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https://www.readbyqxmd.com/read/29333899/social-support-and-mental-health-in-lgbtq-adolescents-a-review-of-the-literature
#1
Kari McDonald
LGBTQ adolescents experience higher rates of mental health disorders than their heterosexual peers. The purpose of this systematic review of the literature was to examine studies evaluating social support and its effects on mental health in the LGBTQ adolescent population. Higher levels of social support were associated with positive self-esteem. Lack of social support (or low social support) was associated with higher levels of depression, anxiety, alcohol or drug misuse, risky sexual behaviors, shame, and low self-esteem...
January 15, 2018: Issues in Mental Health Nursing
https://www.readbyqxmd.com/read/29332949/convergent-synthesis-of-%C3%AE-branched-amines-by-transition-metal-catalyzed-c-h-bond-additions-to-imines
#2
Joshua R Hummel, Jonathan A Ellman
α-Branched amines are ubiquitous in drugs and natural products, and consequently, synthetic methods that provide convergent and efficient entry to these structures are of considerable value. Transition-metal-catalyzed C-H bond additions to imines have the potential to be highly practical and atom-economic approaches for the synthesis of a diverse and complex array of α-branched amine products. These strategies typically employ readily available starting inputs, display high functional group compatibility, and often avoid the production of stoichiometric waste byproducts...
November 2017: Israel Journal of Chemistry
https://www.readbyqxmd.com/read/29332599/the-synthesis-of-chalcones-as-anticancer-prodrugs-and-their-bioactivation-in-cyp1-expressing-breast-cancer-cells
#3
Ketan Ruparelia, Keti Zeka, Randolph R Arroo, Kenneth J M Beresford
BACKGROUND: Although the expression levels of many P450s differ between tumour and corresponding normal tissue, CYP1B1 is one of the few CYP subfamilies which is significantly and consistently overexpressed in tumours. CYP1B1 has been shown to be active within tumours and is capable of metabolising a structurally diverse range of anticancer drugs. Because of this, and its role in the activation of procarcinogens, CYP1B1 is seen as an important target for anticancer drug development. OBJECTIVES: To synthesise a series of chalcone derivatives based on the chemopreventative agent DMU-135 and investigate their antiproliferative activities in human breast cancer cell lines which express CYP1B1 and CYP1A1...
January 12, 2018: Medicinal Chemistry
https://www.readbyqxmd.com/read/29332563/multi-target-directed-drugs-as-a-modern-approach-for-drug-design-towards-alzheimer-s-disease-an-update
#4
Matheus de Freitas Silva, Kris Simone Tranches Dias, Vanessa Silva Gontijo, Cindy Juliet Cristancho Ortiz, Claudio Viega
Alzheimer's disease (AD) is a progressive multifactorial neurodegenerative disorder. Currently, no effective treatment is available and this is due to multiple factors involved in pathophysiology and severity of AD. A recent approach for the rational design of new drug candidates, also called multitarget-directed ligands (MTDL) strategy, has been used to develop a variety of hybrid compounds capable to act simultaneously in diverse biological targets. The discovery of drug molecules capable of targeting multiple factors involved in AD pathogenesis would greatly facilitate in improving therapeutic strategies...
January 10, 2018: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/29331790/c-phycocyanin-cellular-targets-mechanisms-of-action-and-multi-drug-resistance-in-cancer
#5
REVIEW
Estela Fernandes E Silva, Felipe da Silva Figueira, Aline Portantiolo Lettnin, Michele Carrett-Dias, Daza de Moraes Vaz Batista Filgueira, Susana Kalil, Gilma Santos Trindade, Ana Paula de Souza Votto
C-Phycocyanin (C-PC) has been shown to be promising in cancer treatment; however, although several articles detailing this have been published, its main mechanisms of action and its cellular targets have not yet been defined, nor has a detailed exploration been conducted of its role in the resistance of cancer cells to chemotherapy, rendering clinical use impossible. From our extensive examination of the literature, we have determined as our main hypothesis that C-PC has no one specific target, but rather acts on the membrane, cytoplasm, and nucleus with diverse mechanisms of action...
July 26, 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/29331315/ethnobotany-phytochemistry-and-pharmacology-of-arctotis-arctotoides-l-f-o-hoffm-a-review
#6
REVIEW
Md Moshfekus Saleh-E-In, Johannes Van Staden
ETHNOPHARMACOLOGICAL RELEVANCE: Arctotis arctotoides (Asteraceae) is part of the genus Arctotis. Arctotis is an African genus of approximately 70 species that occur widely in the African continent with diverse medicinal values. This plant is used for the treatment of indigestion and catarrh of the stomach, epilepsy, topical wounds and skin disorders among the ethnic groups in South Africa and reported to have a wide spectrum of pharmacological properties. AIM OF THE REVIEW: The aim of the present review is to appraise the botany, traditional uses, phytochemistry, pharmacological potential, analytical methods and safety issues of A...
