合同研究|药物发现与优化|肽优化肽优化

JPT 的肽优化项目使用在聚合物树脂或溶液中合成的纯化化合物进行。如果需要，SPOT™ 和 PepStar™ 等专有的高含量技术支持优化工作。该过程是高度迭代的，同时考虑了所有相关的优化参数。在这方面，我们强调在优化过程的早期就对后期目标（例如 PK/Tox 特性）进行评估和考虑（以便在必要时允许早期回退）。在优化过程中，先导肽通常会转化为更小、更不像肽的化合物（即通过掺入非天然氨基酸、小分子构建单元或空间限制）。

先导优化项目并不局限于药物发现领域。我们的专业知识被应用于许多领域她的生物医学研究领域以及营养和化妆品行业。例如，JPT 的科学家在开发用于纯化治疗性蛋白质的特定肽亲和配体方面拥有丰富的经验。

合同研究|药物发现与优化|命中先导/资格命中先导资格

在 JPT，我们特别关注命中的彻底资格。为此，在与目标参数/属性相关的多种测定中重新合成、纯化和表征命中。连同 SAR 分析，分析结果可以明确优先次序并选择最有希望的优化线索。

JPT 参与了多项命中资格/命中-先导项目，其中激酶、蛋白酶、转移酶、异构酶和磷酸酶的命中被转移到合格的先导中。这些项目是在内部完成的，或者是在与行业合作伙伴的长期合作中完成的。

JPT 的命中资格流程得到了已建立的服务提供商网络的支持，该网络基本上涵盖了所有属性与药物发现和其他应用相关的阳离子。

合同研究|药物发现与优化|肽发现Peptide Discovery

在过去的十年中，JPT 运行了几个成功的肽命中鉴定项目。其中包括孤儿蛋白酶、激酶、磷酸酶和乙酰转移酶的特异性底物。大多数筛选项目的关键是 JPT 专有的 PepSpot™ 或 PepStar™ 技术的应用。各自的筛选库是基于知识或从随机序列开始设计的。

与德国拜耳公司合作，创建了一个用于筛选的高内涵肽库未公开的目标。总体而言，数百万种化合物被选择、合成和筛选。

合同研究|药物发现与优化药物发现与优化

JPT Peptide Technologies 将其专有的肽技术、生物信息学和药物化学专业知识以及长达十年的研发项目合同研究和研发合作管理记录应用于以下领域：

Peptide DiscoveryHit to Lead / QualificationPeptide Optimization

我们在药物发现和优化方面的经验可应用于基于肽的药物和疫苗项目，在发现用于化妆品和营养品行业的肽添加剂、开发用于纯化生物分子的亲和配体以及用于新型免疫诊断的含量测定。

ApplicationsApplicationsDiscovery of蛋白质、蛋白质复合物或抗体的肽激动或拮抗配体在结合亲和力、激动或拮抗功效和物理化学方面优化肽和 PK 特性鉴定和优化用于纯化治疗性蛋白质或抗体的亲和配体鉴定和优化复杂靶蛋白（例如膜蛋白）替代结合测定的开发开发肽作为药物制剂中的活性成分或赋形剂（例如增加稳定性） ) 或营养品和化妆品分别参考文献参考文献Detection of Neurogenerative DiseasesMoussaoui et al, Patent WO 2017/153922 (2017)Peptide Mimotopes of the CD3 T-Cell Co-Receptor Epsilon Chain and uses of the CD3 T-Cell Co-Receptor Epsilon Chain and uses of the CD3 T-Cell Co-Receptor Epsilon Chain and uses of the CD3 T-Cell Co-Receptor Epsilon Chain and uses of the Schnatbaum et al, Patent WO 2017/008844 (2015) 肽Claudin 18.2的模仿及其使用Schnatbaum等人，专利WO 2015/113576（2014）肽微阵列可快速优化新型治疗治疗抗体IMAB362SCHNATBAUM等人的药代动力学分析

Histone Peptide H3 23:42 K23ac_R26me2a (H3.1t)

