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https://www.readbyqxmd.com/read/28527823/antiviral-escin-derivatives-from-the-seeds-of-aesculus-turbinata-blume-japanese-horse-chestnut
#1
Ji Won Kim, Thi-Kim-Quy Ha, Hyomoon Cho, Eunhee Kim, Sang Hee Shim, Jun-Li Yang, Won Keun Oh
Porcine epidemic diarrhea virus (PEDV) causes severe diarrhea and high fatality of piglets, influencing the swine industry. Japanese horse chestnut (seed of Aesculus turbinata) contains many saponin mixtures, called escins, and has been used for a long time as a traditional medicinal plant. Structure-activity relationship (SAR) studies on escins have revealed that acylations at C-21 and C-22 with angeloyl or tigloyl groups were important for their cytotoxic effects. However, the strong cytotoxicity of escins makes them hard to utilize for other diseases and to develop as nutraceuticals...
May 8, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28526475/identification-and-preliminary-structure-activity-relationships-of-1-indanone-derivatives-as-novel-indoleamine-2-3-dioxygenase-1-ido1-inhibitors
#2
Dingding Gao, Yingxia Li
Indoleamine 2,3-dioxygenase 1 (IDO1) plays a vital role in the catabolism of tryptophan along with the kynurenine pathway which is involved in many human diseases including cancer, Alzheimer's disease, etc. In this study, compound 1 bearing a 1-Indanone scaffold was identified as a novel IDO1 inhibitor by structure-based virtual screening, with moderate to good enzymatic and cellular inhibitory activities. Also, surface plasmon resonance analysis validated the direct interaction between compound 1 and IDO1 protein...
May 10, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28525279/double-winged-3-hydroxypyrimidine-2-4-diones-potent-and-selective-inhibition-against-hiv-1-rnase-h-with-significant-antiviral-activity
#3
Sanjeev Kumar V Vernekar, Jing Tang, Bulan Wu, Andrew D Huber, Mary C Casey, Nataliya S Myshakina, Daniel J Wilson, Jayakanth Kankanala, Karen A Kirby, Michael A Parniak, Stefan G Sarafianos, Zhengqiang Wang
Human immunodeficiency virus (HIV) reverse transcriptase (RT)-associated ribonuclease H (RNase H) remains the only virally encoded enzymatic function yet to be exploited as an antiviral target. One of the possible challenges may be that targeting HIV RNase H is confronted with a steep substrate barrier. We have previously reported a 3-hydroxypyrimidine-2,4-dione (HPD) subtype that potently and selectively inhibited RNase H without inhibiting HIV in cell culture. We report herein a critical redesign of the HPD chemotype featuring an additional wing at the C5 position that led to drastically improved RNase H inhibition and significant antiviral activity...
May 19, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28523281/imaging-membrane-potential-changes-from-dendritic-spines-using-computer-generated-holography
#4
Dimitrii Tanese, Ju-Yun Weng, Valeria Zampini, Vincent De Sars, Marco Canepari, Balazs Rozsa, Valentina Emiliani, Dejan Zecevic
Electrical properties of neuronal processes are extraordinarily complex, dynamic, and, in the general case, impossible to predict in the absence of detailed measurements. To obtain such a measurement one would, ideally, like to be able to monitor electrical subthreshold events as they travel from synapses on distal dendrites and summate at particular locations to initiate action potentials. It is now possible to carry out these measurements at the scale of individual dendritic spines using voltage imaging. In these measurements, the voltage-sensitive probes can be thought of as transmembrane voltmeters with a linear scale, which directly monitor electrical signals...
July 2017: Neurophotonics
https://www.readbyqxmd.com/read/28522253/challenges-in-the-development-of-an-m4-pam-preclinical-candidate-the-discovery-sar-and-in-vivo-characterization-of-a-series-of-3-aminoazetidine-derived-amides
#5
James C Tarr, Michael R Wood, Meredith J Noetzel, Jeanette L Bertron, Rebecca L Weiner, Alice L Rodriguez, Atin Lamsal, Frank W Byers, Sichen Chang, Hyekyung P Cho, Carrie K Jones, Colleen M Niswender, Michael W Wood, Nicholas J Brandon, Mark E Duggan, P Jeffrey Conn, Thomas M Bridges, Craig W Lindsley
This letter details the continued chemical optimization of a novel series of M4 positive allosteric modulators (PAMs) based on a 5-amino-thieno[2,3-c]pyridazine core by incorporating a 3-amino azetidine amide moiety. The analogs described within this work represent the most potent M4 PAMs reported for this series to date. The SAR to address potency, clearance, subtype selectivity, CNS exposure, and P-gp efflux are described. This work culminated in the discovery of VU6000918, which demonstrated robust efficacy in a rat amphetamine-induced hyperlocomotion reversal model at a minimum efficacious dose of 0...
