keyword
MENU ▼
Read by QxMD icon Read
search

Biologic Scaffold

keyword
https://www.readbyqxmd.com/read/28342744/synthesis-and-anti-cancer-activity-of-chiral-tetrahydropyrazolo-1-5-a-pyridine-fused-steroids
#1
Susana M M Lopes, Emanuel P Sousa, Luísa Barreira, Cátia Marques, Maria João Rodrigues, Teresa M V D Pinho E Melo
Regio- and stereoselective synthesis of novel chiral 4,5,6,7-tetrahydropyrazolo[1,5-a]pyridine-fused steroids via [8π+2π] cycloaddition of diazafulvenium methides with steroidal scaffolds is reported. The biological evaluation of the new family of hexacyclic steroids as anti-cancer agents was also carried out. Hexacyclic steroids bearing a benzyl group at C-22, derived from 16-dehydropregnenolone and 16-dehydroprogesterone, show considerable cytotoxicity against EL4 (murine T-lymphoma) in contrast with the corresponding C-22-unsubstituted derivatives showing low cytotoxicity...
March 22, 2017: Steroids
https://www.readbyqxmd.com/read/28342366/discovery-of-new-dual-ppar%C3%AE-gpr40-agonists-with-robust-antidiabetic-activity-design-synthesis-and-in-combo-drug-evaluation
#2
Sergio Hidalgo-Figueroa, Gabriel Navarrete-Vázquez, Samuel Estrada-Soto, Diana Giles-Rivas, Francisco J Alarcón-Aguilar, Ismael León-Rivera, Abraham Giacoman-Martínez, Elizabeth Miranda Pérez, Julio C Almanza-Pérez
The design of compounds 1 and 2 was based on the similar scaffold of pharmacophoric groups for PPARγ and GPR40 agonists. In order to find new compounds with improved biological activity, the current manuscript describes a new dual PPARγ-GPR40 agonist. We synthesized two compounds, which were prepared following a multistep synthetic route, and the relative mRNA expression levels of PPARγ, GLUT4, and GPR40 were quantified in cell culture, as well as insulin secretion and [Ca(2+)] intracellular levels. Compound 1 showed a 7-times increase in the mRNA expression of PPARγ, which in turn enhanced the expression levels of GLUT4 respect to control and pioglitazone...
March 22, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28340368/synthesis-molecular-docking-antimycobacterial-and-antimicrobial-evaluation-of-new-pyrrolo-3-2-c-pyridine-mannich-bases
#3
Gilish Jose, Tholappanavara H Suresha Kumara, Haliwana B V Sowmya, Dharmarajan Sriram, Tayur N Guru Row, Amar A Hosamani, Sunil S More, Bhavya Janardhan, B G Harish, Sandeep Telkar, Yalegara Siddappa Ravikumar
In this report, we describe the synthesis and biological evaluation of a new series of pyrrolo[3,2-c]pyridine Mannich bases (7a-v). The Mannich bases were obtained in good yields by one-pot three component condensation of pyrrolo[3,2-c]pyridine scaffold (6a-c) with secondary amines and excess of formaldehyde solution in AcOH. The chemical structures of the compounds were characterized by (1)H NMR, (13)C NMR, LC/MS and elemental analysis. Single crystal X-ray diffraction has been recorded for compound 7k ([C23H29ClN4](+2), H2O)...
March 16, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28337329/antiparasitic-lead-discovery-toward-optimization-of-a-chemotype-with-activity-against-multiple-protozoan-parasites
#4
William Devine, Sarah M Thomas, Jessey Erath, Kelly A Bachovchin, Patricia J Lee, Susan E Leed, Ana Rodriguez, Richard J Sciotti, Kojo Mensa-Wilmot, Michael P Pollastri
Human African trypanosomiasis (HAT), Chagas disease, and leishmaniasis present a significant burden across the developing world. Existing therapeutics for these protozoal neglected tropical diseases suffer from severe side effects and toxicity. Previously, NEU-1045 (3) was identified as a promising lead with cross-pathogen activity, though it possessed poor physicochemical properties. We have designed a library of analogues with improved calculated physicochemical properties built on the quinoline scaffold of 3 incorporating small, polar aminoheterocycles in place of the 4-(3-fluorobenzyloxy)aniline substituent...
