摘要：While a great deal of research has focused on the application of full-sequence ionic complementary peptide, detection of the capability of half-sequence ionic complementary peptide such as drug carriers, is rarely reported. This paper presents that the half-sequence ionic complementary peptide P9 (AC-Pro- Ser-Phe-Asn-Phe-Lys-Phe-Glu-Pro-NH2) can successfully stabilize a model hydrophobic drug pyrene in the aqueous solution. Soybean lecithin vesicles were used to mimic plasma membranes. Fluorescence data show that the pyrene is presented in the crystalline form when stabilized by P9 solution, and molecularly migrated from its peptide encapsulations into the membrane bilayers when the suspension is mixed with lipidosome vesicles. Slower release was observed when thicker coating was applied onto pyrene, which could be to control the wall thickness coating the cargo, and consequently the release rate. The result indicated that P9, with half-sequence ionic complement, may serve as a hydrophobic compounds carrier.

摘要：peptide stapling strategy has been proven a promising solution in addressing two major pharmacological hurdles, proteolytic stability and membrane permeability, for small peptides as therapeutics. This stapling peptides feature a covalent cross-link of side chains, thus effectively mimicking α-helix as inhibitors of protein-protein interactions. In this review, we category and analyze key examples of various peptide stapling strategies based on different cross-links aligned on the side chain of peptides mainly in the last three years.

摘要：The reassembly of a half-sequence ionic self-complementarity peptide CH3CO-Pro-Ser-Phe- Cys-Phe-Lys-Phe-Glu-Pro-NH2 was reported, which could self-assemble into stable nanofibers, and formed hydrogel consisting of 〉99% water. In this study, the nanofiber scaffold was sonicated by an ultrasonic cell disruptor. The effects of sonication were detected by circular dichroism （CD）, atomic force microscopy （AFM）, and rheology. AFM image illustrated that the sonicated fragments could quickly reassemble into nanofibers, while the morphology was distinguishable from the original one. CD spectrum revealed that the conversion occurred mainly between regular β-strand structure and distorted β-strand structure. Rheological analyses showed that the storage modulus （G＇） of the peptide solution at the 7th day after sonication decreased by nearly 40% compared with the value of the solution before sonication. Finally, a plausible conversion model was proposed to interpret the reassembly process.

摘要：The complicated, highly dynamic and diverse nature of biosystems brings great challenges to the specific analysis of molecular processes of interest. Nature provides antibodies for the specific recognition of antigens, which is a straight-forward way for targeted analysis. However, there are still limitations during the practical applications due to the big size of the antibodies, which accelerate the discovery of small molecular probes. peptides built from various optional building blocks and easily achieved by chemical synthetic approaches with predictable conformations, are versatile and can act as tailor-made targeting *** this mini review, we summarize the recent developments in the discovery of novel peptides for bioanalytical and biomedical applications. Progresses in peptide-library design and selection strategies are presented. Recent achievements in the peptide-guided detection, imaging and disease treatment are also focused.

摘要：Chlorin e6-pHLIPss-AuNRs, a gold nanorod-photosensitizer conjugate containing a pH （low） insertion peptide （pHLIP） with a disulfide bond which imparts extracellular pH （pHe）-driven tumor targeting ability, has been successfully developed for bimodal photodynamic and photothermal therapy. In this bimodal therapy, chlorin e6 （Ce6）, a second-generation photosensitizer （PS）, is used for photodynamic therapy （PDT）. Gold nanorods （AuNRs） are used as a hyperthermia agent for photothermal therapy （PTT） and also as a nanocarrier and quencher of Ce6. pHLIPss is designed as a pile-driven targeting probe to enhance accumulation of Ce6 and AuNRs in cancer cells at low pH. In Ce6- pHLIPss-AuNRs, Ce6 is close to and quenched by AuNRs, causing little PDT effect. When exposed to normal physiological pH 7.4, Ce6-pHLIPs^-AuNRs loosely associate with the cell membrane. However, once exposed to acidic pH 6.2, pHLIP actively inserts into the cell membrane, and the conjugates are translocated into cells. When this occurs, Ce6 separates from the AuNRs as a result of disulfide bond cleavage caused by intracellular glutathione （GSH）, and singlet oxygen is produced for PDT upon light irradiation. In addition, as individual PTT agent, AuNRs can enhance the accumulation of PSs in the tumor by the enhanced permeation and retention （EPR） effect. Therefore, as indicated by our data, when exposed to acidic pH, Ce6-pHLIPss-AuNRs can achieve synergistic PTT/PDT bimodality for cancer treatment.