January 10, 2018: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/29330466/target-engagement-imaging-of-parp-inhibitors-in-small-cell-lung-cancer
#7
Brandon Carney, Susanne Kossatz, Benjamin H Lok, Valentina Schneeberger, Kishore K Gangangari, Naga Vara Kishore Pillarsetty, Wolfgang A Weber, Charles M Rudin, John T Poirier, Thomas Reiner
Insufficient chemotherapy response and rapid disease progression remain concerns for small-cell lung cancer (SCLC). Oncologists rely on serial CT scanning to guide treatment decisions, but this cannot assess in vivo target engagement of therapeutic agents. Biomarker assessments in biopsy material do not assess contemporaneous target expression, intratumoral drug exposure, or drug-target engagement. Here, we report the use of PARP1/2-targeted imaging to measure target engagement of PARP inhibitors in vivo. Using a panel of clinical PARP inhibitors, we show that PARP imaging can quantify target engagement of chemically diverse small molecule inhibitors in vitro and in vivo...
January 12, 2018: Nature Communications
https://www.readbyqxmd.com/read/29330433/effect-of-atorvastatin-on-the-gut-microbiota-of-high-fat-diet-induced-hypercholesterolemic-rats
#8
Tariq Jamal Khan, Youssri M Ahmed, Mazin A Zamzami, Saleh A Mohamed, Imran Khan, Othman A S Baothman, Mohamed G Mehanna, Muhammad Yasir
The aim of the present study was to investigate alterations in gut microbiota associated with hypercholesterolemia and treatment with atorvastatin, a commonly prescribed cholesterol-lowering drug. In this study, seven experimental groups of rats were developed based on diets [high-fat diet (HFD) and normal chow diet (NCD)] and various doses of atorvastatin in HFD and NCD groups. 16S rRNA amplicon sequencing was used to analyze the gut microbiota. Atorvastatin significantly reduced the cholesterol level in treated rats...
January 12, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29330137/the-intersection-of-stress-and-reward-bnst-modulation-of-aversive-and-appetitive-states
#9
REVIEW
Sarah Ch'ng, Jingjing Fu, Robyn M Brown, Stuart J McDougall, Andrew J Lawrence
The bed nucleus of the stria terminalis (BNST) is widely acknowledged as a brain structure that regulates stress and anxiety states, as well as aversive and appetitive behaviours. The diverse roles of the BNST are afforded by its highly modular organisation, neurochemical heterogeneity, and complex intrinsic and extrinsic circuitry. There has been growing interest in the BNST in relation to psychopathologies such as anxiety and addiction. Although research on the human BNST is still in its infancy, there have been extensive preclinical studies examining the molecular signature and hodology of the BNST and their involvement in stress and reward seeking behaviour...
January 9, 2018: Progress in Neuro-psychopharmacology & Biological Psychiatry
https://www.readbyqxmd.com/read/29330067/protein-complexes-as-psychiatric-and-neurological-drug-targets
#10
REVIEW
Akihiko S Kato, Jeffrey M Witkin
The need for improved medications for psychiatric and neurological disorders is clear. Difficulties in finding such drugs demands that all strategic means be utilized for their invention. The discovery of forebrain specific AMPA receptor antagonists, which selectively block the specific combinations of principal and auxiliary subunits present in forebrain regions but spare targets in the cerebellum, was recently disclosed. This discovery raised the possibility that other auxiliary protein systems could be utilized to help identify new medicines...
January 9, 2018: Biochemical Pharmacology
https://www.readbyqxmd.com/read/29329884/impurity-profiling-of-drug-candidates-analytical-strategies-using-reversed-phase-and-mixed-mode-high-performance-liquid-chromatography-methods
#11
Elise Lemasson, Sophie Bertin, Philippe Hennig, Eric Lesellier, Caroline West
The development of new active pharmaceutical ingredients (API) requires accurate impurity profiling. Nowadays, reversed-phase HPLC (RPLC) on C18 stationary phase is the method of first choice for this task and usually employed in generic screening methods. However, this method sometimes fails, especially when the target analyte is not sufficiently retained, making impurity analysis difficult or even impossible. In such cases, a second method must be available. In the present paper, we compare the merits of RPLC on C18 phase to those of previously optimized alternative methods, based on the analysis of a large and diverse set of small-molecule drug candidates...
