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https://www.readbyqxmd.com/read/29776930/modifying-the-lantibiotic-mutacin-1140-for-increased-yield-activity-and-stability
#1
Mengxin Geng, Leif Smith
Mutacin 1140 belongs to the epidermin family of type AI lantibiotics. This family has a broad spectrum of activity against Gram-positive bacteria. The binding of mutacin 1140 to lipid II leads to the inhibition of cell wall synthesis. Pharmacokinetic experiments on type AI lantibiotics are generally discouraging for clinical applications due to their short half-life. The unprotected dehydrated and protease susceptible residues outside of the lanthionine rings may play a role in their short half-life in physiological settings...
May 18, 2018: Applied and Environmental Microbiology
https://www.readbyqxmd.com/read/29775778/the-genus-cordyceps-an-extensive-review-of-its-traditional-uses-phytochemistry-and-pharmacology
#2
REVIEW
Opeyemi Joshua Olatunji, Jian Tang, Adesola Tola, Florence Auberon, Omolara Oluwaniyi, Zhen Ouyang
The genus Cordyceps has about 750 identified species which are distributed in many regions of the World, but mainly found in South Asia, Europe and North America. The species of the genus are highly priced and are widely used as food and medicine for the treatment of various ailments. This present review compiles literature information on the ethno-medicinal, phytochemistry and pharmacological properties of species in the genus Cordyceps. In addition, the review also suggest recommendations for the future researches...
May 15, 2018: Fitoterapia
https://www.readbyqxmd.com/read/29775538/discovery-of-potent-and-centrally-active-6-substituted-5-fluoro-1-3-dihydro-oxazine-%C3%AE-secretase-bace1-inhibitors-via-active-conformation-stabilization
#3
Kenji Nakahara, Kouki Fuchino, Kazuo Komano, Naoya Asada, Genta Tadano, Tsuyoshi Hasegawa, Takahiko Yamamoto, Yusuke Sako, Masayoshi Ogawa, Chie Unemura, Motoko Hosono, Hisanori Ito, Gaku Sakaguchi, Shigeru Ando, Shuichi Ohnishi, Yasuto Kido, Tamio Fukushima, Deborah Dhuyvetter, Herman Borghys, Harrie J M Gijsen, Yoshinori Yamano, Yasuyoshi Iso, Ken-Ichi Kusakabe
β-Secretase (BACE1) has an essential role in the production of amyloid β peptides that accumulate in patients with Alzheimer's disease (AD). Thus, inhibition of BACE1 is considered to be a disease-modifying approach for the treatment of AD. Our hit-to-lead efforts led to a cellular potent 1,3-dihydro-oxazine 6, which however inhibited hERG and showed high P-gp efflux. The close analog of 5-fluoro-oxazine 8 reduced P-gp efflux; further introduction of electron withdrawing groups at the 6-position improved potency and also mitigated P-gp efflux and hERG inhibition...
May 18, 2018: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29773065/copper-catalyzed-azide-alkyne-cycloaddition-cuaac-mediated-macrocylization-of-peptides-impact-on-conformation-and-biological-activity
#4
Chiara Testa, Anna Maria Papini, Michael Chorev, Paolo Rovero
The long lasting impetus to design novel modes of macrocyclization, and their implementation into a wide range of bioactive peptides, originates from their contributions to the restriction of conformational space and the stabilization of preferential bioactive conformations that support higher efficacy and binding affinity to cognate macromolecular targets, improved specificity and lowering susceptibility to enzymatic degradation processes. Introducing CuI-catalyzed azide-alkyne cycloadditon (CuAAC), a prototypical click reaction, to the field of peptide sciences as a bio-orthogonal reaction that generates a disubstituted-[1,2,3]triazol-1-yl moiety as a pseudopeptidic bond that is peptidomimetic in nature, paved the way to its wide spread application as a new and promising mode of macrocyclization...
May 17, 2018: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/29773063/conversion-of-protein-active-regions-into-peptidomimetic-therapeutic-leads-using-backbone-cyclization-and-cycloscan-how-to-do-it-yourself
#5
Samuel J S Rubin, Yftah Tal-Gan, Chaim Gilon, Nir Qvit
Protein-protein interactions (PPIs) are particularly important for controlling both physiologic and pathologic biological processes but are difficult to target due to their large and/or shallow interaction surfaces unsuitable for small molecules. Linear peptides found in nature interact with some PPIs, and protein active regions can be used to design synthetic peptide compounds for inhibition of PPIs. However, linear peptides are limited therapeutically by poor metabolic and conformational stability, which can compromise their bioactivity and half-life...
