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Stapled peptide

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https://www.readbyqxmd.com/read/28633506/role-of-glucagon-like-peptide-1and-gastric-inhibitory-peptide-in-anorexia-induction-following-oral-exposure-to-the-trichothecene-mycotoxin-deoxynivalenol-vomitoxin
#1
Hui Jia, Wen-Da Wu, Xi Lu, Jie Zhang, Cheng-Hua He, Hai-Bin Zhang
Deoxynivalenol (DON), which is a Type B trichothecene mycotoxin produced by Fusarium, frequently contaminates cereal staples, such as wheat, barley and corn. DON threatens animal and human health by suppressing food intake and impairing growth. While anorexia induction in mice exposed to DON has been linked to the elevation of the satiety hormones cholecystokinin (CCK) and peptide YY3-36(PYY3-36) in plasma, the effects of DON on the release of other satiety hormones, such as glucagon-like peptide-1 (GLP-1) and gastric inhibitory peptide (GIP), have not been established...
June 19, 2017: Toxicological Sciences: An Official Journal of the Society of Toxicology
https://www.readbyqxmd.com/read/28603971/enhanced-and-prolonged-cell-penetrating-abilities-of-arginine-rich-peptides-by-introducing-cyclic-%C3%AE-%C3%AE-disubstituted-%C3%AE-amino-acids-with-stapling
#2
Makoto Oba, Masayuki Kunitake, Takuma Kato, Atsushi Ueda, Masakazu Tanaka
Cell-penetrating peptides are receiving increasing attention as drug delivery tools, and the search for peptides with high cell-penetrating ability and negligible cytotoxicity has become a critical research topic. Herein, cyclic α,α-disubstituted α-amino acids were introduced into arginine-rich peptides and an additional staple was provided in the side chain. The peptides designed in the present study showed more enhanced and prolonged cell-penetrating abilities than an arginine nonapeptide due to high resistance to protease and conformationally stable helical structures...
June 16, 2017: Bioconjugate Chemistry
https://www.readbyqxmd.com/read/28547390/mono-substitution-effects-on-antimicrobial-activity-of-stapled-heptapeptides
#3
Huy X Luong, Do-Hee Kim, Ngoan T Mai, Bong-Jin Lee, Young-Woo Kim
We previously reported a de novo design of antimicrobial heptapeptide helices using Verdine's all-hydrocarbon peptide stapling system. One of the important structure-activity relationships we found from these previous studies was that extending of the hydrophobic face by replacing of alanine with leucine in positon 5 increases antimicrobial activity. In this study, to further improve the activity profile of this peptide series, we investigated the substitution effects of position 5 on conformational and proteolytic stability as well as antimicrobial and hemolytic activity...
May 25, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/28539610/secondary-metabolite-genes-encoded-by-potato-rhizosphere-microbiomes-in-the-andean-highlands-are-diverse-and-vary-with-sampling-site-and-vegetation-stage
#4
Gajender Aleti, Branislav Nikolić, Günter Brader, Ram Vinay Pandey, Livio Antonielli, Stefan Pfeiffer, Andreas Oswald, Angela Sessitsch
Potato (Solanum tuberosum) is an important staple crop worldwide, it has been cultivated in the Andean Altiplano under low-input farming practices at high altitudes and under harsh environment for centuries. We analyzed secondary metabolite (SM) gene diversity encoded in the potato rhizosphere microbiome during plant growth at three distinct sites located in the Andes at high altitudes by 454-pyrosequencing of non-ribosomal peptide and polyketide biosynthetic genes. Phylogenetic analysis indicated that the majority of rhizosphere SM-encoding sequences differed from previously known sequences and may have distinct ancestors...
May 24, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28530606/effects-of-chemical-composition-and-baking-on-in-vitro-digestibility-of-proteins-in-breads-made-from-selected-gluten-containing-and-gluten-free-flours
#5
Tong Wu, Cheryl Taylor, Thomas Nebl, Ken Ng, Louise E Bennett
Breads prepared from cereal grains are a dietary staple, providing a significant proportion of daily energy, but not necessarily of dietary protein. However, good digestibility of proteins in bread is important to avoid potential immunogenic effects of undigested peptides, including for those gluten-intolerant. Four gluten-containing (white wheat, wholemeal wheat, spelt and rye) and four gluten-free (chick pea, lupin, buckwheat, amaranth) flours were used to make yeast-leavened breads standardized for protein...