May 6, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28511989/biased-agonism-antagonism-at-the-angii-at1-receptor-implications-for-adrenal-aldosterone-production-and-cardiovascular-therapy
#6
REVIEW
Jennifer Maning, Shmuel Negussie, Michelle A Clark, Anastasios Lymperopoulos
Many of the effects of angiotensin II (AngII), including adrenocortical aldosterone release, are mediated by the AngII type 1 receptor (AT1R), a receptor with essential roles in cardiovascular homeostasis. AT1R belongs to the G protein-coupled receptor (GPCR) superfamily, mainly coupling to the Gq/11 type of G proteins. However, it also signals through βarrestins, oftentimes in parallel to eliciting G protein-dependent signaling. This has spurred infinite possibilities for cardiovascular pharmacology, since various beneficial effects are purportedly exerted by AT1R via βarrestins, unlike AT1R-induced G protein-mediated pathways that usually result in damaging cardiovascular effects, including hypertension and aldosterone elevation...
May 13, 2017: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
https://www.readbyqxmd.com/read/28508949/zn-ii-dipicolylamine-based-metallo-lipids-as-novel-non-viral-gene-vectors
#7
Rong-Chuan Su, Qiang Liu, Wen-Jing Yi, Zhi-Gang Zhao
In this study, a series of Zn(II)-dipicolylamine (Zn-DPA) based cationic lipids bearing different hydrophobic tails (long chains, α-tocopherol, cholesterol or diosgenin) were synthesized. Structure-activity relationship (SAR) of these lipids was studied in detail by investigating the effects of several structural aspects including the type of hydrophobic tails, the chain length and saturation degree. In addition, several assays were used to study their interactions with plasmid DNA, and results reveal that these lipids could condense DNA into nanosized particles with appropriate size and zeta-potentials...
May 16, 2017: Journal of Biological Inorganic Chemistry: JBIC
https://www.readbyqxmd.com/read/28507824/non-invasive-radiofrequency-field-treatment-to-produce-hepatic-hyperthermia-efficacy-and-safety-in-swine
#8
Jason C Ho, Lam Nguyen, Justin J Law, Matthew J Ware, V Keshishian, N C Lara, Trac Nguyen, Steven A Curley, Stuart J Corr
The Kanzius non-invasive radio-frequency hyperthermia system (KNiRFH) has been investigated as a treatment option for hepatic hyperthermia cancer therapy. The treatment involves exposing the patient to an external high-power RF (13.56 MHz) electric field, whereby the propagating waves penetrate deep into the tumor causing targeted heating based on differential tissue dielectric properties. However, a comprehensive examination of the Kanzius system alongside any associated toxicities and its ability to induce hepatic hyperthermia in larger animal models, such as swine, are the subjects of the work herein...
2017: IEEE Journal of Translational Engineering in Health and Medicine
https://www.readbyqxmd.com/read/28506753/phenylbenzenesulfonates-and-sulfonamides-as-17%C3%AE-hydroxysteroid-dehydrogenase-type-2-inhibitors-synthesis-and-sar-analysis
#9
Anna Vuorinen, Roger T Engeli, Susanne Leugger, Christoph R Kreutz, Daniela Schuster, Alex Odermatt, Barbara Matuszczak
17β-Hydroxysteroid dehydrogenase type 2 (17β-HSD2) converts the potent estrogen estradiol into the weakly active keto form estrone. Because of its expression in bone, inhibition of 17β-HSD2 provides an attractive strategy for the treatment of osteoporosis, a condition that is often caused by a decrease of the active sex steroids. Currently, there are no drugs on the market targeting 17β-HSD2, but in multiple studies, synthesis and biological evaluation of promising 17β-HSD2 inhibitors have been reported...
May 4, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28505536/design-synthesis-molecular-docking-and-cytotoxic-evaluation-of-novel-2-furybenzimidazoles-as-vegfr-2-inhibitors
#10
Mona A Abdullaziz, Heba T Abdel-Mohsen, Ahmed M El Kerdawy, Fatma A F Ragab, Mamdouh M Ali, Sherifa M Abu-Bakr, Adel S Girgis, Hoda I El Diwani
Inhibition of angiogenesis through inhibition of vascular endothelial growth factor receptor 2 (VEGFR-2) has been applied in cancer therapy because of its important role in promoting cancer growth and metastasis. In the presented study, a series of benzimidazol-furan hybrids was designed and synthesized through facile synthetic pathways. Evaluation of the synthesized compounds for their in vitro cytotoxic activity against breast (MCF-7) and hepatocellular (HepG2) carcinoma cell lines was performed. Two of the synthesized conjugates, 10b and 15, showed potent antiproliferative properties against MCF-7 cell line (IC50 = 21...
