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https://www.readbyqxmd.com/read/28212467/comparison-of-6-mercaptopurine-with-6-thioguanine-for-the-analysis-of-thiopurine-s-methyltransferase-activity-in-human-erythrocyte-by-lc-ms-ms
#1
Shenghui Mei, Xindi Li, Xiaoqing Gong, Xiaoyi Zhang, Xingang Li, Li Yang, Leting Zhu, Heng Zhou, Yonghong Liu, Anna Zhou, Xinghu Zhang, Zhigang Zhao
Thiopurines (TPDs) are first-line drugs in treating neuromyelitis optica spectrum disorders (NMOSD). Thiopurine S-methyltransferase activity (TPMT), a major determinant of TPDs toxicity, was suggested to be evaluated before TPDs treatment by using 6-mercaptopurine (6-MP) and 6-thioguanine (6-TG) as substrate. However, the equivalent of the two substrates in TPMT activity evaluation was unknown, and alternative substrate was required in TPMT activity evaluation in patients who were already taking 6-MP or 6-TG...
February 17, 2017: Biomedical Chromatography: BMC
https://www.readbyqxmd.com/read/28212459/structural-studies-of-nicotinoids-cotinine-vs-nicotine
#2
Iciar Uriarte, Cristóbal Pérez, Elena Caballero-Mancebo, Francisco J Basterretxea, Alberto Lesarri, José A Fernández, Emilio J Cocinero
Nicotinoids are agonists of the acetylcholine receptor (nAChR) and play important biochemical and pharmacological roles. Here we report on the structural and conformational landscape of cotinine, and compare its molecular properties with the nicotine prototype, from which it only differs in the addition of a carbonyl group. The investigation of cotinine included a theoretical survey of the effects of rotamerization of the pyridine moiety, the puckering of the pyrrolidinone ring and the internal rotation of the methyl group...
February 17, 2017: Chemistry: a European Journal
https://www.readbyqxmd.com/read/28212375/epilepsy-associated-gene-nedd4-2-mediates-neuronal-activity-and-seizure-susceptibility-through-ampa-receptors
#3
Jiuhe Zhu, Kwan Young Lee, Kathryn A Jewett, Heng-Ye Man, Hee Jung Chung, Nien-Pei Tsai
The neural precursor cell expressed developmentally down-regulated gene 4-2, Nedd4-2, is an epilepsy-associated gene with at least three missense mutations identified in epileptic patients. Nedd4-2 encodes a ubiquitin E3 ligase that has high affinity toward binding and ubiquitinating membrane proteins. It is currently unknown how Nedd4-2 mediates neuronal circuit activity and how its dysfunction leads to seizures or epilepsies. In this study, we provide evidence to show that Nedd4-2 mediates neuronal activity and seizure susceptibility through ubiquitination of GluA1 subunit of the α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor, (AMPAR)...
February 17, 2017: PLoS Genetics
https://www.readbyqxmd.com/read/28212269/separation-and-characterization-of-angiotensin-i-converting-enzyme-ace-inhibitory-peptides-from-saurida-elongata-proteins-hydrolysate-by-imac-ni-2
#4
Lixia Sun, Shanguang Wu, Liqin Zhou, Feng Wang, Xiongdiao Lan, Jianhua Sun, Zhangfa Tong, Dankui Liao
Lizard fish protein hydrolysates (LFPH) were prepared from Lizard fish (Saurida elongata) proteins possessing powerful angiotensin I converting enzyme (ACE) inhibitory activity and the fraction (LFPH-I) with high ACE inhibitory activity was obtained through ultrafiltration. The active Fraction (F2) was isolated from LFPH-I using immobilized metal affinity chromatography (IMAC-Ni(2+)). Analysis of amino acid levels revealed that F2 eluted from IMAC was enriched in Met, His, Tyr, Pro, Ile, and Leu compared to the crude peptide LFPH-I...
February 15, 2017: Marine Drugs
https://www.readbyqxmd.com/read/28212204/1-2-4-dibromophenyl-3-6-6-trimethyl-1-5-6-7-tetrahydro-4h-indazol-4-one-a-novel-opioid-receptor-agonist-with-less-accompanying-gastrointestinal-dysfunction-than-morphine
#5
Po-Kuan Chao, Shau-Hua Ueng, Li-Chin Ou, Teng-Kuang Yeh, Wan-Ting Chang, Hsiao-Fu Chang, Shu-Chun Chen, Pao-Luh Tao, Ping-Yee Law, Horace H Loh, Ming-Fu Cheng, Jian-Ying Chuang, Chiung-Tong Chen, Chuan Shih, Shiu-Hwa Yeh
BACKGROUND: The authors investigated the pharmacology and signaling pathways of the opioid receptors modulated by compound 1, 1-(2,4-dibromophenyl)-3,6,6-trimethyl-1,5,6,7-tetrahydro-4H-indazol-4-one. METHODS: In vitro studies of compound 1 were assessed by using a radioligand-binding assay (n = 3), a cyclic adenosine monophosphate assay (n = 3), a β-arrestin assay (n = 3), an internalization assay (n = 3), and an immunohistochemistry (n = 8). In vivo studies of compound 1 were characterized using a tail-flick test (n = 5 to 6), tail-clip test (n = 7), von Frey hair test (n = 5), and charcoal meal test (n = 5)...
