (2023). Therapeutic Targeting of TLR4 for Inflammation, Infection, and Cancer: A Perspective for Disaccharide Lipid A Mimetics. Pharmaceuticals, 16.","DOI":"10.3390\/ph16010023"},{"key":"ref_8","doi-asserted-by":"crossref","first-page":"15952","DOI":"10.1523\/JNEUROSCI.1609-13.2013","article-title":"Blockade of Toll-like receptor 4 attenuates morphine tolerance and facilitates the pain relieving properties of morphine","volume":"33","author":"Eidson","year":"2013","journal-title":"J. Neurosci."},{"key":"ref_9","doi-asserted-by":"crossref","first-page":"251","DOI":"10.7150\/ijms.7.251","article-title":"Intrathecal siRNA against Toll-like receptor 4 reduces nociception in a rat model of neuropathic pain","volume":"7","author":"Wu","year":"2010","journal-title":"Int. J. Med. Sci."},{"key":"ref_10","doi-asserted-by":"crossref","first-page":"2881","DOI":"10.1016\/j.pain.2011.09.020","article-title":"Spinal TLR4 mediates the transition to a persistent mechanical hypersensitivity after the resolution of inflammation in serum-transferred arthritis","volume":"152","author":"Christianson","year":"2011","journal-title":"Pain"},{"key":"ref_11","doi-asserted-by":"crossref","first-page":"355","DOI":"10.1038\/351355b0","article-title":"Drosophila Toll and IL-1 receptor","volume":"351","author":"Gay","year":"1991","journal-title":"Nature"},{"key":"ref_12","doi-asserted-by":"crossref","first-page":"2582","DOI":"10.1161\/01.ATV.0000250933.92917.dd","article-title":"Regulation of TLR4 expression is a tale about tail","volume":"26","author":"Yan","year":"2006","journal-title":"Arterioscler. Thromb. Vasc. Biol."},{"key":"ref_13","doi-asserted-by":"crossref","first-page":"393","DOI":"10.1016\/j.ejmech.2013.10.019","article-title":"Novel toll-like receptor 4 (TLR4) antagonists identified by structure- and ligand-based virtual screening","volume":"70","author":"Brus","year":"2013","journal-title":"Eur. J. Med. Chem."},{"key":"ref_14","doi-asserted-by":"crossref","first-page":"742","DOI":"10.2174\/1573406412666160314151900","article-title":"Synthesis and Biological Evaluation of N-Aryl-N\u2019-(5-(2-hydroxybenzoyl) pyrimidin-2-yl)guanidines as Toll-Like Receptor 4 Antagonists","volume":"12","author":"Sova","year":"2016","journal-title":"Med. Chem."},{"key":"ref_15","doi-asserted-by":"crossref","first-page":"111307","DOI":"10.1016\/j.fct.2020.111307","article-title":"Crocin attenuates cisplatin-induced hepatotoxicity via TLR4\/NF-\u03baBp50 signaling and BAMBI modulation of TGF-\u03b2 activity: Involvement of miRNA-9 and miRNA-29","volume":"140","author":"Khedr","year":"2020","journal-title":"Food Chem. Toxicol."},{"key":"ref_16","doi-asserted-by":"crossref","first-page":"2774","DOI":"10.1007\/s12035-018-1280-9","article-title":"Ferulic Acid Rescues LPS-Induced Neurotoxicity via Modulation of the TLR4 Receptor in the Mouse Hippocampus","volume":"56","author":"Rehman","year":"2019","journal-title":"Mol. Neurobiol."},{"key":"ref_17","first-page":"4125","article-title":"Human monoclonal anti-TLR4 antibody negatively regulates lipopolysaccharide-induced inflammatory responses in mouse macrophages","volume":"22","author":"Wang","year":"2020","journal-title":"Mol. Med. Rep."},{"key":"ref_18","doi-asserted-by":"crossref","first-page":"106","DOI":"10.1038\/s41588-019-0559-8","article-title":"The Indian cobra reference genome and transcriptome enables comprehensive identification of venom toxins","volume":"52","author":"Suryamohan","year":"2020","journal-title":"Nat. Genet."},{"key":"ref_19","doi-asserted-by":"crossref","first-page":"1315","DOI":"10.1126\/science.4001944","article-title":"Filamentous Fusion Phage: Novel Expression Vectors That Display Cloned Antigens on the Virion Surface","volume":"228","author":"Smith","year":"1985","journal-title":"Science"},{"key":"ref_20","doi-asserted-by":"crossref","unstructured":"Lu, R.