October 15, 2017: Food Chemistry
https://www.readbyqxmd.com/read/28500289/stapled-big3-helical-peptide-erap-potentiates-anti-tumour-activity-for-breast-cancer-therapeutics
#6
Tetsuro Yoshimaru, Keisuke Aihara, Masato Komatsu, Yosuke Matsushita, Yasumasa Okazaki, Shinya Toyokuni, Junko Honda, Mitsunori Sasa, Yasuo Miyoshi, Akira Otaka, Toyomasa Katagiri
Estradiol (E2) and the oestrogen receptor-alpha (ERα) signalling pathway play pivotal roles in the proliferative activity of breast cancer cells. Recent findings show that the brefeldin A-inhibited guanine nucleotide-exchange protein 3-prohibitin 2 (BIG3-PHB2) complex plays a crucial role in E2/ERα signalling modulation in breast cancer cells. Moreover, specific inhibition of the BIG3-PHB2 interaction using the ERα activity-regulator synthetic peptide (ERAP: 165-177 amino acids), derived from α-helical BIG3 sequence, resulted in a significant anti-tumour effect...
May 12, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28497694/stapled-rgd-peptide-enables-glioma-targeted-drug-delivery-by-overcoming-multiple-barriers
#7
Huitong Ruan, Xishan Chen, Cao Xie, Beibei Li, Man Ying, Yu Liu, Mingfei Zhang, Xuesai Zhang, Changyou Zhan, Wuyuan Lu, Weiyue Lu
Malignant glioma, the most frequent and aggressive central nervous system (CNS) tumor, severely threatens human health. One reason for its poor prognosis and short survival is the presence of the blood-brain barrier (BBB) and blood-brain tumor barrier (BBTB), which restrict the penetration of therapeutics into the brain at different stages of glioma. Herein, inspired by the peptide stapling technique, we designed a cyclic RGD ligand via an all-hydrocarbon staple (stapled RGD, sRGD) to facilitate BBB penetration while retaining the capacity of BBTB penetration and targeting ability to glioma cells...
May 18, 2017: ACS Applied Materials & Interfaces
https://www.readbyqxmd.com/read/28496125/enhancing-specific-disruption-of-intracellular-protein-complexes-by-hydrocarbon-stapled-peptides-using-lipid-based-delivery
#8
D Thean, J S Ebo, T Luxton, Xue'Er Cheryl Lee, T Y Yuen, F J Ferrer, C W Johannes, D P Lane, C J Brown
Linear peptides can mimic and disrupt protein-protein interactions involved in critical cell signaling pathways. Such peptides however are usually protease sensitive and unable to engage with intracellular targets due to lack of membrane permeability. Peptide stapling has been proposed to circumvent these limitations but recent data has suggested that this method does not universally solve the problem of cell entry and can lead to molecules with off target cell lytic properties. To address these issues a library of stapled peptides was synthesized and screened to identify compounds that bound Mdm2 and activated cellular p53...
May 11, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28481338/eating-glutinous-brown-rice-twice-a-day-for-8-weeks-improves-glycemic-control-in-japanese-patients-with-diabetes-mellitus
#9
T Nakayama, Y Nagai, Y Uehara, Y Nakamura, S Ishii, H Kato, Y Tanaka
OBJECTIVE: We recently reported that eating glutinous brown rice (GBR) for 1 day improved the whole-day glucose profile and postprandial plasma glucose level compared with eating white rice (WR) or standard brown rice. However, it was unknown whether eating GBR could maintain improvement of glycemic control for a longer period. Therefore, we evaluated the effect of GBR intake for 8 weeks on glycemic control in outpatients with diabetes mellitus. METHODS: This was an open-label randomized crossover study in outpatients with type 2 diabetes...
May 8, 2017: Nutrition & Diabetes
https://www.readbyqxmd.com/read/28436014/a-critical-assessment-of-the-synthesis-and-biological-activity-of-p53-hdm2-stapled-peptide-inhibitors
#10
Rike Wallbrecher, Patrick Chène, Stephan Ruetz, Therese Stachyra, Thomas Vorherr, Roland Brock
BACKGROUND AND PURPOSE: Helix stapling enhances the activity of peptides that interact with a target protein in a helical conformation. These staples are also supposed to change the pharmacokinetics of the molecules and promote cytoplasmic targeting. We scrutinized to which degree the pharmacokinetic characteristics are a function of the staple and differ from those of the standard cationic cell-penetrating peptide nonaarginine for a peptide inhibiting the interaction of p53 with the human double minute 2 (Hdm2) protein...
