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Phosphodiesterase 4

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https://www.readbyqxmd.com/read/27901486/triple-negative-breast-cancer-development-can-be-selectively-suppressed-by-sustaining-an-elevated-level-of-cellular-cyclic-amp-through-simultaneously-blocking-its-efflux-and-decomposition
#1
Wei Wang, Yue Li, Jessica Y Zhu, Dongdong Fang, Han-Fei Ding, Zheng Dong, Qing Jing, Shi-Bing Su, Shuang Huang
Triple negative breast cancer (TNBC) has the highest mortality among all breast cancer types and lack of targeted therapy is a key factor contributing to its high mortality rate. In this study, we show that 8-bromo-cAMP, a cyclic adenosine monophosphate (cAMP) analog at high concentration (> 1 mM) selectively suppresses TNBC cell growth. However, commonly-used cAMP-elevating agents such as adenylyl cyclase activator forskolin and pan phosphodiesterase inhibitor 3-isobutyl-1-methylxanthine (IBMX) are ineffective...
November 25, 2016: Oncotarget
https://www.readbyqxmd.com/read/27896836/radiosynthesis-and-biological-evaluation-of-the-new-pde10a-radioligand-18-f-aq28a
#2
Sally Wagner, Rodrigo Teodoro, Winnie Deuther-Conrad, Mathias Kranz, Matthias Scheunemann, Steffen Fischer, Barbara Wenzel, Ute Egerland, Norbert Hoefgen, Jörg Steinbach, Peter Brust
Cyclic nucleotide phosphodiesterase 10A (PDE10A) regulates the level of the second messengers cAMP and cGMP in particular in brain regions assumed to be associated with neurodegenerative and psychiatric diseases. A better understanding of the pathophysiological role of the expression of PDE10A could be obtained by quantitative imaging of the enzyme by positron emission tomography (PET). Thus, in this study we developed, radiolabeled, and evaluated a new PDE10A radioligand, 8-bromo-1-(6-[(18) F]fluoropyridin-3-yl)-3,4-dimethylimidazo[1,5-a]quinoxaline ([(18) F]AQ28A)...
November 29, 2016: Journal of Labelled Compounds & Radiopharmaceuticals
https://www.readbyqxmd.com/read/27890378/design-and-synthesis-of-4-5-6-7-tetrahydro-1h-1-2-diazepin-7-one-derivatives-as-a-new-series-of-phosphodiesterase-4-pde4-inhibitors
#3
Sara Guariento, Anna Karawajczyk, James A Bull, Gessica Marchini, Martyna Bielska, Xenia Iwanowa, Olga Bruno, Paola Fossa, Fabrizio Giordanetto
Phosphodiesterase 4 (PDE4) inhibitors have attractive therapeutic potential in respiratory, inflammatory, metabolic and CNS disorders. The present work details the design, chemical exploration and biological profile of a novel PDE4 inhibitor chemotype. A diazepinone ring was identified as an under-represented heterocyclic system fulfilling a set of PDE4 structure-based design hypotheses. Rapid exploration of the structure activity relationships for the series was enabled by robust and scalable two/three-steps parallel chemistry protocols...
November 16, 2016: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/27878061/oral-apremilast-for-the-treatment-of-plaque-psoriasis
#4
REVIEW
James Q Del Rosso, Leon Kircik
This article provides an update on the use of oral apremilast, a phosphodiesterase-4 (PDE4) inhibitor, for the treatment of plaque psoriasis. Emphasis is placed on safety evaluations, although efficacy considerations are also addressed. Both two-year and three -year data analyses support the favorable safety profile reported in pivotal trials with this agent. Although effective in many study subjects despite baseline characteristics, higher response rates were noted in those with a baseline psoriasis area and severity index (PASI) score <20 and in subjects not previously treated with systemic therapy for psoriasis...
September 2016: Journal of Clinical and Aesthetic Dermatology
https://www.readbyqxmd.com/read/27873367/mir-219-attenuates-demyelination-in-cuprizone-induced-demyelinated-mice-by-regulating-monocarboxylate-transporter-1
#5
Sihan Liu, Chuanlu Ren, Xuebin Qu, Xiuxiang Wu, Fuxing Dong, Yadav Kaushal Chand, Hongbin Fan, Ruiqin Yao, Deqin Geng
Remyelination is limited in patients with multiple sclerosis (MS) due to the difficulties in recruiting proliferating oligodendrocyte precursors (OPCs), the inhibition of OPC differentiation and/or maturation, and/or failure in the generation of the myelin sheath. In vitro studies have revealed that miR-219 is necessary for OPC differentiation and monocarboxylate transporter 1 (MCT1) plays a vital role in oligodendrocyte maturation and myelin synthesis. Herein, we hypothesized that miR-219 might promote oligodendrocyte differentiation and attenuate demyelination in a cuprizone (CPZ)-induced demyelinated model by regulating the expression of MCT1...