May 17, 2018: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/29773062/backbone-cyclized-peptides-a-critical-review
#6
Samuel J S Rubin, Nir Qvit
Backbone-cyclized peptides and peptidomimetics integrate the biological activity and pharmacological features necessary for successful research tools and therapeutics. In general, these structures demonstrate improved maintenance of bioactive conformation, stability and cell permeability compared to their linear counterparts, while maintaining support for a variety of side chain chemistries. We explain how backbone cyclization and cycloscan techniques allow scientists to cyclize linear peptides with retained or enhanced biological activity and improved drug-like features...
May 17, 2018: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/29772211/synthesis-folding-structure-and-activity-of-a-predicted-peptide-from-the-sea-anemone-oulactis-sp-with-an-shkt-fold
#7
Bankala Krishnarjuna, Jessica Villegas-Moreno, Michela L Mitchell, Agota Csoti, Steve Peigneur, Carlos Amero, Michael W Pennington, Jan Tytgat, Gyorgy Panyi, Raymond S Norton
Sea anemone venom is rich in bioactive compounds, including peptides containing multiple disulfide bridges. In a transcriptomic study on Oulactis sp., we identified the putative 36-residue peptide, OspTx2b, which is an isoform of the KV channel blocker OspTx2a (Sunanda P et al. (2018) Identification, chemical synthesis, structure and function of a new KV 1 channel blocking peptide from Oulactis sp. Peptide Science, in press). As OspTx2b contains a ShK/BgK-like cysteine framework, with high amino acid sequence similarity to BgK, we were interested to investigate its structure and function...
May 14, 2018: Toxicon: Official Journal of the International Society on Toxinology
https://www.readbyqxmd.com/read/29771457/transition-metal-ions-mediated-tyrosine-based-short-peptide-amphiphile-nanostructures-inhibit-bacterial-growth
#8
Khashti Ballabh Joshi, Ramesh Singh, Narendra Kumar Mishra, Vikas Kumar, Vandana Vinayak
We report the design and synthesis of biocompatible small peptide based molecule for the controlled and targeted delivery of the encapsulated bioactive metal ions via transforming their internal nanostructures. Tyrosine based short peptide amphiphile (sPA) was synthesized which self-assembled into β-sheet like secondary structures. The self assembly of the designed sPA was modulated by using different bioactive transition metal ions which is confirmed by spectroscopic and microscopic techniques. These bioactive metal ions conjugated sPA hybrid structures are further used to develop antibacterial materials...
May 17, 2018: Chembiochem: a European Journal of Chemical Biology
https://www.readbyqxmd.com/read/29770392/promotion-of-neurite-outgrowth-by-rationally-designed-ngf-%C3%AE-binding-peptide-nanofibers
#9
Zeynep Okur, Oya I Senturk, Canelif Yilmaz, Gulcihan Gulseren, Busra Mammadov, Mustafa O Guler, Ayse B Tekinay
Promotion of neurite outgrowth is an important limiting step for regeneration in nerve injury and depends strongly on the local expression of nerve growth factor (NGF). The rational design of bioactive materials is a promising approach for the development of novel therapeutic methods for nerve regeneration, and biomaterials capable of presenting NGF to nerve cells are especially suitable for this purpose. In this study, we show bioactive peptide amphiphile (PA) nanofibers capable of promoting neurite outgrowth by displaying high density binding epitopes for NGF...
May 17, 2018: Biomaterials Science
https://www.readbyqxmd.com/read/29768188/micropatterned-biodegradable-polyesters-clicked-with-cqaasikvav-promote-cell-alignment-directional-migration-and-neurite-outgrowth
#10
Deteng Zhang, Sai Wu, Jianyong Feng, Yiyuan Duan, Dongming Xing, Changyou Gao
The interplay of microstructures and biological cues is critical to regulate the behaviors of Schwann cells (SCs) in terms of cellular spatial arrangement and directional migration as well as neurite orientation for bridging the proximal and distal stumps of the injured peripheral nervous system. In this study, stripe micropatterns having ridges/grooves of width 20/20 and 20/40 μm were fabricated on the surface of maleimide-functionalized biodegradable poly(ester carbonate) (P(LLA-MTMC)) films by the polydimethylsiloxane mold-pressing method, respectively...