January 8, 2018: Journal of Chromatography. A
https://www.readbyqxmd.com/read/29329423/development-and-early-validation-of-a-patient-reported-outcome-measure-to-assess-sleep-amongst-people-experiencing-problems-with-alcohol-or-other-drugs
#12
Joanne Neale, Silia Vitoratou, Paul Lennon, Robert Meadows, Sarah Nettleton, Daria Panebianco, John Strang, John Marsden
Study Objectives: To develop a patient reported outcome measure to assess sleep amongst people experiencing problems with alcohol or other drugs. Methods: Item development included secondary analyses of qualitative interviews with drug/alcohol users in residential treatment, a review of validated sleep measures, focus groups with drug/alcohol users in residential treatment, and feedback from drug/alcohol users recruited from community and residential settings. An initial version of the measure was completed by 549 current and former drug/alcohol users (442 in person [IP] and 107 online [OL])...
January 10, 2018: Sleep
https://www.readbyqxmd.com/read/29329257/synthesis-and-pharmacological-activities-of-pyrazole-derivatives-a-review
#13
REVIEW
Khalid Karrouchi, Smaail Radi, Youssef Ramli, Jamal Taoufik, Yahia N Mabkhot, Faiz A Al-Aizari, M'hammed Ansar
Pyrazole and its derivatives are considered a pharmacologically important active scaffold that possesses almost all types of pharmacological activities. The presence of this nucleus in pharmacological agents of diverse therapeutic categories such as celecoxib, a potent anti-inflammatory, the antipsychotic CDPPB, the anti-obesity drug rimonabant, difenamizole, an analgesic, betazole, a H2-receptor agonist and the antidepressant agent fezolamide have proved the pharmacological potential of the pyrazole moiety...
January 12, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29327758/a-computational-analysis-of-pro-angiogenic-therapies-for-peripheral-artery-disease
#14
Lindsay E Clegg, Feilim Mac Gabhann
Inducing therapeutic angiogenesis to effectively form hierarchical, non-leaky networks of perfused vessels in tissue engineering applications and ischemic disease remains an unmet challenge, despite extensive research and multiple clinical trials. Here, we use a previously-developed, multi-scale, computational systems pharmacology model of human peripheral artery disease to screen a diverse array of promising pro-angiogenic strategies, including gene therapy, biomaterials, and antibodies. Our previously-validated model explicitly accounts for VEGF immobilization, Neuropilin-1 binding, and weak activation of VEGF receptor 2 (VEGFR2) by the "VEGFxxxb" isoforms...
January 12, 2018: Integrative Biology: Quantitative Biosciences From Nano to Macro
https://www.readbyqxmd.com/read/29327158/comparison-of-warfarin-requirements-in-post-cardiac-surgery-patients-valve-replacement-versus-non-valve-replacement
#15
Logan M Olson, Andrea M Nei, David L Joyce, Narith N Ou, Ross A Dierkhising, Scott D Nei
INTRODUCTION: Anticoagulation with warfarin affects approximately 140,000 post-cardiac surgery patients every year, yet there remains limited published data in this patient population. Dosing remains highly variable due to intrinsic risk factors that plague cardiac surgery candidates and a lack of diverse literature that can be applied to those who have undergone a cardiac surgery alternative to heart valve replacement (HVR). In the present study, our aim was to compare the warfarin requirements between HVR and non-HVR patients...
January 11, 2018: American Journal of Cardiovascular Drugs: Drugs, Devices, and Other Interventions
https://www.readbyqxmd.com/read/29326268/mapping-the-malaria-parasite-druggable-genome-by-using-in-vitro-evolution-and-chemogenomics
#16
Annie N Cowell, Eva S Istvan, Amanda K Lukens, Maria G Gomez-Lorenzo, Manu Vanaerschot, Tomoyo Sakata-Kato, Erika L Flannery, Pamela Magistrado, Edward Owen, Matthew Abraham, Gregory LaMonte, Heather J Painter, Roy M Williams, Virginia Franco, Maria Linares, Ignacio Arriaga, Selina Bopp, Victoria C Corey, Nina F Gnädig, Olivia Coburn-Flynn, Christin Reimer, Purva Gupta, James M Murithi, Pedro A Moura, Olivia Fuchs, Erika Sasaki, Sang W Kim, Christine H Teng, Lawrence T Wang, Aslı Akidil, Sophie Adjalley, Paul A Willis, Dionicio Siegel, Olga Tanaseichuk, Yang Zhong, Yingyao Zhou, Manuel Llinás, Sabine Ottilie, Francisco-Javier Gamo, Marcus C S Lee, Daniel E Goldberg, David A Fidock, Dyann F Wirth, Elizabeth A Winzeler
Chemogenetic characterization through in vitro evolution combined with whole-genome analysis can identify antimalarial drug targets and drug-resistance genes. We performed a genome analysis of 262 Plasmodium falciparum parasites resistant to 37 diverse compounds. We found 159 gene amplifications and 148 nonsynonymous changes in 83 genes associated with drug-resistance acquisition, where gene amplifications contributed to one-third of resistance acquisition events. Beyond confirming previously identified multidrug-resistance mechanisms, we discovered hitherto unrecognized drug target-inhibitor pairs, including thymidylate synthase and a benzoquinazolinone, farnesyltransferase and a pyrimidinedione, and a dipeptidylpeptidase and an arylurea...
