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https://www.readbyqxmd.com/read/28551908/-involvement-of-epigenetic-regulation-in-cerebral-cell-death-following-traumatic-brain-injury-in-a-rat-model
#1
Mona Shehadeh, Moti Ben-Shabat, Jana Livshits, Eilam Palzur
INTRODUCTION: Traumatic brain injuries (TBI) are a major cause of mortality and disability among young adults. TBI are characterized by primary injury, the result of a mechanical impact to the cranium and a secondary injury, a series of molecular mechanism processes developing thereafter. Cerebral cells modify their gene and protein expression as a result of the injury. Epigenetic modifications have a key role as regulators of gene transcription and may simultaneously be involved in the regulation of the molecular pathways following TBI...
May 2017: Harefuah
https://www.readbyqxmd.com/read/28551817/discovery-of-novel-inhibitors-for-leishmania-nucleoside-diphosphatase-kinase-ndk-based-on-its-structural-and-functional-characterization
#2
Arjun K Mishra, Nidhi Singh, Pragati Agnihotri, Shikha Mishra, Saurabh P Singh, Bala K Kolli, Kwang Poo Chang, Amogh A Sahasrabuddhe, M I Siddiqi, J Venkatesh Pratap
Nucleoside diphosphate kinases (NDKs) are ubiquitous enzymes that catalyze the transfer of the γ-phosphate moiety from an NTP donor to an NDP acceptor, crucial for maintaining the cellular level of nucleoside triphosphates (NTPs). The inability of trypanosomatids to synthesize purines de novo and their dependence on the salvage pathway makes NDK an attractive target to develop drugs for the diseases they cause. Here we report the discovery of novel inhibitors for Leishmania NDK based on the structural and functional characterization of purified recombinant NDK from Leishmania amazonensis...
May 27, 2017: Journal of Computer-aided Molecular Design
https://www.readbyqxmd.com/read/28551676/hodgkin-lymphoma-transformation-of-chronic-lymphocytic-leukemia-under-ibrutinib-therapy-chance-association-or-therapy-related
#3
Sotirios Sachanas, Gerassimos A Pangalis, Maria Moschogiannis, Xanthi Yiakoumis, Efstathios Koulieris, Pantelis Tsirkinidis, Christina Kalpadakis, Dimitra Rontogianni
The established treatment algorithms for chronic lymphocytic leukemia (CLL)/small lymphocytic lymphoma (SLL) are currently challenged by novel classes of drugs, with ibrutinib being one of the most effective. Published data suggest that patients with early progression under ibrutinib often emerge as having Richter's transformation (RT) with a rapidly fatal prognosis, mostly developing diffuse large B-cell lymphoma (DLBCL). In this respect, it is known that RT to large DLBCL occurs in about 5% of patients with CLL during the disease course and less frequently to Hodgkin lymphoma (HL)...
June 2017: Anticancer Research
https://www.readbyqxmd.com/read/28551612/pancreatic-cancer-stem-cells-and-therapeutic-approaches
#4
REVIEW
Gulinnaz Ercan, Ayfer Karlitepe, Bulent Ozpolat
Pancreatic ductal adenocarcinoma (PDAC) is considered one of the deadliest human cancers, with 1-5% 5-year survival rates (~6-month median survival duration) despite therapy; thus, PDAC represents an unmet therapeutic challenge. PDAC is the major histological subtype, comprising 90% of all pancreatic cancers. It is a highly complex and aggressive malignancy, presenting with early local invasion and metastasis, and is resistant to most therapies, all of which are believed to contribute to its extremely poor prognosis...
June 2017: Anticancer Research
https://www.readbyqxmd.com/read/28551587/efficient-click-chemistry-towards-fatty-acids-containing-1-2-3-triazole-design-and-synthesis-as-potential-antifungal-drugs-for-candida-albicans
#5
Nina Fu, Suiliang Wang, Yuqian Zhang, Caixia Zhang, Dongliang Yang, Lixing Weng, Baomin Zhao, Lianhui Wang
Candida is an important opportunistic human fungal pathogen. The cis-2-dodecenoic acid (BDSF) showing in vitro activity of against C. albicans growth, germ-tube germination and biofilm formation has been a potential inhibitor for Candida and other fungi. In this study, facile synthetic strategies toward a novel family of BDSF analogue, 1-alkyl-1H-1,2,3-triazole-4-carboxylic acids (ATCs) was developed. The straightforward synthetic method including converting the commercial available alkyl bromide to alkyl azide, consequently with a typical click chemistry method, copper(II) sulfate and sodium ascorbate as catalyst in water to furnish ATCs with mild to good yields...
