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Screening peptide inhibitors Using Phage peptide Library with Isocitrate Lyase in Mycobacterium tuberculosis as Target

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Chemical Research in Chinese Universities 2011年第4期27卷 635-640页

作者： YIN Yu-he NIU Xue SUN BO TENG Guo-sheng ZHAO Yun-hui WU Cong-mei College of Chemistry and Life Science Changchun University of Technology Changchun 130012 P. R. China College of Life Science Jilin University Changchun 130012 P. R. China

When devoured by macrophages,Mycobacterium tuberculosis remains persistent in macrophages and gains energy through the glyoxylate bypass to maintain its long-term existence in host *** it is possible to stop persistent infections by interdicting the glyoxylate bypass in which the isocitrate lyase（ICL） is the key rate-limiting enzyme and a persistence *** is the target of anti-TB（TB：tubercular） drugs,which could screen ICL out and effectively inhibit the activity of ICL in Mycobacterium tuberculosis,and because of this,anti-TB drugs can be used to kill persistent Mycobacterium *** this study,the ICL gene of the Mycobacterium tuberculosis H37Rv was cloned successfully and recombinant protein with bioactivity was obtained through the enzyme characteristic *** specific activity of the recombined ICL is 24μmol·mg-1·*** recombined ICL protein was used as the target,and phages which can specifically combine to ICL were screened in the phage 7 peptide *** to the results of the ELISA and DNA sequence detection,eventually three 7-peptide chains were *** the peptide chains were reacted with ICL,respectively,to detect their inhibitory effects on *** results show that all the three 7-peptide chains possessed varying inhibitory effects on the activity of *** study provided lead compounds for the research and development of new peptide anti-TB drugs.

关键词： Mycobacterium tuberculosis Isocitrate lyase Gene expression Phage peptide library peptide inhibitor

Screening of peptide inhibitors of TACE from a Phage Display Random 15-peptide Library by Recombinant TACE Ectodomain

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Frontiers in Biology 2006年第1期1卷 56-60页

作者： Huang Wei Yang Yuzhen Wang Zhen Hang Ling Department of Biochemistry and Molecular Biology Tongji Medical CollegeHuazhong University of Science and TechnologyWuhan 430030 HubeiChina Wuhan Institute of Medical Sciences Wuhan 430014China

Tumor necrosis factor(TNF)-α-converting enzyme(TACE)is the major protease responsible for processing pro-TNF-αfrom membrane-anchored precursors to secreted TNF-α.In the present study,a 15-peptide library was used to identify potential TACE *** obtain the recombinant TACE ectodomain and to use it as a selective molecule for the screening of peptide inhibitors of TACE,cDNA coding for the catalytic domain(T800)and full-length ectodomain(T1300)of TACE were amplified by reverse transcription–polymerase chain *** expression plasmid were constructed by inserting T800/T1300 into plasmid pET-28a/c respectively and were transformed into Escherichia coli BL21(DE3).Sodium dodecyl sulfate–polyacrylamide gel electrophoresis(SDSPAGE)andWestern blot analysis revealed that T800/T1300 were highly expressed in the form of an inclusion body induced by *** Ni2+–NTA resin affinity chromatography,the purity of the recombinant T800/T1300 protein was more than 90%.T800 and T1300 proteins were used in the screening of T800/T1300-binding peptides from a phage display random 15-peptide *** four rounds of biopanning,the positive phage clones were analyzed by enzyme-linked immunosorbent assay,competitive inhibition assay(ELESA),and DNA sequencing.A common amino acid sequence(TRWLVYFS RPYLVAT)was confirmed and synthesized.A synthetic peptide was shown to bind to TACE and to inhibit TNF-αrelease from lipopolysaccharide(LPS)-stimulated human peripheral blood mononuclear cells(PBMC)by up to 60.3%.Fluorescence-activated cell sorter(FACS)analysis revealed that the peptide mediated the accumulation of TNF-αon an LPS-stimulated PBMC *** results demonstrate that the TACE-binding peptide is an effective antagonist of TACE and that the deduced motif might be applied to the molecular design of anti-inflammatory drugs.