March 9, 2017: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28337318/development-of-18-f-maleimide-based-glycogen-synthase-kinase-3%C3%AE-ligands-for-positron-emission-tomography-imaging
#5
Kongzhen Hu, Debasis Patnaik, Thomas Lee Collier, Katarzyna N Lee, Han Gao, Matthew R Swoyer, Benjamin H Rotstein, Hema S Krishnan, Steven H Liang, Jin Wang, Zhiqiang Yan, Jacob M Hooker, Neil Vasdev, Stephen J Haggarty, Ming-Yu Ngai
Dysregulation of glycogen synthase kinase-3β (GSK-3β) is implicated in the pathogenesis of neurodegenerative and psychiatric disorders. Thus, development of GSK-3β radiotracers for positron emission tomography (PET) imaging is of paramount importance, because such a noninvasive imaging technique would allow better understanding of the link between the activity of GSK-3β and central nervous system disorders in living organisms, and it would enable early detection of the enzyme's aberrant activity. Herein, we report the synthesis and biological evaluation of a series of fluorine-substituted maleimide derivatives that are high-affinity GSK-3β inhibitors...
March 9, 2017: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28337223/emerging-perspectives-in-scaffold-for-tissue-engineering-in-oral-surgery
#6
REVIEW
Gabriele Ceccarelli, Rossella Presta, Laura Benedetti, Maria Gabriella Cusella De Angelis, Saturnino Marco Lupi, Ruggero Rodriguez Y Baena
Bone regeneration is currently one of the most important and challenging tissue engineering approaches in regenerative medicine. Bone regeneration is a promising approach in dentistry and is considered an ideal clinical strategy in treating diseases, injuries, and defects of the maxillofacial region. Advances in tissue engineering have resulted in the development of innovative scaffold designs, complemented by the progress made in cell-based therapies. In vitro bone regeneration can be achieved by the combination of stem cells, scaffolds, and bioactive factors...
2017: Stem Cells International
https://www.readbyqxmd.com/read/28336879/in-vitro-and-in-vivo-evaluation-of-a-three-dimensional-porous-multi-walled-carbon-nanotube-scaffold-for-bone-regeneration
#7
Manabu Tanaka, Yoshinori Sato, Mei Zhang, Hisao Haniu, Masanori Okamoto, Kaoru Aoki, Takashi Takizawa, Kazushige Yoshida, Atsushi Sobajima, Takayuki Kamanaka, Hiroyuki Kato, Naoto Saito
Carbon nanotubes (CNTs) have attracted a great deal of attention for the biological and medical science fields because of their characteristic physical and biological properties. In this study, we investigated the capacity of the 3D porous CNT scaffold (CNT porous block; CNTp) for bone regenerative medicine. Surface observations using a scanning electron microscope (SEM), crystal depositions on the surface of CNTps immersed in simulated body fluid (SBF), and evaluations of protein adsorption and controlled releasing were conducted to assess physical properties...
February 17, 2017: Nanomaterials
https://www.readbyqxmd.com/read/28336598/draft-genome-sequence-of-the-mycoparasitic-oomycete-pythium-periplocum-strain-cbs-532-74
#8
Sandeep K Kushwaha, Ramesh R Vetukuri, Laura J Grenville-Briggs
The oomycete Pythium periplocum is an aggressive mycoparasite of a number of plant pathogenic fungi and oomycetes and therefore has potential as a biological control agent. Here, we report the first draft genome sequence of P. periplocum, which comprises 35.89 Mb. It contains 1,043 scaffolds and 14,399 predicted protein-coding genes.