May 2, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28551549/preparation-of-a-chlorophyll-derivative-and-investigation-of-its-photodynamic-activities-against-cholangiocarcinoma
#6
Zhong-Ming Wu, Li Wang, Wei Zhu, Ying-Hua Gao, Hai-Ming Wu, Mi Wang, Tai-Shan Hu, Yi-Jia Yan, Zhi-Long Chen
Photodynamic therapy (PDT) is emerging as a promising method for the treatment of various cancer diseases. However, the clinical application of PDT is limited due to the lack of effective photosensitizers. In this study, a novel chlorophyll derivative, N,N-bis(2-carboxyethyl)pyropheophorbide a (BPPA), had been synthesized and characterized. BPPA had a characteristic long wavelength absorption peak at 669nm and a singlet oxygen quantum yield of 0.54. To investigate the photodynamic ability of BPPA against cholangiocarcinoma (CCA), cellular uptake, subcellular location and bio-distribution, in vitro and in vivo PDT efficacy of BPPA were studied...
May 24, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28551545/cytotoxicity-of-temozolomide-on-human-glioblastoma-cells-is-enhanced-by-the-concomitant-exposure-to-an-extremely-low-frequency-electromagnetic-field-100hz-100g
#7
Zeinab Akbarnejad, Hossein Eskandary, Luciana Dini, Cristian Vergallo, Seyed Noureddin Nematollahi-Mahani, Alireza Farsinejad, Maryam Fekri Soofi Abadi, Meysam Ahmadi
Glioblastoma multiforme (GBM) is the most malignant brain cancer that causes high mortality in humans. It responds poorly to the most common cancer treatments, such as surgery, chemo- and radiation therapy. Temozolomide (TMZ) is an alkylating agent that has been widely used to treat GBM; resistance to this drug is often found. One unexplored possibility for overcoming this resistance is a treatment based on concomitant exposure to electromagnetic fields (EMF) and TMZ. Indeed, many evidences show that EMF affects cancer cells and drug performance...
May 24, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28551413/applying-the-chicken-embryo-chorioallantoic-membrane-assay-to-study-treatment-approaches-in-urothelial-carcinoma
#8
Margaretha A Skowron, Anuja Sathe, Andrea Romano, Michèle J Hoffmann, Wolfgang A Schulz, Gommert A van Koeveringe, Peter Albers, Roman Nawroth, Günter Niegisch
BACKGROUND: Rapid development of novel treatment options demands valid preclinical screening models for urothelial carcinoma (UC). The translational value of high-throughput drug testing using 2-dimensional (2D) cultures is limited while for xenograft models handling efforts and costs often become prohibitive for larger-scale drug testing. Therefore, we investigated to which extent the chicken chorioallantoic membrane (CAM) assay might provide an alternative model to study antineoplastic treatment approaches for UC...
May 25, 2017: Urologic Oncology
https://www.readbyqxmd.com/read/28551190/clinical-trial-of-local-anesthetic-protocols-for-acute-pain-associated-with-caustic-paste-disbudding-in-dairy-calves
#9
Charlotte B Winder, Stephen J LeBlanc, Derek B Haley, Kerry D Lissemore, M Ann Godkin, Todd F Duffield
Caustic paste disbudding is becoming more commonplace in North America. A large body of work has examined pain control for cautery disbudding and surgical dehorning, but fewer studies have evaluated pain control for caustic paste disbudding, and results conflict regarding benefits of local anesthesia. In humans, the pain associated with a caustic, chemical burn can differ in nature, duration, and intensity compared with a thermal burn. The objective of this clinical trial was to evaluate the effects of either a lidocaine cornual nerve block or a topical anesthetic incorporated into caustic paste on the acute pain of caustic paste disbudding...
May 24, 2017: Journal of Dairy Science
https://www.readbyqxmd.com/read/28551118/synthesis-of-hydrazide-functionalized-hydrophilic-polymer-hybrid-graphene-oxide-for-highly-efficient-n-glycopeptide-enrichment-and-identification-by-mass-spectrometry
#10
Haihong Bai, Yiting Pan, Cong Guo, Xinyuan Zhao, Bingquan Shen, Xinghe Wang, Zeyuan Liu, Yuanguo Cheng, Weijie Qin, Xiaohong Qian
Protein N-glycosylation is one of the most important post-translational modifications, participating in many key biological and pathological processes. Large-scale and precise identification of N-glycosylated proteins and peptides is especially beneficial for understanding their biological functions and for discovery of new clinical biomarkers and therapeutic drug targets. However, protein N-glycosylation is microheterogeneous and low abundant in living organisms, therefore specific enrichment of N-glycosylated proteins/peptides before mass spectrometry analysis is a prerequisite...
