Zeng Wenbin, Chen Yue-Lei
Protein & Peptide Letters School of Pharmaceutical Sciences Central South University 172 Tongzipo Road, Changsha 410013 China.
Protein Pept Lett. 2014;21(10):975. doi: 10.2174/092986652110140905121934.
Glycopeptides, peptides containing sugar β-amino acids, have significant impact on medicinal chemistry research and pharmaceutical industr. In 1956, the discovery of one classic glycopeptide, vancomycin, broke the dawn of a new age for antibacterial research. Employing glycopeptides for the therapeutic purposes used to be regarded as proposals. Owing largely to the recent improvements in separation practices, characterization techniques, synthetic methods, and biological research, these proposals have been transformed into ongoing research projects in many laboratories around the world. Previously known as antibiotics, glycopeptides have been used as chemotherapeutic, antiviral, antitubercular, antifungal, antiproliferative and apoptotic agents. Nowadays they are even considered for the development of HIV and cancer vaccines. While several of them are in clinical trials, it could be expected that in the near future, treatment regimen of such difficult diseases might be reformed accordingly. Many interesting preliminary results are being produced in this emerging area. As witnesses and practitioners in this exciting area, however, we notice that the related communication in public domain is still limited due to the relatively small number of researchers involved. Thus, we feel the necessity to compile a timely issue about the special topic "Advances in Therapeutic Glycopeptides", covering state-of-the-art research papers and expert reviews from this area. We are glad that Protein & Peptide Letters is willing to realize the idea with us. The opening paper of this issue by Dr. Voglmeir and coauthor discusses three types of PNGases in respect of their general properties and applications of the commercially available PNGases in glycopeptide and glycoprotein analysis. Dr. Liu and coauthors describe current techniques such as high-performance liquid chromatography (HPLC), capillary electrophoresis (CE), and mass spectrometry (MS), for the characterization of glycoproteins, with a focus on available therapeutic glycoproteins. Next three papers discuss the synthetic chemistry of glycopeptides. Dr. Zhu and coauthor describe a facile synthesis of differently protected cystathionines by the reaction of γ-bromohomoalanine with cysteine derivatives in an ethyl acetate/water biphasic system. Dr. Chen et al. report a neoglycopeptides synthesis by aqueous Suzuki-Miyaura reaction between glycosyl boronic acid and iodopeptides. Dr. Zeng et al. developed a novel strategy to prepare glycopeptide-based molecular imaging and therapy agents using fluorine-rich (fluorous) technology. The following review by Dr. Li et al. outlines a sample of mAbs currently approved for cancer treatment by the FDA, as well as antibody platforms in the research pipeline and clinic that have been engineered for greater tumor penetration, binding, and therapy efficacy. The asialoglycoprotein receptor (ASGPR) is a high-capacity C-type lectin receptor expressed on mammalian hepatocytes. Research in this field is summarized by Dr. Lu, Dr. Yin and coauthors. Recent progresses of cationic polysomes and liposomes as effective non-viral delivery system via ASGPR are also presented by these authors. Proteoglycans (PGs), a core protein and glycosaminoglycans (GAGs) chain, play important roles in amyloid-beta protein as well as tau processing, and have potential significance in Alzheimer's disease (AD) therapy. Next, Dr. Zeng and coworkers summarized recent advances of the chemistry and biology of glycopeptides with antibiotic activity. The last review of this issue by Dr. Ding and coworker provide the progress of PGs and GAGs in AD and their therapeutic implication. In summary, experts from different fields of therapeutic glycopeptides have showcased new results and expressed their opinions in this special thematic issue of Protein & Peptide Letters. As the guest editors, we wish that this diverse collection of valuable intellectual contributions will positively influence this emerging area and gain broad readership. At the end, we would like to express our sincerest gratitude to all authors and referees for their invaluable contribution to this issue. We would also like to extend our appreciation to Editor-in-Chief, Professor Ben M. Dunn and the staffs of Protein & Peptide Letters, especially Ms Rukhshanda Rehman, for their excellent support and for providing us with the opportunity to pursue this exciting project.
糖肽,即含有糖β-氨基酸的肽,对药物化学研究和制药行业有着重大影响。1956年,一种经典糖肽万古霉素的发现,开启了抗菌研究新时代的曙光。将糖肽用于治疗目的曾被视为提议。很大程度上由于近期分离技术、表征技术、合成方法和生物学研究的改进,这些提议已在世界各地许多实验室转变为正在进行的研究项目。糖肽以前被称为抗生素,已被用作化学治疗剂、抗病毒剂、抗结核剂、抗真菌剂、抗增殖剂和凋亡剂。如今,它们甚至被考虑用于开发HIV和癌症疫苗。虽然其中几种正在进行临床试验,但可以预期在不久的将来,此类疑难疾病的治疗方案可能会相应改革。在这个新兴领域正在产生许多有趣的初步结果。然而,作为这个令人兴奋领域的见证者和从业者,我们注意到由于涉及的研究人员相对较少,公共领域的相关交流仍然有限。因此,我们觉得有必要及时汇编一期关于“治疗性糖肽进展”的专题,涵盖该领域的前沿研究论文和专家评论。我们很高兴《蛋白质与肽快报》愿意与我们一起实现这个想法。本期的开篇论文由沃格迈尔博士及其合著者讨论了三种PNG酶的一般特性以及市售PNG酶在糖肽和糖蛋白分析中的应用。刘博士及其合著者描述了用于糖蛋白表征的当前技术,如高效液相色谱(HPLC)、毛细管电泳(CE)和质谱(MS),重点是可用的治疗性糖蛋白。接下来的三篇论文讨论了糖肽的合成化学。朱博士及其合著者描述了在乙酸乙酯/水双相体系中γ-溴高丙氨酸与半胱氨酸衍生物反应简便合成不同保护的胱硫醚。陈博士等人报道了糖基硼酸与碘肽之间通过水相铃木-宫浦反应合成新糖肽。曾博士等人开发了一种使用富氟(氟代)技术制备基于糖肽的分子成像和治疗剂的新策略。李博士等人的以下综述概述了目前美国食品药品监督管理局(FDA)批准用于癌症治疗的单克隆抗体样本,以及正在研发和临床中的抗体平台,这些平台经过工程改造以实现更大的肿瘤穿透、结合和治疗效果。去唾液酸糖蛋白受体(ASGPR)是一种在哺乳动物肝细胞上表达的高容量C型凝集素受体。卢博士、尹博士及其合著者总结了该领域的研究。这些作者还介绍了阳离子多聚体和脂质体作为通过ASGPR的有效非病毒递送系统的最新进展。蛋白聚糖(PGs),一种核心蛋白和糖胺聚糖(GAGs)链,在β-淀粉样蛋白以及tau蛋白加工中起重要作用,并且在阿尔茨海默病(AD)治疗中具有潜在意义。接下来,曾博士及其同事总结了具有抗生素活性的糖肽的化学和生物学最新进展。本期的最后一篇综述由丁博士及其同事提供了PGs和GAGs在AD中的进展及其治疗意义。总之,治疗性糖肽不同领域的专家在《蛋白质与肽快报》的这个专题特刊中展示了新成果并发表了他们的观点。作为客座编辑,我们希望这一系列多样的宝贵知识贡献将对这个新兴领域产生积极影响并获得广泛读者。最后,我们要向所有作者和审稿人表示最诚挚的感谢,感谢他们对本期的宝贵贡献。我们还要感谢主编本·M·邓恩教授和《蛋白质与肽快报》的工作人员,特别是鲁赫尚达·雷曼女士,感谢他们的出色支持以及为我们提供机会开展这个令人兴奋的项目。