February 17, 2017: Anesthesiology
https://www.readbyqxmd.com/read/28212072/neural-network-based-solutions-for-stochastic-optimal-control-using-path-integrals
#6
Karthikeyan Rajagopal, Sivasubramanya Nadar Balakrishnan, Jerome R Busemeyer
In this paper, an offline approximate dynamic programming approach using neural networks is proposed for solving a class of finite horizon stochastic optimal control problems. There are two approaches available in the literature, one based on stochastic maximum principle (SMP) formalism and the other based on solving the stochastic Hamilton-Jacobi-Bellman (HJB) equation. However, in the presence of noise, the SMP formalism becomes complex and results in having to solve a couple of backward stochastic differential equations...
March 2017: IEEE Transactions on Neural Networks and Learning Systems
https://www.readbyqxmd.com/read/28212021/discovery-and-development-of-1-2-bromophenyl-sulfonyl-5-methoxy-3-4-methyl-1-piperazinyl-methyl-1h-indole-dimesylate-monohydrate-suvn-502-a-novel-potent-selective-and-orally-active-serotonin-6-5-ht6-receptor-antagonist-for-potential-treatment-of-alzheimer-s
#7
Ramakrishna Nirogi, Anil Shinde, Rama Sastry Kambhampati, Abdul Rasheed Mohammed, Sangram Keshari Saraf, Rajesh Kumar Badange, Thrinath Reddy Bandyala, Venugopalarao Bhatta, Kumar Bojja, Veena Reballi, Ramkumar Subramanian, Vijay Benade, Raghava Choudary Palacharla, Gopinadh Bhyrapuneni, Pradeep Jayarajan, Vinod Goyal, Venkat Jasti
Optimization of a novel series of 3-(piperazinylmethyl) indole derivatives as 5-hydroxytryptamine-6 receptor (5-HT6R) antagonists resulted in identification of 1-[(2-bromophenyl)sulfonyl]-5-methoxy-3-[(4-methyl-1-piperazinyl)methyl]-1H-indole dimesylate monohydrate (5al, SUVN-502) as a clinical candidate for potential treatment of cognitive disorders. It has high affinity at human 5-HT6R (Ki = 2.04 nM) and selectivity over 100 target sites which include receptors, enzymes, peptides, growth factors, ion channels, steroids, immunological factors, second messengers, and prostaglandins...
February 17, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28211930/stable-amphiphilic-supramolecular-self-assembly-based-on-cyclodextrin-and-carborane-for-the-efficient-photodynamic-therapy
#8
Hejian Xiong, Dongfang Zhou, Xiaohua Zheng, Yanxin Qi, Yongheng Wang, Xiabin Jing, Yubin Huang
Novel and stable supramolecular nanoparticles (NP) were prepared based on the high affinity of carboranes to β-cyclodextrin for the efficient photodynamic therapy of porphyrin in vitro.
February 17, 2017: Chemical Communications: Chem Comm
https://www.readbyqxmd.com/read/28211669/3-aminomethyl-derivatives-of-2-phenylimidazo-1-2-a-pyridine-as-positive-allosteric-modulators-of-gabaa-receptor-with-potential-antipsychotic-activity
#9
Monika Marcinkowska, Marcin Kolaczkowski, Krzysztof Kamiński, Adam Bucki, Maciej Henryk Pawlowski, Agata Siwek, Tadeusz Karcz, Gabriela Starowicz, Karolina Sloczynska, Elżbieta Pękala, Anna Wesołowska, Jerzy Samochowiec, Paweł Mierzejewski, Przemyslaw Bienkowski
Schizophrenia is a mental illness characterized by behavioral changes as well as anatomical and neurochemical abnormalities. There has been a remarkable progress in the drug discovery for schizophrenia; however, antipsychotics that act through molecular targets, other than monoaminergic receptors, have not been developed. One of the hypotheses of schizophrenia states that GABAergic dysfunction might be implemented in the pathophysiology of this disease. Our recent findings and previous clinical observations have suggested that modulation of GABAergic system through α1-GABAA receptors would represent an original approach for the treatment of schizophrenia...