August 15, 2017: Talanta
https://www.readbyqxmd.com/read/28550603/development-of-novel-high-density-gastroretentive-multiparticulate-pulsatile-tablet-of-clopidogrel-bisulfate-using-quality-by-design-approach
#11
Nilesh Desai, Ravindra Purohit
Myocardial infarction, i.e., heart attack, is a fatal condition which is on the increase all over the world. It is reported that a large number of heart attack occur in morning hours which are attributable to platelet aggregation. Chronotherapy at this stage can be crucial. Clopidogrel bisulfate (CLB) is an antiplatelet agent and has become a drug of choice for prevention of heart attack. It is soluble in acidic pH and has a narrow absorption window. So, its long residence time in stomach is desirable. Therefore, a novel high density tablet was developed comprising multiparticulate pellets with pulsatile release necessary to maintain chronotherapy of heart attack...
May 26, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28550455/-effects-of-the-novel-relatively-short-acting-kappa-opioid-receptor-antagonist-ly2444296-in-behaviors-observed-after-chronic-extended-access-cocaine-self-administration-in-rats
#12
Marta Valenza, Eduardo R Butelman, Mary Jeanne Kreek
RATIONALE: The recruitment of the stress circuitry contributes to a shift from positive to negative reinforcement mechanisms sustaining long-term cocaine addiction. The kappa opioid receptor (KOPr) signaling is upregulated by stress and chronic cocaine exposure. While KOPr agonists induce anhedonia and dysphoria, KOPr antagonists display antidepressant and anxiolytic properties. Most of the knowledge on KOPr antagonism is based on drugs with unusual pharmacokinetic and pharmacodynamic properties, complicating interpretation of results...
May 27, 2017: Psychopharmacology
https://www.readbyqxmd.com/read/28550450/abcc4-functional-snp-in-the-3-splice-acceptor-site-of-exon-8-g912t-is-associated-with-unfavorable-clinical-outcome-in-children-with-acute-lymphoblastic-leukemia
#13
Hamzeh Mesrian Tanha, Soheila Rahgozar, Marjan Mojtabavi Naeini
OBJECTIVES: ATP-binding cassette subfamily C member 4 (ABCC4) encoding MRP4 protein is involved in pediatric acute lymphoblastic leukemia (ALL) drug resistance. The nonsynonymous single nucleotide polymorphism (SNP) rs2274407 (G912T; K304N) is located in the 3' splice acceptor site of exon 8 of ABCC4 pre-mRNA. The aim of this study was to investigate the prognostic value of rs2274407 in childhood ALL and its possible functional effect on MRP4. METHODS: ABCC4 G912T SNP was genotyped in 145 Iranian Philadelphia-negative (Ph(-)) children with ALL using modified tetra-primer ARMS PCR and evaluated for possible association with 3-year disease-free survival (3DFS)...
May 26, 2017: Cancer Chemotherapy and Pharmacology
https://www.readbyqxmd.com/read/28550447/trends-in-surgical-research-in-head-and-neck-cancer
#14
REVIEW
Genrich Tolstonog, Christian Simon
The task of surgical research is to improve the efficacy of available surgical therapeutic modalities, develop new ones, and balance this well with favorable functional outcome. Therefore, surgical research is composed of a translational and a clinical component. In translational surgical research, animal models are used to better understand the biology of head and neck cancers, but even more importantly, the biology of changes to the disease and the microenvironment created by surgical interventions. Animal models additionally allow for the development of image-guided surgery systems, novel strategies of intraoperative adjuvant treatment, and patient "avatars" to test innovative anticancer drug combinations...
June 2017: Current Treatment Options in Oncology
https://www.readbyqxmd.com/read/28550249/avn-492-a-novel-highly-selective-5-ht6r-antagonist-preclinical-evaluation
#15
Alexandre V Ivachtchenko, Ilya Okun, Vladimir Aladinskiy, Yan Ivanenkov, Angela Koryakova, Ruben Karapetyan, Oleg Mitkin, Ramiz Salimov, Andrey Ivashchenko
Discovery of 5-HT6 receptor subtype and its exclusive localization within the central nervous system led to extensive investigations of its role in Alzheimer's disease, schizophrenia, and obesity. In the present study, we present preclinical evaluation of a novel highly-potent and highly-selective 5-HT6R antagonist, AVN-492. The affinity of AVN-492 to bind to 5-HT6R (Ki = 91 pM) was more than three orders of magnitude higher than that to bind to the only other target, 5-HT2BR, (Ki = 170 nM). Thus, the compound displayed great 5-HT6R selectivity against all other serotonin receptor subtypes, and is extremely specific against any other receptors such as adrenergic, GABAergic, dopaminergic, histaminergic, etc...