May 13, 2018: Acta Biomaterialia
https://www.readbyqxmd.com/read/29767957/magnetic-manipulation-of-reversible-nanocaging-controls-in-vivo-adhesion-and-polarization-of-macrophages
#11
Heemin Kang, Hee Joon Jung, Sung Kyu Kim, Dexter Siu Hong Wong, Sien Lin, Gang Li, Vinayak P Dravid, Liming Bian
Macrophages are key immune cells that perform various physiological functions, such as the maintenance of homeostasis, host defense, disease progression, and tissue regeneration. Macrophages adopt distinctly polarized phenotypes, such as pro-inflammatory M1 phenotype or anti-inflammatory (pro-healing) M2 phenotype, to execute disparate functions. The remotely controlled reversible uncaging of bioactive ligands, such as Arg-Gly-Asp (RGD) peptide, is an appealing approach for temporally regulating the adhesion and resultant polarization of macrophages on the implants in vivo...
May 16, 2018: ACS Nano
https://www.readbyqxmd.com/read/29764719/potential-use-of-bitter-melon-momordica-charantia-derived-compounds-as-antidiabetics-in-silico-and-in-vivo-studies
#12
Olusola Olalekan Elekofehinti, Esther Opeyemi Ariyo, Moses Orimoloye Akinjiyan, Olanrewaju Sam Olayeriju, Akeem Olalekan Lawal, Isaac Gbadura Adanlawo, Joao Batista Teixeira Rocha
Momordica charantia (bitter lemon) belongs to the cucurbitaceae family which has been extensively used in traditional medicines for the cure of various ailments such as cancer and diabetes. The underlying mechanism of M. charantia to maintain glycemic control was investigated. GLP-1 and DPP-4 gene modulation by M. charantia (5-20% inclusion in rats diet) was investigated in vivo by RT-PCR and possible compounds responsible for diabetic action predicted through in silico approach. Phytochemicalss previously characterized from M...
May 12, 2018: Pathophysiology: the Official Journal of the International Society for Pathophysiology
https://www.readbyqxmd.com/read/29764301/bioinspired-biocompatible-and-peptide-decorated-silk-fibroin-coatings-for-enhanced-osteogenesis-of-bioinert-implant
#13
Chunyan Wang, Shengnan Wang, Yuanyi Yang, Zhuo Jiang, Yi Deng, Shaoli Song, Weizhong Yang, Zhi-Gang Chen
In this study, we develop an osteopromotive polyetheretherketone (PEEK) implant decorated with silk fibroin and bone forming peptide, in which the surface of bioinert PEEK implant is firstly sulfonated to form a three-dimensional, porous topography and then is functionalized with silk fibroin via spin-coating process and peptide decoration. The bio-test results show that cells on the functional bioinert implants exhibit better cell adhesion, proliferation and spreading, when compared with the uncoated ones...
May 15, 2018: Journal of Biomaterials Science. Polymer Edition
https://www.readbyqxmd.com/read/29758266/alanine-rich-peptide-from-populus-trichocarpa-inhibit-growth-of-staphylococcus-aureus-via-targetting-its-extracellular-domain-of-sensor-histidine-kinase-yycgex-protein
#14
Raid Al Akeel, Ayesha Mateen, Rabbani Syed, Mohammed S Al-Qahtani, A Alqahtani
BACKGROUND: Due to growing concern towards microbial resistance, ongoing search for developing novel bioactive compounds such as peptides is on rise. The aim of this study was to evaluate antimicrobial effect of Populus trichocarpa extract, chemically identify the active peptide fraction and finds its target in Staphylococcus aureus. METHODS: In this study the active fraction of P. trichocarpa crude extract was purified and characterized using MS/MS. This peptide PT13 antimicrobial activity was confirmed by in-vitro agar based disk diffusion and in-vivo infection model of G...
May 11, 2018: Microbial Pathogenesis
https://www.readbyqxmd.com/read/29757237/investigation-of-the-anti-prostate-cancer-properties-of-marine-derived-compounds
#15
REVIEW
Meiqi Fan, Amit Kumar Nath, Yujiao Tang, Young-Jin Choi, Trishna Debnath, Eun-Ju Choi, Eun-Kyung Kim
This review focuses on marine compounds with anti-prostate cancer properties. Marine species are unique and have great potential for the discovery of anticancer drugs. Marine sources are taxonomically diverse and include bacteria, cyanobacteria, fungi, algae, and mangroves. Marine-derived compounds, including nucleotides, amides, quinones, polyethers, and peptides are biologically active compounds isolated from marine organisms such as sponges, ascidians, gorgonians, soft corals, and bryozoans, including those mentioned above...