April 26, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28504862/poly-adenine-modulated-dna-conformation-monitored-with-sers-on-multibranched-gold-nanoparticle-and-its-sensing-application
#11
Huangxian Ju, Jingxing Guo, Yunlong Chen, Yongjia Jiang
This work proposes a facile way to modulate the conformation of DNA from "Lie Down" to "Stand Up" on the surface of multibranched gold nanoparticles (AuNS), which is realized by regulating the length of polyA linked to the DNA sequence and/or the hybridization of this sequence with target DNA, and can be monitored with Raman signal owing to the excellent performance of AuNS as SERS substrate and the distance change between Raman reporter and the substrate. The probable mechanism that depends on the repulsion of polyA to the sequence and the tip assembly has been also raised by theoretical simulation with finite difference time domain method...
May 15, 2017: Chemistry: a European Journal
https://www.readbyqxmd.com/read/28501516/is-dual-inhibition-of-metalloenzymes-hdac-8-and-mmp-2-a-potential-pharmacological-target-to-combat-hematological-malignancies
#12
REVIEW
Sk Abdul Amin, Nilanjan Adhikari, Tarun Jha
For the last three decades, metalloenzymes such as histone deacetylases (HDACs) and matrix metalloproteinases (MMPs) have been identified in promoting solid as well as hematological carcinogenesis. Histone deacetylase 8 (HDAC-8), a class I HDAC enzyme, may serve as 'epigenetic player' that affects in the regulation of transcription factors and alters the structure of chromosome associated with tumorigenesis. It is established that the influence of MMP-2 in invasion, metastasis and angiogenenic events of hematological malignancies may be suppressed by HDAC inhibitors through reversion-inducing-cysteine-rich protein with kazal motifs (RECK) protein...
May 10, 2017: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
https://www.readbyqxmd.com/read/28498328/multilook-sar-image-segmentation-with-an-unknown-number-of-clusters-using-a-gamma-mixture-model-and-hierarchical-clustering
#13
Quanhua Zhao, Xiaoli Li, Yu Li
This paper presents a novel multilook SAR image segmentation algorithm with an unknown number of clusters. Firstly, the marginal probability distribution for a given SAR image is defined by a Gamma mixture model (GaMM), in which the number of components corresponds to the number of homogeneous regions needed to segment and the spatial relationship among neighboring pixels is characterized by a Markov Random Field (MRF) defined by the weighting coefficients of components in GaMM. During the algorithm iteration procedure, the number of clusters is gradually reduced by merging two components until they are equal to one...
May 12, 2017: Sensors
https://www.readbyqxmd.com/read/28496375/revisiting-the-etiological-aspects-of-dissociative-identity-disorder-a-biopsychosocial-perspective
#14
REVIEW
Vedat Şar, Martin J Dorahy, Christa Krüger
Dissociative identity disorder (DID) is a chronic post-traumatic disorder where developmentally stressful events in childhood, including abuse, emotional neglect, disturbed attachment, and boundary violations are central and typical etiological factors. Familial, societal, and cultural factors may give rise to the trauma and/or they may influence the expression of DID. Memory and the construction of self-identity are cognitive processes that appear markedly and centrally disrupted in DID and are related to its etiology...
2017: Psychology Research and Behavior Management
https://www.readbyqxmd.com/read/28495610/-allergic-mood-depressive-and-anxiety-symptoms-in-patients-with-seasonal-allergic-rhinitis-sar-and-their-association-to-inflammatory-endocrine-and-allergic-markers
#15
Katharina Trikojat, Hella Luksch, Angela Rösen-Wolff, Franziska Plessow, Jochen Schmitt, Angelika Buske-Kirschbaum
A growing number of studies show an association between seasonal allergic rhinitis (SAR) with depression and anxiety. The underlying mechanisms of a link between SAR and affect, however, are still unclear. The objective of the present study was to investigate depressive symptoms and anxiety in SAR patients and their association to inflammatory and endocrine parameters. SAR patients (n=41) and non-allergic, healthy controls (n=42) were assessed during (pollen season) and out of symptomatic periods (non-pollen season)...