May 25, 2017: Journal of Alzheimer's Disease: JAD
https://www.readbyqxmd.com/read/28549949/recent-advancements-in-liposomes-targeting-strategies-to-cross-blood-brain-barrier-bbb-for-the-treatment-of-alzheimer-s-disease
#16
REVIEW
Mukta Agrawal, Ajazuddin, Dulal K Tripathi, Swarnlata Saraf, Shailendra Saraf, Sophia G Antimisiaris, Spyridon Mourtas, Margareta Hammarlund-Udenaes, Amit Alexander
In this modern era, with the help of various advanced technologies, medical science has overcome most of the health-related issues successfully. Though, some diseases still remain unresolved due to various physiological barriers. One such condition is Alzheimer; a neurodegenerative disorder characterized by progressive memory impairment, behavioral abnormalities, mood swing and disturbed routine activities of the person suffering from. It is well known to all that the brain is entirely covered by a protective layer commonly known as blood brain barrier (BBB) which is responsible to maintain the homeostasis of brain by restricting the entry of toxic substances, drug molecules, various proteins and peptides, small hydrophilic molecules, large lipophilic substances and so many other peripheral components to protect the brain from any harmful stimuli...
May 23, 2017: Journal of Controlled Release: Official Journal of the Controlled Release Society
https://www.readbyqxmd.com/read/28549898/brainstem-mechanisms-underlying-the-cough-reflex-and-its-regulation
#17
REVIEW
Donatella Mutolo
Cough is a very important airway protective reflex. Cough-related inputs are conveyed to the caudal nucleus tractus solitarii (cNTS) that projects to the brainstem respiratory network. The latter is reconfigured to generate the cough motor pattern. A high degree of modulation is exerted on second-order neurons and the brainstem respiratory network by sensory inputs and higher brain areas. Two medullary structures proved to have key functions in cough production and to be strategic sites of action for centrally active drugs: the cNTS and the caudal ventral respiratory group (cVRG)...
May 23, 2017: Respiratory Physiology & Neurobiology
https://www.readbyqxmd.com/read/28549889/synthesis-and-evaluation-of-novel-dual-brd4-hdac-inhibitors
#18
Seika Amemiya, Takao Yamaguchi, Yuichi Hashimoto, Tomomi Noguchi-Yachide
Epigenetic regulation of gene expression via histone acetylation modulates many cellular processes, including apoptosis, the cell cycle, cell growth and differentiation, and inhibitors are promising drug candidates. We have previously developed inhibitors of BRD4, which recognizes acetylated lysine residue on histones and recruits transcription elongation factor to the transcription start site, while inhibitors of histone deacetylase (HDAC), which catalyzes the removal of acetyl groups on histones, are already in clinical use for cancer treatment...
May 17, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28549802/design-synthesis-and-biological-evaluation-of-novel-androst-3-5-diene-3-carboxylic-acid-derivatives-as-inhibitors-of-5%C3%AE-reductase-type-1-and-2
#19
Kejing Lao, Jie Sun, Chong Wang, Weiting Lyu, Boshen Zhou, Ruheng Zhao, Qian Xu, Qidong You, Hua Xiang
5α-Reductase is a key enzyme responsible for dihydrotestosterone biosynthesis and has been recognized as an important target for discovering new drugs against benign prostatic hyperplasia (BPH). In this study, a series of novel steroidal androst-3,5-diene-3-carboxylic acids have been designed and synthesized. Biological evaluations were performed on their 5α-reductase inhibitory activities by both in vitro enzyme inhibition assay and in vivo by prostate weighing method. Results showed that most of them displayed excellent 5α-reductase inhibitory potency...
May 23, 2017: Steroids
https://www.readbyqxmd.com/read/28549799/a-randomized-controlled-trial-of-the-impact-of-pharmacist-led-patient-centered-pharmaceutical-care-on-patients-medicine-therapy-related-quality-of-life
#20
Phantipa Sakthong, Todsaporn Sangthonganotai
BACKGROUND: Due to a lack of pharmaceutical care (PC)-specific measures for health-related quality of life, a novel generic questionnaire "Patient-Reported Outcomes Measure of Pharmaceutical Therapy for Quality of Life (PROMPT-QoL) was developed. Little was also known about an impact of pharmaceutical care on medicine therapy-related quality of life. OBJECTIVE: First, evaluate the impact of PC on medicine therapy-related QoL using the PROMPT-QoL in Thai patients...
May 11, 2017: Research in Social & Administrative Pharmacy: RSAP
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