March 23, 2017: Genome Announcements
https://www.readbyqxmd.com/read/28336399/synthetic-matrix-of-polyether-polyurethane-as-a-biological-platform-for-pancreatic-regeneration
#9
Luciana Xavier Pereira, Celso Tarso Rodrigues Viana, Laura Alejandra Ariza Orellano, Simone Aparecida de Almeida, Anilton Cesar Vasconcelos, Alfredo de Miranda Goes, Alexander Birbrair, Silvia Passos Andrade, Paula Peixoto Campos
AIMS: Several alternative cellular approaches using biomaterials to host insulin-producing cells derived from stem cells have been developed to overcome the limitations of type 1 diabetes treatment (exogenous insulin injection). However, none seem to fulfill all requirements needed to induce pancreatic cells successful colonization of the scaffolds. Here, we report a polymeric platform adherent to the native mice pancreas filled with human adipose stem cells (hASCs) that was able to induce growth of pancreatic parenchyma...
March 20, 2017: Life Sciences
https://www.readbyqxmd.com/read/28335186/ex-vivo-tissues-engineering-modeling-for-reconstructive-surgery-using-human-adult-adipose-stem-cells-and-polymeric-nanostructured-matrix
#10
Francesco Morena, Chiara Argentati, Eleonora Calzoni, Marino Cordellini, Carla Emiliani, Francesco D'Angelo, Sabata Martino
The major challenge for stem cell translation regenerative medicine is the regeneration of damaged tissues by creating biological substitutes capable of recapitulating the missing function in the recipient host. Therefore, the current paradigm of tissue engineering strategies is the combination of a selected stem cell type, based on their capability to differentiate toward committed cell lineages, and a biomaterial, that, due to own characteristics (e.g., chemical, electric, mechanical property, nano-topography, and nanostructured molecular components), could serve as active scaffold to generate a bio-hybrid tissue/organ...
March 31, 2016: Nanomaterials
https://www.readbyqxmd.com/read/28334966/structural-and-mechanistic-insights-into-regulation-of-hbo1-histone-acetyltransferase-activity-by-brpf2
#11
Ye Tao, Chen Zhong, Junjun Zhu, Shutong Xu, Jianping Ding
HBO1, a member of the MYST family of histone acetyltransferases (HATs), is required for global acetylation of histone H3K14 and embryonic development. It functions as a catalytic subunit in multisubunit complexes comprising a BRPF1/2/3 or JADE1/2/3 scaffold protein, and two accessory proteins. BRPF2 has been shown to be important for the HAT activity of HBO1 toward H3K14. Here we demonstrated that BRPF2 can regulate the HAT activity of HBO1 toward free H3 and H4, and nucleosomal H3. Particularly, a short N-terminal region of BRPF2 is sufficient for binding to HBO1 and can potentiate its activity toward H3K14...
February 24, 2017: Nucleic Acids Research
https://www.readbyqxmd.com/read/28334215/systematic-inference-of-functional-phosphorylation-events-in-yeast-metabolism
#12
Yu Chen, Yonghong Wang, Jens Nielsen
Motivation: Protein phosphorylation is a post-translational modification that affects proteins by changing their structure and conformation in a rapid and reversible way, and it is an important mechanism for metabolic regulation in cells. Phosphoproteomics enables high-throughput identification of phosphorylation events on metabolic enzymes, but identifying functional phosphorylation events still requires more detailed biochemical characterization. Therefore, development of computational methods for investigating unknown functions of a large number of phosphorylation events identified by phosphoproteomics has received increased attention...