February 17, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28211613/novel-anticarcinoembryonic-antigen-antibody-drug-conjugate-has-antitumor-activity-in-the-existence-of-soluble-antigen
#10
Daisuke Shinmi, Ryosuke Nakano, Keisuke Mitamura, Minami Suzuki-Imaizumi, Junko Iwano, Yuya Isoda, Junichi Enokizono, Yasuhisa Shiraishi, Emi Arakawa, Kazuma Tomizuka, Kazuhiro Masuda
Carcinoembryonic antigen (CEA) is a classic tumor-specific antigen that is overexpressed in several cancers, including gastric cancer. Although some anti-CEA antibodies have been tested, to the best of our knowledge, there are currently no clinically approved anti-CEA antibody therapies. Because of this, we have created the novel anti-CEA antibody, 15-1-32, which exhibits stronger binding to membrane-bound CEA on cancer cells than existing anti-CEA antibodies. 15-1-32 also shows poor affinity for soluble CEA; thus, the binding activity of 15-1-32 to membrane-bound CEA is not influenced by soluble CEA...
February 17, 2017: Cancer Medicine
https://www.readbyqxmd.com/read/28211542/identification-of-the-core-regulators-of-the-hla-i-peptide-binding-process
#11
Yu-Hang Zhang, Zhihao Xing, Chenglin Liu, ShaoPeng Wang, Tao Huang, Yu-Dong Cai, Xiangyin Kong
During the display of peptide/human leukocyte antigen (HLA) -I complex for further immune recognition, the cleaved and transported antigenic peptides have to bind to HLA-I protein and the binding affinity between peptide epitopes and HLA proteins directly influences the immune recognition ability in human beings. Key factors affecting the binding affinity during the generation, selection and presentation processes of HLA-I complex have not yet been fully discovered. In this study, a new method describing the HLA class I-peptide interactions was proposed...
February 17, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28211541/antibody-controlled-actuation-of-dna-based-molecular-circuits
#12
Wouter Engelen, Lenny H H Meijer, Bram Somers, Tom F A de Greef, Maarten Merkx
DNA-based molecular circuits allow autonomous signal processing, but their actuation has relied mostly on RNA/DNA-based inputs, limiting their application in synthetic biology, biomedicine and molecular diagnostics. Here we introduce a generic method to translate the presence of an antibody into a unique DNA strand, enabling the use of antibodies as specific inputs for DNA-based molecular computing. Our approach, antibody-templated strand exchange (ATSE), uses the characteristic bivalent architecture of antibodies to promote DNA-strand exchange reactions both thermodynamically and kinetically...
February 17, 2017: Nature Communications
https://www.readbyqxmd.com/read/28211525/focus-on-pna-flexibility-and-rna-binding-using-molecular-dynamics-and-metadynamics
#13
Massimiliano Donato Verona, Vincenzo Verdolino, Ferruccio Palazzesi, Roberto Corradini
Peptide Nucleic Acids (PNAs) can efficiently target DNA or RNA acting as chemical tools for gene regulation. Their backbone modification and functionalization is often used to increase the affinity for a particular sequence improving selectivity. The understanding of the trading forces that lead the single strand PNA to bind the DNA or RNA sequence is preparatory for any further rational design, but a clear and unique description of this process is still not complete. In this paper we report further insights into this subject, by a computational investigation aiming at the characterization of the conformations of a single strand PNA and how these can be correlated to its capability in binding DNA/RNA...
February 17, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28211013/electrostatic-forces-as-dominant-interactions-between-proteins-and-polyanions-an-esi-ms-study-of-fibroblast-growth-factor-binding-to-heparin-oligomers
#14
Burcu Baykal Minsky, Paul L Dubin, Igor A Kaltashov
The interactions between fibroblast growth factors (FGFs) and their receptors (FGFRs) are facilitated by heparan sulfate (HS) and heparin (Hp), highly sulfated biological polyelectrolytes. The molecular basis of FGF interactions with these polyelectrolytes is highly complex due to the structural heterogeneity of HS/Hp, and many details still remain elusive, especially the significance of charge density and minimal chain length of HS/Hp in growth factor recognition and multimerization. In this work, we use electrospray ionization mass spectrometry (ESI MS) to investigate the association of relatively homogeneous oligoheparins (octamer, dp8, and decamer, dp10) with acidic fibroblast growth factor (FGF-1)...
February 16, 2017: Journal of the American Society for Mass Spectrometry
https://www.readbyqxmd.com/read/28211007/daclizumab-a-review-in-relapsing-multiple-sclerosis
#15
Matt Shirley
Daclizumab (Zinbryta(®); previously known as daclizumab high-yield process) is a therapeutic monoclonal antibody that has recently been approved for the treatment of relapsing forms of multiple sclerosis (MS) in adults. Daclizumab is a humanized IgG1 monoclonal antibody directed against CD25, the alpha subunit of the high-affinity interleukin-2 receptor. As demonstrated in the phase III DECIDE trial, once-monthly subcutaneous daclizumab was superior to once-weekly intramuscular interferon (IFN) β-1a in reducing the clinical relapse rate and radiological measures of disease in patients with relapsing-remitting MS...