关键词： TACE ectodomain phage display random peptide library peptide inhibitor

Development of peptide inhibitors of HIV transmission

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Bioactive Materials 2016年第2期1卷 109-121页

作者： Siyu Shi Peter K.Nguyen Henry J.Cabral Ramon Diez-Barroso Paul J.Derry Satoko M.Kanahara Vivek A.Kumar Department of Chemistry Rice UniversityHoustonTX 77030USA Baylor College of Medicine HoustonTX 77030USA Community Healthcare Network New YorkNY 10010USA Department of Biomedical Engineering New Jersey Institute of TechnologyUniversity HeightsNewarkNJ 07102USA Department of Chemical Biological and Pharmaceutical EngineeringNew Jersey Institute of TechnologyUniversity HeightsNewarkNJ 07102USA

Treatment of HIV has long faced the challenge of high mutation rates leading to rapid development of resistance,with ongoing need to develop new methods to effectively fight the ***,early HIV medications were designed to inhibit RNA replication and protein production through small molecular *** based therapeutics are a versatile,promising field in HIV therapy,which continues to develop as we expand our understanding of key protein-protein interactions that occur in HIV replication and *** review begins with an introduction to HIV,followed by the biological basis of disease,current clinical management of the disease,therapeutics on the market,and finally potential avenues for improved drug development.

关键词： HIV HIV treatment Drug development peptide therapeutic peptide inhibitor

Screening of TACE peptide inhibitors from Phage Display peptideLibrary

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Journal of Huazhong University of Science and Technology(Medical Sciences) 2005年第5期25卷 473-476页

作者：黄巍李凌波韩玲杨渝珍 Department of Biochemistry & Molecular Biology School of Basic Medical Sciences Tongji Medical College Huazhong University of Science and Technology Wuhan 430030 China Wuhan Institute of Medical Sciences Wuhan 430014 China

Summary： To obtain the recombinant tumor necrosis factor-α converting enzyme （TACE） ectodomain and use it as a selective molecule for the screening of TACE peptide inhibitors, the cDNA coding catalytic domain （TS00） and full-length ectodomain （T1300） of TACE were amplified by RT-PCR, and the *** plasmids were constructed by inserting T800 and T1300 into plasmid pET-28a and pET-28c respectively. The recombinant TS00 and T1300 were induced by IPTG, and SDS-PAGE and Western blotting analysis results revealed that TS00 and T1300 were highly expressed in the form of inclusion body. After Ni^2＋-NTA resin affinity chromatography, the recombinant proreins were used in the screening of TACE-binding peptides from phage display peptide library respectively. After 4 rounds of biopanning, the positive phage clones were analyzed by ELISA, competitive inhibition assay and DNA sequencing. A common amino acid sequence （TRWLVYFSRPYLVAT） was found and synthesized. The synthetic peptide could inhibit the TNF-α release from LPS-stimulated human peripheral blood mononuclear cells （PBMC） up to 60.3%. FACS analysis revealed that the peptide mediated the accumulation of TNF-α on the cell surface. These results demonstrate that the TACE binding peptide is an effective antagonist of TACE.

关键词： tumor necrosis factor-α converting enzyme ectodomain prokaryote expression phage display peptide inhibitor

Microwave-assisted Solid-phase Synthesis, Biological Evaluation and Molecular Docking of Angiotensin I-converting Enzyme inhibitors

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Chemical Research in Chinese Universities 2012年第1期28卷 108-113页

作者： SUN Yang1, HUANG Da-wei1, LI Xiao-hui1, HU Jian-en2 and XIU Zhi-long1 1. School of Life Science and Biotechnology, Dalian University of Technology, Dalian 116024, P. R. China 2. School of Food Engineering, Dalian Ocean University, Dalian 116023, P. R. China School of Life Science and Biotechnology Dalian University of Technology Dalian 116024 School of Food Engineering Dalian Ocean University Dalian 116023

Short peptides based on the tripeptides, Leu-Arg-Pro and Leu-Lys-Pro, were synthesized by microwave assisted solid-phase synthesis method, in order to make a search for potential inhibitors for angiotensin I-converting enzyme（ACE） with minimum side effects in the treatment of hypertension. One peptide with the sequence Leu-Arg-Pro-Phe-Phe shows the strongest inhibition towards ACE with an IC50 value of 0.26 μmol/L in vitro. The study of structure-activity relationship shows that the introduction of a bulky group into the N-terminal of this series of inhibitors may enlarge steric hindrance, resulting in the poor inhibitory activity towards ACE. The inhibitory activity decreased in turn when L-Pro, D-Pro or Ac6c was at the C-terminal respectively. The binding interaction between each of these inhibitors and testicular ACE（tACE） was performed by molecular docking. The results suggest that Leu-Arg-Pro-Phe-Phe mainly occupied the S1 subsite of tACE, and made contact with tACE via seven H-bonds. It appeared that the site on the peptide that bound with tACE was influenced by the configuration of the amino acid, L or D-form, at the C-terminal of the peptide.