摘要：Objective： To provide essential information for peptide inhibitor design, the interactions of Eps15 homology domain of Eps15 homology domain-containing protein 1 （EHD1 EH domain） with three peptides containing NPF （asparagine-proline-phenylalanine）, DPF （aspartic acid-proline-phenylalanine）, and GPF （glycine-proline-phenylalanine） motifs were deciphered at the atomic level. The binding affinities and the underlying structure basis were investigated. Methods： Molecular dynamics （MD） simulations were performed on EHD1 EH domain/peptide complexes for 60 ns using the GROMACS package. The binding free energies were calculated and decomposed by molecular mechanics/ generalized Born surface area （MM/GBSA） method using the AMBER package. The alanine scanning was performed to evaluate the binding hot spot residues using FoldX software. Results： The different binding affinities for the three peptides were affected dominantly by van der Waals interactions. Intermolecular hydrogen bonds provide the struc- tural basis of contributions of van der Waals interactions of the flanking residues to the binding. Conclusions： van der Waals interactions should be the main consideration when we design peptide inhibitors of EHD1 EH domain with high affinities. The ability to form intermolecular hydrogen bonds with protein residues can be used as the factor for choosing the flanking residues.

摘要：背景：心力衰竭（heart failure，HF）这一综合征的表现多种多样。虽然医生可以根据患者射血分数（ejection fraction，EF）和舒张功能加以诊断，但是，目前有关社区人群心力衰竭特点的资料却寥寥无几，而且多数相关研究都是以医院为单位、有赖于实验室检查的回顾性研究。此外，鲜有研究采用标准化技术对患者舒张功能进行系统评价。目的：对社区心力衰竭患者的EF、心室舒张功能和脑型利钠肽（brain natriuretic peptide，BNP）水平进行前瞻性研究。主要观测指标：超声心动图测得的EF值和舒张功能、血BNP水平、6个月死亡率。设计、地点及参试者：于2003年9月10日至2005年10月27日在奥姆斯特德郡（Olmsted County）招募HF新发病例及陈旧病例（住院患者或门诊患者）。应用超声心动图测定EF和舒张功能，检测BNP水平。结果：共有556例参试者在确诊HF时接受了超声心动图检查。其中EF值正常（〉150％）者有308例（55％），多见于年长、女性和既往无心肌梗死病史的患者（P均〈0．001）。242例患者（44％）存在单纯舒张功能不全（即舒张功能不全，但EF值正常）。与EF正常的患者相比，EF降低的患者合并中、重度舒张功能不全的比例较高（风险比，1．67；95％可信区间[confidence interval，CI]，1．11～2．51；P=0．01）。EF降低以及舒张功能不全均与BNP水平升高独立相关。EF正常者及降低者6个月死亡率均为16％（对年龄和性别进行校正后风险比为0．85；95％CI，0．61—1．19；P=0．33）。结论：社区中半数以上的心力衰竭患者EF值正常，40％以上的患者存在单纯舒张功能不全。射血分数和舒张功能不全均与BNP水平升高独立相关。与EF降低的心力衰竭患者相似，EF正常的心力衰竭患者死亡率也较高。

摘要：背景：明确心血管事件高危人群对最佳实施一、二级预防措施非常重要。目的：研究血浆脑型利钠肽N端片段（prohormone braintype natriuretic peptide，NT—proBNP）水平是否能独立于现有其他诊断性检查预测心血管事件和死亡。设计、地点及参试者：HSS研究（Heart and Soul Study）于2000年-2002年入选987例来自加利福尼亚州的稳定性冠心病患者进行前瞻性队列研究，平均随访3．7年（范围，0．1—5．3年）。