March 2, 2017: Bioinformatics
https://www.readbyqxmd.com/read/28330896/cell-specific-variation-in-e-selectin-ligand-expression-among-human-peripheral-blood-mononuclear-cells-implications-for-immunosurveillance-and-pathobiology
#13
Mariana Silva, Ronald Kam Fai Fung, Conor Brian Donnelly, Paula Alexandra Videira, Robert Sackstein
Both host defense and immunopathology are shaped by the ordered recruitment of circulating leukocytes to affected sites, a process initiated by binding of blood-borne cells to E-selectin displayed at target endothelial beds. Accordingly, knowledge of the expression and function of leukocyte E-selectin ligands is key to understanding the tempo and specificity of immunoreactivity. In this study, we performed E-selectin adherence assays under hemodynamic flow conditions coupled with flow cytometry and Western blot analysis to elucidate the function and structural biology of glycoprotein E-selectin ligands expressed on human PBMCs...
March 22, 2017: Journal of Immunology: Official Journal of the American Association of Immunologists
https://www.readbyqxmd.com/read/28330463/global-transcriptome-analysis-of-huperzia-serrata-and-identification-of-critical-genes-involved-in-the-biosynthesis-of-huperzine-a
#14
Mengquan Yang, Wenjing You, Shiwen Wu, Zhen Fan, Baofu Xu, Mulan Zhu, Xuan Li, Youli Xiao
BACKGROUND: Huperzia serrata (H. serrata) is an economically important traditional Chinese herb with the notably medicinal value. As a representative member of the Lycopodiaceae family, the H. serrata produces various types of effectively bioactive lycopodium alkaloids, especially the huperzine A (HupA) which is a promising drug for Alzheimer's disease. Despite their medicinal importance, the public genomic and transcriptomic resources are very limited and the biosynthesis of HupA is largely unknown...
March 22, 2017: BMC Genomics
https://www.readbyqxmd.com/read/28328217/development-of-a-selective-inhibitor-of-protein-arginine-deiminase-2
#15
Aaron Muth, Venkataraman Subramanian, Edward Beaumont, Mitesh Nagar, Philip Kerry, Paul McEwan, Hema Srinath, Kathleen Wanda Clancy, Sangram S Parelkar, Paul R Thompson
Protein arginine deiminase 2 (PAD2) plays a key role in the onset and progression of multiple sclerosis, rheumatoid arthritis and breast cancer. To date, no PAD2-selective inhibitor has been developed. Such a compound will be critical for elucidating the biological roles of this isozyme and may ultimately be useful for treating specific diseases in which PAD2 activity is dysregulated. To achieve this goal, we synthesized a series of benzimidazole-based derivatives of Cl-amidine, hypothesizing that this scaffold would allow access to a series of PAD2-selective inhibitors with enhanced cellular efficacy...
March 22, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28327996/genome-sequencing-of-the-sweetpotato-whitefly-bemsia-tabaci-med-q
#16
Wen Xie, Chunhai Chen, Zezhong Yang, Litao Guo, Xin Yang, Dan Wang, Ming Chen, Jinqun Huang, Yanan Wen, Yang Zeng, Yating Liu, Jixing Xia, Lixia Tian, Hongying Cui, Qingjun Wu, Shaoli Wang, Baoyun Xu, Xianchun Li, Xinqiu Tan, Murad Ghanim, Baoli Qiu, Huipeng Pan, Dong Chu, Helene Delatte, M N Maruthi, Feng Ge, Xueping Zhou, Xiaowei Wang, Fanghao Wan, Yuzhou Du, Chen Luo, Fengming Yan, Evan L Preisser, Xiaoguo Jiao, Brad S Coates, Jinyang Zhao, Qiang Gao, Jinquan Xia, Ye Yin, Yong Liu, Judith K Brown, Xuguo Joe Zhou, Youjun Zhang
Background: The sweetpotato whitefly Bemisia tabaci is a highly destructive agricultural and ornamental crop pest. It damages host plants through both phloem feeding and vectoring plant pathogens. Introductions of B. tabaci are difficult to quarantine and eradicate because of its high reproductive rates, broad host plant range, and insecticide resistance. Findings: A total of 791 Gb of raw DNA sequence from whole genome shotgun sequencing, and 13 BAC pooling libraries were generated by Illumina sequencing using different combinations of mate-pair and pair-end libraries...