关键词： Angiotensin I-converting enzyme peptide inhibitor Molecular docking Microwave-assisted solid-phasesynthesis

Screening of TACE peptide inhibitors From a Phage Display Random 15-peptide Library by TACE Recombinant Ecotodomain

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Screening of TACE Peptide Inhibitors From a Phage Display Ra...

A peptide Binder of E3 Ligase Adaptor SPOP Disrupts Oncogenic SPOP-Protein Interactions in Kidney Cancer Cells

2006年度学术研讨会

作者： Wei Huang, Ling-bo Li,Ling Hang,Yu-zhen Yang, Deparptment of Biochemistry & Molecular Biology, Tongji Medical College, Huazhong University of Science and Technology, Wuhan 430030, People’s republic of China Wuhan Medical Research Instituti, Wuhan 430014, People’s republic of China

Tumour necrosis factor- α converting enzyme(TACE) is the major protease responsible for processing proTNF from membrane-anchored precursor to secreted TNF-α. In the present study, a 15-peptide library was used identify potential TACE antagonists. To obtain the recombinant TACE ectodomain and use it as a selective molecule for the screening of TACE peptide inhibitors, the cDNA coded for catalytic domain (T800) and full-length ectodomain (T1300) of TACE were amplified by RT-PCR, the expression plasmid was constructed by inserting T800/T1300 into plasmid pET-28a/c and transformed into *** BL21 (DE3). SDS-PAGE and Western blotting analysis revealed that T800/T1300 was highly expressed in the form of inclusion body being induced by the *** Ni2+-NTA resin affinity chromatography, the purity of the recombinant T800/T1300 protein was more than 90%. T800 and T1300 protein were used in the screening of TACE binding peptides from the phage display random 15-peptide library respectively. After four rounds of biopanning, the positive phage clones were analyzed by ELISA,competitive inhibition assay and DNA sequencing. A common amino acid sequence-TRWLVYFSRPYLVAT was found and synthesized. The synthetic peptide was shown to bind to TACE and inhibit the TNF-α release from LPS-stimulated human peripheral blood mononuclear cells(PBMC) up to 60.3%. FACS analysis revealed that the peptide mediated the accumulation of TNF-α on LPS-stimulated PBMC surface. These results demonstrate that the TACE-binding peptide is effective antagonist of TACE and the deduced motif might be applied to molecular design of anti-inflammation drugs.

关键词： TACE Ectodomain Phage display peptide inhibitor

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Chinese Journal of Chemistry 2021年第2期39卷 274-280页

作者： Zhen Wang Hao Zhang Baoen Chen Sisheng Ouyang Tong Zheng Ran Zhou Ze Dong Yue Huang Tao Zhang Hualiang Jiang Jianhua Gan Cheng Luo Cai-Guang Yang School of Chinese Materia Medica Nanjing University of Chinese MedicineNanjingJiangsu210023 China State Key Laboratory of Drug Research Shanghai Institute of Materia MedicaChinese Academy of SciencesShanghai201203 China University of Chinese Academy of Sciences Beijing100049 China School of Pharmaceutical Science and Technology Hangzhou Institute for Advanced StudyUCASHangzhouZhejiang310024 China Shanghai Institute for Advanced Immunochemical Studies ShanghaiTech UniversityShanghai201210 China School of Life Sciences Fudan UniversityShanghai200433 China