February 17, 2017: Drugs
https://www.readbyqxmd.com/read/28210988/real-life-experience-with-the-specific-reversal-agent-idarucizumab-for-the-management-of-emergency-situations-in-dabigatran-treated-patients-a-series-of-11-cases
#16
Milan R Vosko, Christof Bocksrucker, Rafał Drwiła, Petr Dulíček, Tomas Hauer, Johannes Mutzenbach, Christoph J Schlimp, David Špinler, Thomas Wolf, Daša Zugwitz
Non-vitamin K antagonist oral anticoagulants (NOACs) have a favorable benefit-risk profile compared with vitamin K antagonists. However, the lack of specific reversal agents has made the management of some patients receiving long-term treatment with NOACs problematic in emergency situations such as major bleeding events or urgent procedures. Idarucizumab, a fully humanized Fab antibody fragment that binds specifically and with high affinity to dabigatran, was recently approved for use in adult patients treated with dabigatran when rapid reversal of its anticoagulant effect is required...
February 16, 2017: Journal of Thrombosis and Thrombolysis
https://www.readbyqxmd.com/read/28210729/self-assembly-of-cucurbit-7-uril-based-triangular-4-molecular-necklaces-and-their-fluorescence-properties
#17
Soumen K Samanta, Kimberly G Brady, Lyle Isaacs
Self-assembly of rigid-rod dipyridine ligand 1 with M(en)(NO3)2 (M = Pd, Pt) affords triangular (3, 5) and square (4, 6) supramolecular coordination complexes (SCCs). The binding affinity of 1 toward CB[n]-type containers results in the formation of triangular [4]molecular necklaces ([4]MNs, 7-10) by either one-pot or post complexation approaches as evidenced by (1)H NMR, diffusion ordered spectroscopy, and ESI-MS.
February 17, 2017: Chemical Communications: Chem Comm
https://www.readbyqxmd.com/read/28210726/exploring-the-interaction-of-phenothiazinium-dyes-methylene-blue-new-methylene-blue-azure-a-and-azure-b-with-trna-phe-spectroscopic-thermodynamic-voltammetric-and-molecular-modeling-approach
#18
Puja Paul, Soumya Sundar Mati, Subhash Chandra Bhattacharya, Gopinatha Suresh Kumar
This study focuses on the understanding of the interaction of phenothiazinium dyes methylene blue (MB), new methylene blue (NMB), azure A (AZA) and azure B (AZB) with tRNA(Phe) with particular emphasis on deciphering the mode and energetics of the binding. Strong intercalative binding to tRNA(Phe) was observed for MB, NMB and AZB, bound by a partial intercalative mode. AZA has shown groove binding characteristics. From spectroscopic studies binding affinity values of the order of 10(5) M(-1) were deduced for these dyes; the trend varied as MB > NMB > AZB > AZA...
February 17, 2017: Physical Chemistry Chemical Physics: PCCP
https://www.readbyqxmd.com/read/28210565/label-free-proteome-analysis-of-plasma-from-patients-with-breast-cancer-stage-specific-protein-expression
#19
Marina Duarte Pinto Lobo, Frederico Bruno Mendes Batista Moreno, Gustavo Henrique Martins Ferreira Souza, Sara Maria Moreira Lima Verde, Renato de Azevedo Moreira, Ana Cristina de Oliveira Monteiro-Moreira
Breast cancer is one of the most commonly diagnosed types of cancer among women. Breast cancer mortality rates remain high probably because its diagnosis is hampered by inaccurate detection methods. Since changes in protein expression as well as modifications in protein glycosylation have been frequently reported in cancer development, the aim of this work was to study the differential expression as well as modifications of glycosylation of proteins from plasma of women with breast cancer at different stages of disease (n = 30) compared to healthy women (n = 10)...
2017: Frontiers in Oncology
https://www.readbyqxmd.com/read/28210398/injection-adipolysis-mechanisms-agents-and-future-directions
#20
REVIEW
Shahraam Kamalpour, Keith Leblanc
Noninvasive procedures targeting the elimination of unwanted adipose tissues have recently been developed. injection adipolysis is the term for the injection of cytotoxic substances into these tissues, with the intent of cosmetic improvement by volume reduction. initial attempts in the field utilized intravenous preparations of sodium deoxycholate and soy-derived phosphatidylcholine, approved for the intravenous treatment of fat emboli and dyslipidemias in countries outside the United States. it was initially purported that the active ingredient in these injections was phosphatidylcholine...
December 2016: Journal of Clinical and Aesthetic Dermatology
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