May 8, 2017: Brain, Behavior, and Immunity
https://www.readbyqxmd.com/read/28495556/synthesis-crystal-structure-determination-biological-screening-and-docking-studies-of-n-1-substituted-derivatives-of-2-3-dihydroquinazolin-4-1h-one-as-inhibitors-of-cholinesterases
#16
Nargis Sultana, Muhammad Sarfraz, Saba Tahir Tanoli, Muhammad Safwan Akram, Abdul Sadiq, Umer Rashid, Muhammad Ilyas Tariq
Pursuing the strategy of developing potent AChE inhibitors, we attempted to carry out the N(1)-substitution of 2,3-dihydroquinazolin-4(1H)-one core. A set of 32 N-alkylated/benzylated quinazoline derivatives were synthesized, characterized and evaluated for their inhibition against cholinesterases. N-alkylation of the series of the compounds reported previously (N-unsubstituted) resulted in improved activity. All the compounds showed inhibition of both enzymes in the micromolar to submicromolar range. Structure activity relationship (SAR) of the 32 derivatives showed that N-benzylated compounds possess good activity than N-alkylated compounds...
April 17, 2017: Bioorganic Chemistry
https://www.readbyqxmd.com/read/28495384/medicinal-chemistry-of-antischistosomal-drugs-praziquantel-and-oxamniquine
#17
REVIEW
Vinícius Barros Ribeiro da Silva, Bruna Rafaella Koresch Leiva Campos, Jamerson Ferreira de Oliveira, Jean-Luc Decout, Maria do Carmo Alves de Lima
Neglected tropical diseases (NTDs) are a group of diseases that, besides prevailing in poverty conditions, contribute to the maintenance of social inequality, being a strong barrier to a country development. Schistosomiasis, a NTD, is a tropical and subtropical disease caused by the trematode Schistosoma mansoni (Africa, Middle East, Caribbean, Brazil, Venezuela, Suriname), japonicum (China, Indonesia, the Philippines), mekongi (several districts of Cambodia and the Lao People's Democratic Republic), intercalatum and guianensis (areas of tropical rainforests in Central Africa) and hematobium (Middle East Africa, Corsica, France) whose adult forms inhabit the mesenteric vessels of the host, while the intermediate forms are found in the aquatic gastropod snails of the genus Biomphalaria...
April 27, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28494701/spindle-cell-lipoma-in-dogs
#18
Giancarlo Avallone, Valeria Pellegrino, Luisa V Muscatello, Giuseppe Sarli, Paola Roccabianca
Spindle cell lipoma (SCL) is a benign neoplasm of the adipose tissue that may resemble an undifferentiated soft tissue sarcoma (STS). This report describes the histopathological features of 6 SCLs in dogs. All SCLs were located in the subcutis and were composed of bland, occasionally vacuolated spindle cells intermixed with ropey collagen and myxoid matrix. Sudan IV stain performed in 1 case demonstrated the lipid content of vacuoles. Mature adipocytes represented less than 10% of the neoplasm in 3 cases and were absent in the remaining 3...
January 1, 2017: Veterinary Pathology
https://www.readbyqxmd.com/read/28494252/design-synthesis-and-primary-biological-evaluation-of-the-novel-2-pyridone-derivatives-as-potent-non-nucleoside-hbv-inhibitors
#19
Haiyong Jia, Yang Song, Ji Yu, Peng Zhan, Diwakar Rai, Xiaohong Liang, Chunhong Ma, Xinyong Liu
In continuation of our efforts toward the discovery of potent non-nucleoside hepatitis B virus (HBV) inhibitors with novel structures, we have employed bioisosterism and hybrid pharmacophore-based strategy to explore the chemically diverse space of bioactive compounds. Cytotoxicity, anti-HBV antigen secretion activities and anti-HBV DNA replication activity were assayed with cell counting kit-8 (CCK-8), enzyme linked immunosorbent assay (ELISA) and a real-time PCR, respectively. Some of the new compounds were able to inhibit the replication of HBV DNA activity in the low micromolar range...
April 24, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28486912/structural-investigation-of-vinca-domain-tubulin-binders-by-pharmacophore-atom-based-qsar-docking-and-molecular-dynamics-simulations
#20
Mohd Athar, Mohsin Yousuf Lone, Vijay M Khedkar, Ashish Radadiya, Anamik Shah, Prakash C Jha
Vinca domain of tubulin protein is a potent binding domain for various microtubule targeting drugs (MTD). However, binding mechanism and structure-activity-relationship (SAR) of this domain is not well understood in terms of ligand-receptor interactions and structure functionality requirements. Possibly, this limits the exploitation of this domain for developing novel clinical leads. Therefore, any step towards modelling and comprehension is of central contour. With this objective, we present here an In-silico insight through the development of a robust pharmacophore model and SAR analysis on a set of 26 well known Vinca domain binders of tubulin protein...
May 9, 2017: Combinatorial Chemistry & High Throughput Screening
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