The E3 ligase adaptor SPOP,overexpressed in the nucleus but frequently dislocated into the cytoplasm in all clear cell Renal Cell Carcinomas(ccRCC),serves as a regulatory hub to promote kidney cancer through the ubiquitination and degradation of multiple downstream cancer ***,our identification of a selective small-molecule inhibitor of the SPOP-phosphatase and tensin homolog(PTEN)interaction has demonstrated that the oncogenic SPOP-protein interaction would be a druggable target specific to ccRCC *** our knowledge,this is the first time such a small-molecule inhibitor has been ***,we have identified a peptide binder for the SPOP-MATH domain that disrupts the oncogenic SPOP-protein interactions in kidney cancer *** design and biophysical characterization yielded peptide Pep38 that binds to the MATH domain of SPOP and competes on PTEN-binding to SPOP in *** X-ray complex structure reveals that the peptide binder features the following combination:one,a mimic of the native peptide binder and two,an additionalβ-strand motif in sequence,which could contribute to increased binding *** order to improve cellular permeability,we fused Pep38 with the delivery peptide TAT to prepare peptide TAT38,which inhibits the endogenous substrate binding to SPOP and suppresses the proliferation of the ccRCC *** identification of the peptide inhibitors for SPOP-protein interactions provides further validation that the oncogenic SPOP-signaling pathway in ccRCC could be a druggable target specifically applicable to the therapy of kidney cancers.

关键词： SPOP Protein-protein interaction Clear cell Renal Cell Carcinomas Crystal structure peptide inhibitor

Mechanism of Three inhibitors of TACE in Blocking the Converting of pro-TNFα into sTNFα

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Journal of Huazhong University of Science and Technology(Medical Sciences) 2003年第2期23卷 116-120页

作者：王震王茵朱孔黎郭莲军杨渝珍 Department of Pharmacology Tongji Medical CollegeHuazhong University of Science and Technology Wuhan 430030 Life Sciences College Wuhan UniversityWuhan 430072 Department of Biochemistry & Molecular Biology School of Basic Medical SciencesTongji Medical College Huazhong University of Science and TechnologyWuhan 430030 Department of Pharmacology Tongji Medical College Huazhong University of Science and Technology Wuhan 430030 Department of Biochemistry & Molecular Biology School of Basic Medical Sciences Tongji Medical College Huazhong University of Science and Technology Wuhan 430030 The effects of inhibitors of TNFαconverting enzyme (TACE) on TNFαsecretion werestudied to develop an approach to interfere inflammation processes. The HL-60 cell lines were stimu-lated in vitro with LPS intravenously for different time to establish the cellular model of inflammationand simultaneously induce in vivo inflammation animal model by LPS The cytotoxic effects of solubleTNFαwere checked using MTT colorimetric method to determine the rate of cell proliferation. Thelevel of expression of TACE was detected by using RT-PCR FCM and immuno-histochemical tech-nique respectively. It was found Chinese medicine Reduqing (RDQ) could inhibit the transcription ofTNFαmRNA induced by LPS stimulation (P<0.01 compared with the control). The anti-oligodeoxyribonucleotide (anti-ODN) of TNFαmRNA could inhibit 78.9% of TNFαsecretion. Themimic peptides of TACE substrates with hydroxamine group showed potency in vivo and in vitro a-gainst converting of pro-TNFα. It was concluded that all the three types of TACE inhibitors can reg-ulate the expression of TACE at different levels and inhibit sTNFαsecretion indicating TACE is anovel target for inflammation therapy.

The effects of inhibitors of TNFα converting enzyme (TACE) on TNFα secretion were studied to develop an approach to interfere inflammation processes. The HL-60 cell lines were stimulated in vitro with LPS intravenously for different time to establish the cellular model of inflammation and simultaneously induce in vivo inflammation animal model by LPS The cytotoxic effects of soluble TNFa were checked using MTT colorimetric method to determine the rate of cell proliferation. The level of expression of TACE was detected by using RT-PCR, FCM and immuno-histochemical technique respectively. It was found Chinese medicine Reduqing (RDQ) could inhibit the transcription of TNFa mRNA induced by LPS stimulation (Ppeptides of TACE substrates with hydroxamine group showed potency in vivo and in vitro a-gainst converting of pro-TNFα. It was concluded that all the three types of TACE inhibitors can regulate the expression of TACE at different levels and inhibit sTNFα secretion, indicating TACE is a novel target for inflammation therapy.

关键词： TNFα converting enzyme tumor necrosis factor-α Reduqing anti-oligodeoxyri-bonucleotide peptide inhibitor

In Silico Insights into peptide Self-Assembly in Biological and Material Research

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In Silico Insights into Peptide Self-Assembly in Biological ...