Product Code: SP-His_0603

C-terminally biotinylated synthetic Histone peptide carrying 2 modifications (K23ac, R26me2a) derived from human Histone H3, H3.1t (Swiss-Prot Id(s): Q16695). Amino acid sequence: Ac-Lys(Ac)-VA-Arg(Me2a)-KSAPATGGVKKPHRYR-Lys(Biotinoyl)-NH2Amount: 1 vial containing 10nmol (appr. 35µg)Purity: >70% (HPLC-MS)Delivery format: Freeze-dried in amber type glass vialsApplication(s): Western Blot, Binding experiments, ELISA, Enzyme kinetics, Pull down assays, Substrate SpecifityIndication(s)/Topic(s): Cancer, Phosphatase,Kinase, Methyltransferase, Acetyltransferase, Histones, Phosphatase, Gene regulation & expression, Epigenetics, Cell signaling, Nucleosome, AgingDelivery time: 2-5 days

JPTs Histone Code Peptides As histones are a major focus of epigenetics, JPTs computational scientists compiled a unique library of synthetic posttranslationally modified and unmodified human histone peptides that is now available as individual biotinylated peptides. The peptide library consists of more than seven hundred 20mer peptides from 29 histone families (e.g. H2A[1,19,85...], H2B[1,22,42...], H3[1,23,43...], H4[1,14,44...]). Peptides carry PTMs at reported sites (e.g. acetylation, methylation, phosphorylation, citrullination) in various combinations representing natural variants. JPTs highly skilled and committed scientific staff ensures that the most appropriate methods and techniques are selected for every synthesis project. All of JPTs catalog peptides are provided with HPLC-MS analyses to confirm the identity and demonstrate the high quality of our peptides.

Benefits of JPTs Histone Code Peptides - Whole production performed in a regulated European environment according to DIN EN ISO 9001:2015 & GCLP standards; audits welcome! - For high-throughput screening the whole Histone Code Peptide library is also available displayed on peptide microarrays- Provision of freeze dried aliquots for enhanced stability - Proven track record for many applications

Histone Peptide H3 23:42 K23ac_R26me2a (H3.1t)

Selected References for Histone Peptide Tools \"Histone H2A and H4 N-Terminal Tails are Positioned by the MEP50 WD-Repeat Protein for Efficient Methylation by the PRMT5 Arginine Methyltransferase\"Burgos et al., J. Biol. Chem. (2015) - PMID: 25713080 \"H3K23me2 is a New Heterochromatic Mark in Caenorhabditis elegans\" Vandamme et al., Nucleic Acids Res. (2015) - PMID: 26476455\"Structure of the Arginine Methyltransferase PRMT5-MEP50 Reveals a Mechanism for Substrate Specificity\"Ho et al. PLOS ONE (2013) - PMID:23451136\"Use of High-Density Histone Peptide Arrays for Parsing the Specificity of a Histone-Modifying Enzyme Complex\"Shechter et al, Application Note (2013) (full text)\"Comprehensive Peptide Microarrays for Histone Research\"Schnatbaum et al, 32th EPS (2012) (full text)

Application Notes\"Use of High-Density Histone Peptide Arrays for Parsing the Specificity of a Histone-Modifying Enzyme Complex\"Shechter et al. Application Note (2013) (full text)\"Comprehensive Characterization of Antibodies Directed towards Epigenetic Histone-Modifications\" Masch et al. Application Note (2015) (full text)

Testimonial for Histone Code Peptide Microarray \"JPTs new extremely high-density histone peptide array is a dramatic leap forward for analysis of the histone code hypothesis. The complete sequence coverage across core histones and histone variants as well as the presence of common and rare histone post-translational modifications\"alone and in combination\" makes this an unparalleled tool for studying the \"writers\" and \"readers\" of the histone code. My laboratory has used these arrays to ask the sequence and PTM dependence of a histone writer enzyme and we have discovered an activity specifying code that will keep us busy for years to come.\"David Shechter, PhD, Department of Biochemistry, Albert Einstein College of Medicine, YU (NY, USA)

Histone Peptide H3 23:42 K23ac_R26me2a (H3.1t)

Technical Data:

Histone Family	Histone H3
Modification	2 Modifications
Sequence Position	Tail (1-42)
Isoform	H3.1t
Biotinylation	Biotinylated Peptide
Application	ELISA
Protein Name	Histones
Organism	Homo sapiens (Human)
Indication / Topic	AcetyltransferaseEpigeneticsKinase
Number of peptides	1

Further Information:

Amount	1 vial containing 10nmol (appr. 35µg)
Specifications	C-terminally biotinylated synthetic Histone peptide carrying 2 modifications (K23ac, R26me2a)
Documentation	Product Datasheet
Swiss-Prot ID	Q16695
Sequence	Ac-Lys(Ac)-VA-Arg(Me2a)-KSAPATGGVKKPHRYR-Lys(Biotinoyl)-NH2