March 15, 2017: GigaScience
https://www.readbyqxmd.com/read/28327943/whole-genome-sequencing-of-chinese-clearhead-icefish-protosalanx-hyalocranius
#17
Kai Liu, Dongpo Xu, Jia Li, Chao Bian, Jinrong Duan, Yanfeng Zhou, Minying Zhang, Xinxin You, Yang You, Jieming Chen, Hui Yu, Gangchun Xu, Di-An Fang, Jun Qiang, Shulun Jiang, Jie He, Junmin Xu, Qiong Shi, Zhiyong Zhang, Pao Xu
Background: Chinese clearhead icefish, Protosalanx hyalocranius , is a representative icefish species with economic importance and special appearance. Due to its great economic values in China, the fish was introduced into Lake Dianchi and several other lakes from the Lake Taihu half a century ago. Similar to the Sinocyclocheilus cavefish, the clearhead icefish has certain cavefish-like traits, such as transparent body and nearly scaleless skin. Here, we provide the whole genome sequence of this surface-dwelling fish and generated a draft genome assembly, aiming at exploring molecular mechanisms for the biological interests...
February 24, 2017: GigaScience
https://www.readbyqxmd.com/read/28327307/discovery-characterization-and-biological-evaluation-of-a-novel-r-4-4-difluoropiperidine-scaffold-as-dopamine-receptor-4-d4r-antagonists
#18
Daniel E Jeffries, Jonathan O Witt, Andrea L McCollum, Kayla J Temple, Miguel A Hurtado, Joel M Harp, Anna L Blobaum, Craig W Lindsley, Corey R Hopkins
Herein, we report the synthesis and structure-activity relationship of a novel series of (R)-4,4-difluoropiperidine core scaffold as dopamine receptor 4 (D4) antagonists. A series of compounds from this scaffold are highly potent against the D4 receptor and selective against the other dopamine receptors. In addition, we were able to confirm the active isomer as the (R)-enantiomer via an X-ray crystal structure.
December 1, 2016: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28326549/the-three-finger-toxin-fold-a-multifunctional-structural-scaffold-able-to-modulate-cholinergic-functions
#19
REVIEW
Pascal Kessler, Pascale Marchot, Marcela Silva, Denis Servent
Three-finger fold toxins are miniproteins frequently found in Elapidae snake venoms. This fold is characterized by three distinct loops rich in β-strands and emerging from a dense, globular core reticulated by four highly conserved disulfide bridges. The number and diversity of receptors, channels, and enzymes identified as targets of three-finger fold toxins is increasing continuously. Such manifold diversity highlights the specific adaptability of this fold for generating pleiotropic functions. Although this toxin superfamily disturbs many biological functions by interacting with a large diversity of molecular targets, the most significant target is the cholinergic system...
March 21, 2017: Journal of Neurochemistry
https://www.readbyqxmd.com/read/28325314/the-use-of-calcium-ions-instead-of-heat-treatment-for-%C3%AE-1-3-glucan-gelation-improves-biocompatibility-of-the-%C3%AE-1-3-glucan-ha-bone-scaffold
#20
Katarzyna Klimek, Agata Przekora, Aleksandra Benko, Wiktor Niemiec, Marta Blazewicz, Grazyna Ginalska
The aim of this study was to determine which procedure for β-1,3-glucan gelation - newly developed dialysis against calcium salt or described in the literature thermal technique - is more appropriate for fabrication of a biomaterial designed for bone tissue engineering applications. Thus, β-1,3-glucan/hydroxyapatite scaffolds were prepared based on two different methods and their physicochemical, microstructural, and biological properties were compared. Obtained results demonstrated that unlike thermal method-prepared β-1,3-glucan/hydroxyapatite material (glu/HAT), bone scaffold fabricated via dialysis method (glu/HA D) possessed rough surface resulting from the presence of CaCl2 precipitates as proven by SEM and EDS analysis...
May 15, 2017: Carbohydrate Polymers
keyword
keyword
76657
1
2
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read
×

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"