April 23, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28433781/prevalence-of-celiac-disease-autoimmunity-among-adolescents-and-young-adults-in-china
#11
Juanli Yuan, Chunyan Zhou, Jinyan Gao, Jingjing Li, Fenglian Yu, Jun Lu, Xin Li, Xiaozhong Wang, Ping Tong, Zhihua Wu, Anshu Yang, Yonghong Yao, Sarah Nadif, Heng Shu, Jiang Xu, Yujie Wu, Luud Gilissen, Hongbing Chen
BACKGROUND & AIMS: In China, epidemiological information on celiac disease autoimmunity is scarce and fragmented. We investigated the prevalence of celiac disease autoimmunity in the general Chinese population. METHODS: In a cross-sectional prospective study, 19,778 undiagnosed Chinese adolescents and young adults (16-25 years old) were recruited from consecutive new students who underwent routine physical examinations at 2 universities in Jiangxi, China from Sep...
April 19, 2017: Clinical Gastroenterology and Hepatology
https://www.readbyqxmd.com/read/28425639/designing-dual-inhibitors-of-mdm2-mdmx-unexpected-coupling-of-water-with-gatekeeper-y100-99
#12
Xiong An Lee, Chandra Verma, Adelene Y L Sim
Mdm2 and MdmX share high structural similarity in their N-terminal domains, yet dual inhibitors are challenging to design due to differences in the conformations of the binding pockets, and notably of the proposed gatekeeper residue, Y100/99. Analysis of crystal structures and molecular dynamics (MD) simulations of complexes of Mdm2 and MdmX resulted in the identification of a water molecule with a long residence time that appears to be modulated by the conformation of Y100/99. These observations lead us to speculate that dual inhibitors either i) stabilize both Mdm2 and MdmX with Y100/99 in the open conformation typically seen in complexes of Mdm2 with p53, or ii) the dual inhibitors are agnostic to the conformation of Y100/99...
April 20, 2017: Proteins
https://www.readbyqxmd.com/read/28414223/diversity-oriented-stapling-yields-intrinsically-cell-penetrant-inducers-of-autophagy
#13
Leila Peraro, Zhongju Zou, Kamlesh M Makwana, Ashleigh E Cummings, Haydn L Ball, Hongtao Yu, Yu-Shan Lin, Beth Levine, Joshua A Kritzer
Autophagy is an essential pathway by which cellular and foreign material are degraded and recycled in eukaryotic cells. Induction of autophagy is a promising approach for treating diverse human diseases, including neurodegenerative disorders and infectious diseases. Here, we report the use of a diversity-oriented stapling approach to produce autophagy-inducing peptides that are intrinsically cell-penetrant. These peptides induce autophagy at micromolar concentrations in vitro, have aggregate-clearing activity in a cellular model of Huntington's disease, and induce autophagy in vivo...
June 14, 2017: Journal of the American Chemical Society
https://www.readbyqxmd.com/read/28388005/a-new-methodology-for-incorporating-chiral-linkers-into-stapled-peptides
#14
Juan C Serrano, James Sipthorp, Wenshu Xu, Laura S Itzhaki, Steven V Ley
Stapled peptides have arisen as a new class of chemical probe and potential therapeutic agents for modulating protein-protein interactions. Here, we report the first two-component i,i+7 stapling methodology that makes use of two orthogonal, on-resin stapling reactions to incorporate linkers bearing a chiral centre into a p53-derived stapled peptide. Post-stapling modifications to the chain were performed on-resin and enabled rapid access to various peptide derivatives from a single staple. The stapled peptides have increased helicity, protease stability and in vitro binding affinities to MDM2 compared to the equivalent unstapled peptide...
April 7, 2017: Chembiochem: a European Journal of Chemical Biology
https://www.readbyqxmd.com/read/28366833/molecular-characterization-of-fmrfamide-like-peptides-in-meloidogyne-graminicola-and-analysis-of-their-knockdown-effect-on-nematode-infectivity
#15
Chanchal Kumari, Tushar K Dutta, Sonam Chaudhary, Prakash Banakar, Pradeep K Papolu, Uma Rao
The rice root-knot nematode, Meloidogyne graminicola, seriously impairs the growth and yield of rice which is an important staple food worldwide. The disruption of neuropeptide signalling leading to attenuation in nematode behaviour and thereby perturbed infection, offers an attractive alternative to control nematodes. In this direction, the present study was aimed at mining of putative FMRFamide-like peptides (FLPs) from the transcriptomic dataset of M. graminicola followed by characterization of those FLPs via sequencing of PCR products, qRT-PCR and Southern hybridization analysis...