January 12, 2018: Science
https://www.readbyqxmd.com/read/29325708/promising-roles-for-pharmacists-in-addressing-the-u-s-opioid-crisis
#17
Wilson M Compton, Christopher M Jones, Jack B Stein, Eric M Wargo
Overdoses of prescription or illicit opioids claimed the lives of 116 Americans each day in 2016, and the crisis continues to escalate. As healthcare systems evolve to address the crisis, the potential of pharmacists to make a positive difference is significant. In addition to utilizing available prescription drug monitoring programs to help prevent diversion of opioids, practicing pharmacists can be alert for signs of opioid misuse by patients (e.g., multiple prescriptions from different physicians) as well as inappropriate prescribing or hazardous drug combinations that physicians may not be aware of (e...
December 31, 2017: Research in Social & Administrative Pharmacy: RSAP
https://www.readbyqxmd.com/read/29325558/systematic-target-function-annotation-of-human-transcription-factors
#18
Yong Fuga Li, Russ B Altman
BACKGROUND: Transcription factors (TFs), the key players in transcriptional regulation, have attracted great experimental attention, yet the functions of most human TFs remain poorly understood. Recent capabilities in genome-wide protein binding profiling have stimulated systematic studies of the hierarchical organization of human gene regulatory network and DNA-binding specificity of TFs, shedding light on combinatorial gene regulation. We show here that these data also enable a systematic annotation of the biological functions and functional diversity of TFs...
January 10, 2018: BMC Biology
https://www.readbyqxmd.com/read/29324849/the-b-cell-death-function-of-obinutuzumab-hdel-produced-in-plant-nicotiana-benthamiana-l-is-equivalent-to-obinutuzumab-produced-in-cho-cells
#19
Jin Won Lee, Woon Heo, Jinu Lee, Narae Jin, Sei Mee Yoon, Ki Youl Park, Eun Yu Kim, Woo Taek Kim, Joo Young Kim
Plants have attracted attention as bio-drug production platforms because of their economical and safety benefits. The preliminary efficacy of ZMapp, a cocktail of antibodies produced in N. benthamiana (Nicotiana benthamiana L.), suggested plants may serve as a platform for antibody production. However, because the amino acid sequences of the Fab fragment are diverse and differences in post-transcriptional processes between animals and plants remain to be elucidated, it is necessary to confirm functional equivalence of plant-produced antibodies to the original antibody...
2018: PloS One
https://www.readbyqxmd.com/read/29324785/phylogenetic-diversity-antimicrobial-susceptibility-and-virulence-gene-profiles-of-brachyspira-hyodysenteriae-isolates-from-pigs-in-germany
#20
Jessica Joerling, Stefanie A Barth, Karen Schlez, Hermann Willems, Werner Herbst, Christa Ewers
Swine dysentery (SD) is an economically important diarrheal disease in pigs caused by different strongly hemolytic Brachyspira (B.) species, such as B. hyodysenteriae, B. suanatina and B. hampsonii. Possible associations of epidemiologic data, such as multilocus sequence types (STs) to virulence gene profiles and antimicrobial susceptibility are rather scarce, particularly for B. hyodysenteriae isolates from Germany. In this study, B. hyodysenteriae (n = 116) isolated from diarrheic pigs between 1990 and 2016 in Germany were investigated for their STs, susceptibility to the major drugs used for treatment of SD (tiamulin and valnemulin) and genes that were previously linked with virulence and encode for hemolysins (tlyA, tlyB, tlyC, hlyA, BHWA1_RS02885, BHWA1_RS09085, BHWA1_RS04705, and BHWA1_RS02195), outer membrane proteins (OMPs) (bhlp16, bhlp17...
2018: PloS One
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