May 12, 2018: Marine Drugs
https://www.readbyqxmd.com/read/29756539/skin-regeneration-with-a-scaffold-of-predefined-shape-and-bioactive-peptide-hydrogels
#16
Heejung Im, Su Hee Kim, Soo Hyun Kim, Youngmee Jung
We developed a highly elastic customized scaffold for soft-tissue regeneration and combined them with bioactive hydrogels with stem-cell-inducing ability. This was done to mimic mechanical properties of native soft tissues and improve the viability of transplanted cells as well as efficiency of tissue regeneration. The proposed study was aimed at evaluating various characteristics of scaffolds and investigating their tissue regenerating ability. Finger shaped porous scaffolds were successfully fabricated by an indirect 3D printing of poly (L-lactide-co-ε-caprolactone) (PLCL) which provides a high elasticity for soft tissue engineering...
May 14, 2018: Tissue Engineering. Part A
https://www.readbyqxmd.com/read/29752337/oa-gl21-a-novel-bioactive-peptide-from-odorrana-andersonii-accelerated-the-healing-of-skin-wounds
#17
Wenxin Bian, Buliang Meng, Xiaojie Li, Siyuan Wang, Xiaoqing Cao, Naixin Liu, Meifeng Yang, Jing Tang, Ying Wang, Xinwang Yang
Nowadays, the number of chronic trauma cases caused by variety of factors such as the world's population-aging and chronic diseases is increasing steadily, and thus effective treatment for chronic wounds has become a severe clinical challenge, which also burdens the patient both physically and financially. Therefore, it is urgent to develop new drugs to accelerate the healing of wounds. Bioactive peptides, which are relatively low cost, easy to produce, store and transport, have become an excellent choice. In this research, we identified a novel peptide OA-GL21, with an amino acid sequence of 'GLLSGHYGRVVSTQSGHYGRG', from the skin secretions of Odorrana andersonii...
May 11, 2018: Bioscience Reports
https://www.readbyqxmd.com/read/29751919/effect-of-enzymatic-hydrolysis-on-bioactive-properties-and-allergenicity-of-cricket-gryllodes-sigillatus-protein
#18
Felicia Hall, Philip E Johnson, Andrea Liceaga
Food-derived bioactive peptides have gained attention for their role in preventing chronic diseases. Edible insects are viable sources of bioactive peptides owing to their high protein content and sustainable production. In this study, whole crickets (Gryllodes sigillatus) were alcalase-hydrolyzed to a degree of hydrolysis (DH) ranging from 15 to 85%. Antioxidant activity, angiotensin converting enzyme (ACE), and dipeptidyl peptidase-4 (DPP-IV)- inhibition of the cricket protein hydrolysates (CPH) were evaluated before and after simulated gastrointestinal digestion (SGD)...
October 1, 2018: Food Chemistry
https://www.readbyqxmd.com/read/29750291/collagen-peptides-from-soft%C3%A2-shelled-turtle-induce-calpain%C3%A2-1-expression-and-regulate-inflammatory-cytokine-expression-in-hacat-human-skin-keratinocytes
#19
Tetsushi Yamamoto, Saori Nakanishi, Kuniko Mitamura, Atsushi Taga
Collagen peptides (CPs), derived by hydrolyzing collagen with chemicals or enzymes, are often used as functional materials, due to their various bioactivities and high bioavailability. A previous study by our group reported that collagen from soft‑shelled turtle, Pelodiscus sinensis, induces keratinocytes to undergo epithelial‑mesenchymal transition and facilitates wound healing. Therefore, CPs derived from soft‑shelled turtle collagen may have useful effects on the skin. In the present study, the functional effects of CPs on human skin were examined by analyzing CP‑treated human keratinocytes with a shotgun liquid chromatography/mass spectrometry‑based global proteomic approach...
May 8, 2018: International Journal of Molecular Medicine
https://www.readbyqxmd.com/read/29747543/activation-of-%C3%AE-and-%C3%AE-carbonic-anhydrases-from-pathogenic-bacteria-with-tripeptides
#20
Azzurra Stefanucci, Andrea Angeli, Marilisa Pia Dimmito, Grazia Luisi, Sonia Del Prete, Clemente Capasso, William A Donald, Adriano Mollica, Claudiu T Supuran
Six tripeptides incorporating acidic amino acid residues were prepared for investigation as activators of β- and γ-carbonic anhydrases (CAs, EC 4.2.1.1) from the pathogenic bacteria Vibrio cholerae, Mycobacterium tuberculosis, and Burkholderia pseudomallei. The primary amino acid residues that are involved in the catalytic mechanisms of these CA classes are poorly understood, although glutamic acid residues near the active site appear to be involved. The tripeptides that contain Glu or Asp residues can effectively activate VchCAβ and VchCAγ (enzymes from V...
December 2018: Journal of Enzyme Inhibition and Medicinal Chemistry
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