-M., Hwang, Y.-C., Liu, I.J., Lee, C.-C., Tsai, H.-Z., Li, H.-J., and Wu, H.-C. (2020). Development of therapeutic antibodies for the treatment of diseases. J. Biomed. Sci., 27.","DOI":"10.1186\/s12929-019-0592-z"},{"key":"ref_21","doi-asserted-by":"crossref","unstructured":"Roth, K.D.R., Wenzel, E.V., Ruschig, M., Steinke, S., Langreder, N., Heine, P.A., Schneider, K.-T., Ballmann, R., F\u00fchner, V., and Kuhn, P. (2021). Developing Recombinant Antibodies by Phage Display Against Infectious Diseases and Toxins for Diagnostics and Therapy. Front. Cell. Infect. Microbiol., 11.","DOI":"10.3389\/fcimb.2021.697876"},{"key":"ref_22","doi-asserted-by":"crossref","first-page":"4850","DOI":"10.1016\/j.bmcl.2005.07.017","article-title":"Camptothecin binds to a synthetic peptide identified by a T7 phage display screen","volume":"15","author":"Takakusagi","year":"2005","journal-title":"Bioorg Med. Chem. Lett."},{"key":"ref_23","doi-asserted-by":"crossref","first-page":"790","DOI":"10.3390\/molecules16010790","article-title":"Phage Display: Selecting Straws Instead of a Needle from a Haystack","volume":"16","author":"Vodnik","year":"2011","journal-title":"Molecules"},{"key":"ref_24","doi-asserted-by":"crossref","first-page":"W402","DOI":"10.1093\/nar\/gkz297","article-title":"The PSIPRED Protein Analysis Workbench: 20 years on","volume":"47","author":"Buchan","year":"2019","journal-title":"Nucleic Acids Res."},{"key":"ref_25","doi-asserted-by":"crossref","first-page":"W296","DOI":"10.1093\/nar\/gky427","article-title":"SWISS-MODEL: Homology modelling of protein structures and complexes","volume":"46","author":"Waterhouse","year":"2018","journal-title":"Nucleic Acids Res."},{"key":"ref_26","doi-asserted-by":"crossref","first-page":"W365","DOI":"10.1093\/nar\/gkx407","article-title":"HDOCK: A web server for protein-protein and protein-DNA\/RNA docking based on a hybrid strategy","volume":"45","author":"Yan","year":"2017","journal-title":"Nucleic Acids Res."},{"key":"ref_27","first-page":"28","article-title":"Surface plasmon resonance: A technique for characterizing biomaterial surfaces","volume":"9","author":"Corneillie","year":"1998","journal-title":"Med. Device Technol."},{"key":"ref_28","first-page":"60","article-title":"BioEdit: An important software for molecular biology","volume":"2","author":"Alzohairy","year":"2011","journal-title":"GERF Bull. Biosci."},{"key":"ref_29","doi-asserted-by":"crossref","first-page":"1","DOI":"10.1016\/S0003-2697(03)00193-3","article-title":"Frontal affinity chromatography-mass spectrometry assay technology for multiple stages of drug discovery: Applications of a chromatographic biosensor","volume":"319","author":"Chan","year":"2003","journal-title":"Anal. Biochem."},{"key":"ref_30","doi-asserted-by":"crossref","first-page":"906","DOI":"10.1016\/j.cell.2007.08.002","article-title":"Crystal structure of the TLR4-MD-2 complex with bound endotoxin antagonist Eritoran","volume":"130","author":"Kim","year":"2007","journal-title":"Cell"},{"key":"ref_31","doi-asserted-by":"crossref","first-page":"114291","DOI":"10.1016\/j.ejmech.2022.114291","article-title":"Toll-like receptor 4 (TLR4) inhibitors: Current research and prospective","volume":"235","author":"Zhang","year":"2022","journal-title":"Eur. J. Med. Chem."},{"key":"ref_32","doi-asserted-by":"crossref","first-page":"103464","DOI":"10.1016\/j.drudis.2022.103464","article-title":"Peptide-based drug discovery: Current status and recent advances","volume":"28","author":"Sharma","year":"2023","journal-title":"Drug Discov. Today"},{"key":"ref_33","doi-asserted-by":"crossref","first-page":"386","DOI":"10.1126\/science.1696028","article-title":"Searching for peptide ligands with an epitope library","volume":"249","author":"Scott","year":"1990","journal-title":"Science"},{"key":"ref_34","first-page":"883","article-title":"Identification of receptor ligands with phage display peptide libraries","volume":"40","author":"Koivunen","year":"1999","journal-title":"J. Nucl. Med."