July 1, 2017: Gene
https://www.readbyqxmd.com/read/28358924/processing-and-targeting-of-proteins-derived-from-polyprotein-with-2a-and-lp4-2a-as-peptide-linkers-in-a-maize-expression-system
#16
He Sun, Ni Zhou, Hai Wang, Dafang Huang, Zhihong Lang
In the transformation of multiple genes, gene fusion is an attractive alternative to other methods, including sexual crossing, re-transformation, and co-transformation, among others. The 2A peptide from the foot-and-mouth disease virus (FMDV) causes the co-translational "cleavage" of polyprotein and operates in a wide variety of eukaryotic cells. LP4, a linker peptide that originates from a natural polyprotein occurring in the seed of Impatiens balsamina, can be split between the first and second amino acids in post-translational processing...
2017: PloS One
https://www.readbyqxmd.com/read/28345248/application-of-thiol-yne-thiol-ene-reactions-for-peptide-and-protein-macrocyclizations
#17
Yuanxiang Wang, Benjamin J Bruno, Sean Cornillie, Jason M Nogieira, Diao Chen, Thomas E Cheatham, Carol S Lim, Danny Hung-Chieh Chou
The application of thiol-yne/thiol-ene reactions to synthesize mono- and bicyclic-stapled peptides and proteins is reported. First, a thiol-ene-based peptide-stapling method in aqueous conditions was developed. This method enabled the efficient stapling of recombinantly expressed coil-coiled proteins. The resulting stapled protein demonstrated higher stability in its secondary structure than the unstapled version. Furthermore, a thiol-yne coupling was performed by using an α,ω-diyne to react with two cysteine residues to synthesize a stapled peptide with two vinyl sulfide groups...
May 23, 2017: Chemistry: a European Journal
https://www.readbyqxmd.com/read/28342286/switching-aurora-a-kinase-on-and-off-at-an-allosteric-site
#18
REVIEW
Richard Bayliss, Selena G Burgess, Patrick J McIntyre
Protein kinases are central players in the regulation of cell cycle and signalling pathways. Their catalytic activities are strictly regulated through post-translational modifications and protein-protein interactions that control switching between inactive and active states. These states have been studied extensively using protein crystallography, although the dynamic nature of protein kinases makes it difficult to capture all relevant states. Here, we describe two recent structures of Aurora-A kinase that trap its active and inactive states...
March 25, 2017: FEBS Journal
https://www.readbyqxmd.com/read/28340032/osptr7-osnpf8-1-a-putative-peptide-transporter-in-rice-is-involved-in-dimethylarsenate-accumulation-in-rice-grain
#19
Zhong Tang, Yi Chen, Fei Chen, Yuchen Ji, Fang-Jie Zhao
Rice (Oryza sativa) is a major dietary source of arsenic (As) for the population consuming rice as their staple food. Rice grain contains both inorganic As and methylated As species, especially dimethyarsinate (DMA). DMA is highly mobile in long-distance translocation in plants, but the underlying mechanism remains unknown. In the present study, we showed that OsPTR7 (OsNPF8.1), a putative peptide transporter in rice, was permeable to DMA in Xenopus laevis oocytes. Transient expression of the OsPTR7-green fluorescent protein (GFP) in tobacco protoplasts showed that OsPTR7 was localized in the cell plasma membrane...
May 1, 2017: Plant & Cell Physiology
https://www.readbyqxmd.com/read/28326635/structure-enabled-discovery-of-a-stapled-peptide-inhibitor-to-target-the-oncogenic-transcriptional-repressor-tle1
#20
Sally McGrath, Marcello Tortorici, Ludovic Drouin, Savade Solanki, Lewis Vidler, Isaac Westwood, Peter Gimeson, Rob vanMontfort, Swen Hoelder
TLE1 is an oncogenic transcriptional co-repressor that exerts its repressive effects through binding of transcription factors. Inhibition of this protein-protein interaction represents a putative cancer target but no small molecule inhibitors have been published for this challenging interface. In this manuscript, we report the structure enabled design and synthesis of a constrained peptide inhibitor of TLE1. Our design featured introduction of a four carbon atom linker into the peptide epitope found in many TLE1 binding partners...
March 22, 2017: Chemistry: a European Journal
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