},{"key":"ref_35","doi-asserted-by":"crossref","first-page":"20651","DOI":"10.1073\/pnas.1314702110","article-title":"The king cobra genome reveals dynamic gene evolution and adaptation in the snake venom system","volume":"110","author":"Vonk","year":"2013","journal-title":"Proc. Natl. Acad. Sci. USA"},{"key":"ref_36","doi-asserted-by":"crossref","unstructured":"Apostolopoulos, V., Bojarska, J., Chai, T.T., Elnagdy, S., Kaczmarek, K., Matsoukas, J., New, R., Parang, K., Lopez, O.P., and Parhiz, H. (2021). A Global Review on Short Peptides: Frontiers and Perspectives. Molecules, 26.","DOI":"10.3390\/molecules26020430"},{"key":"ref_37","doi-asserted-by":"crossref","first-page":"898","DOI":"10.1002\/prot.22927","article-title":"Salt bridges: Geometrically specific, designable interactions","volume":"79","author":"Donald","year":"2011","journal-title":"Proteins"},{"key":"ref_38","doi-asserted-by":"crossref","first-page":"1898","DOI":"10.1002\/pro.5560070906","article-title":"Effects of salt bridges on protein structure and design","volume":"7","author":"Sindelar","year":"1998","journal-title":"Protein Sci."},{"key":"ref_39","doi-asserted-by":"crossref","first-page":"1829","DOI":"10.1038\/s41596-020-0312-x","article-title":"The HDOCK server for integrated protein-protein docking","volume":"15","author":"Yan","year":"2020","journal-title":"Nat. Protoc."},{"key":"ref_40","doi-asserted-by":"crossref","first-page":"3098","DOI":"10.1093\/bioinformatics\/btx345","article-title":"Protein\u2013Sol: A web tool for predicting protein solubility from sequence","volume":"33","author":"Hebditch","year":"2017","journal-title":"Bioinformatics"},{"key":"ref_41","doi-asserted-by":"crossref","unstructured":"Walker, J.M. (2005). The Proteomics Protocols Handbook, Humana Press.","DOI":"10.1385\/1592598900"},{"key":"ref_42","doi-asserted-by":"crossref","first-page":"37","DOI":"10.1002\/pro.4153","article-title":"DichroWeb, a website for calculating protein secondary structure from circular dichroism spectroscopic data","volume":"31","author":"Miles","year":"2022","journal-title":"Protein Sci."},{"key":"ref_43","doi-asserted-by":"crossref","first-page":"1630","DOI":"10.1093\/bioinformatics\/btr234","article-title":"A reference dataset for the analyses of membrane protein secondary structures and transmembrane residues using circular dichroism spectroscopy","volume":"27","author":"Miles","year":"2011","journal-title":"Bioinformatics"},{"key":"ref_44","doi-asserted-by":"crossref","first-page":"155","DOI":"10.1016\/0003-2697(86)90241-1","article-title":"Analysis of protein circular dichroism spectra for secondary structure using a simple matrix multiplication","volume":"155","author":"Compton","year":"1986","journal-title":"Anal. Biochem."}],"container-title":["Toxins"],"original-title":[],"language":"en","link":[{"URL":"https:\/\/www.mdpi.com\/2072-6651\/16\/3\/113\/pdf","content-type":"unspecified","content-version":"vor","intended-application":"similarity-checking"}],"deposited":{"date-parts":[[2025,10,10]],"date-time":"2025-10-10T14:04:28Z","timestamp":1760105068000},"score":1,"resource":{"primary":{"URL":"https:\/\/www.mdpi.com\/2072-6651\/16\/3\/113"}},"subtitle":[],"short-title":[],"issued":{"date-parts":[[2024,2,24]]},"references-count":44,"journal-issue":{"issue":"3","published-online":{"date-parts":[[2024,3]]}},"alternative-id":["toxins16030113"],"URL":"https:\/\/doi.org\/10.3390\/toxins16030113","relation":{},"ISSN":["2072-6651"],"issn-type":[{"value":"2072-6651","type":"electronic"}],"subject":[],"published":{"date-parts":[[2024,2,24]]}}}