November 22, 2016: European Journal of Neuroscience
https://www.readbyqxmd.com/read/27872196/induction-of-ectonucleotide-pyrophosphatase-phosphodiesterase-3-during-the-periovulatory-period-in-the-rat-ovary
#6
Fei-Xue Li, Jiao-Jiao Yu, Ying Liu, Xiao-Ping Miao, Thomas E Curry
Ectonucleotide pyrophosphatase/phosphodiesterase 3 (Enpp3) is involved in multiple physiological processes, such as morphological changes and inflammatory processes. The present study investigated the spatiotemporal expression pattern and regulatory mechanisms controlling expression of Enpp3 in the rat ovary during the periovulatory period. Immature female rats were injected with pregnant mare serum gonadotropin to stimulate follicular development. Ovaries, granulosa cells, or theca-interstitial cells were collected at various times after human chorionic gonadotropin (hCG) administration...
November 20, 2016: Reproductive Sciences
https://www.readbyqxmd.com/read/27869356/apremilast-an-oral-phosphodiesterase-4-pde4-inhibitor-a-novel-treatment-option-for-nurse-practitioners-treating-patients-with-psoriatic-disease
#7
Melodie Young, Heather L Roebuck
BACKGROUND AND PURPOSE: Apremilast is an oral nonbiologic medication approved for the treatment of adult patients with active psoriatic arthritis and for patients with moderate to severe plaque psoriasis. This article summarizes the efficacy and safety of apremilast and provides characterization of the novel medication with clinical perspectives to successfully incorporate this therapy into practice for appropriate patients. DATA SOURCES: A review and synthesis of the results from the ESTEEM (Efficacy and Safety Trial Evaluating the Effects of Apremilast in Psoriasis) phase 3 clinical studies evaluating the efficacy, safety, and tolerability of apremilast for the treatment of moderate to severe plaque psoriasis was conducted...
November 21, 2016: Journal of the American Association of Nurse Practitioners
https://www.readbyqxmd.com/read/27869315/aminoalkyl-derivatives-of-8-alkoxypurine-2-6-diones-multifunctional-5-ht1a-5-ht7-receptor-ligands-and-pde-inhibitors-with-antidepressant-activity
#8
Grażyna Chłoń-Rzepa, Agnieszka Zagórska, Paweł Żmudzki, Adam Bucki, Marcin Kołaczkowski, Anna Partyka, Anna Wesołowska, Grzegorz Kazek, Monika Głuch-Lutwin, Agata Siwek, Gabriela Starowicz, Maciej Pawłowski
In the search for potential psychotropic agents, a new series of 3,7-dimethyl- and 1,3-dimethyl-8-alkoxypurine-2,6-dione derivatives of arylpiperazines, perhydroisoquinolines, or tetrahydroisoquinolines with flexible alkylene spacers (5-16 and 21-32) were synthesized and evaluated for 5-HT1A /5-HT7 receptor affinities as well as PDE4B1 and PDE10A inhibitory properties. The 1-(4-(4-(2-hydroxyphenyl)piperazin-1-yl)butyl)-3,7-dimethyl-8-propoxypurine-2,6-dione (16) and 7-(2-hydroxyphenyl)piperazinylalkyl-1,3-dimethyl-8-ethoxypurine-2,6-diones (31 and 32) as potent dual 5-HT1A /5-HT7 receptor ligands with antagonistic activity produced an antidepressant-like effect in the forced swim test in mice...
November 21, 2016: Archiv der Pharmazie
https://www.readbyqxmd.com/read/27863377/variable-patterns-of-ectopic-mineralization-in-enpp1asj-2j-mice-a-model-for-generalized-arterial-calcification-of-infancy
#9
Sarah Y Siu, Nathaniel A Dyment, David W Rowe, John P Sundberg, Jouni Uitto, Qiaoli Li
Generalized arterial calcification of infancy (GACI) is an autosomal recessive disorder characterized by early onset of extensive mineralization of the cardiovascular system. The classical forms of GACI are caused by mutations in the ENPP1 gene, encoding a membrane-bound pyrophosphatase/phosphodiesterase that hydrolyzes ATP to AMP and inorganic pyrophosphate. The asj-2J mouse harboring a spontaneous mutation in the Enpp1 gene has been characterized as a model for GACI. These mutant mice develop ectopic mineralization in skin and vascular connective tissues as well as in cartilage and collagen-rich tendons and ligaments...
November 14, 2016: Oncotarget
https://www.readbyqxmd.com/read/27862445/identification-of-the-camp-phosphodiesterase-cpda-as-novel-key-player-in-camp-dependent-regulation-in-corynebacterium-glutamicum
#10
Julia Schulte, Meike Baumgart, Michael Bott
The second messenger cyclic AMP (cAMP) plays an important role in the metabolism of Corynebacterium glutamicum, as the global transcriptional regulator GlxR requires complex formation with cAMP to become active. Whereas a membrane-bound adenylate cyclase, CyaB, was shown to be involved in cAMP synthesis, enzymes catalyzing cAMP degradation have not been described yet. In this study we identified a class II cAMP phosphodiesterase named CpdA (Cg2761), homologs of which are present in many Actinobacteria. The purified enzyme has a Km(app) value of 2...
November 12, 2016: Molecular Microbiology
https://www.readbyqxmd.com/read/27861916/sildenafil-therapy-for-fetal-cardiovascular-dysfunction-during-hypoxic-development-studies-in-the-chick-embryo
#11
Nozomi Itani, Katie L Skeffington, Christian Beck, Dino A Giussani
There is a need for developing clinically translatable therapy for preventing fetal origins of cardiovascular disease in pregnancy complicated by chronic fetal hypoxia. Evidence shows that sildenafil protects placental perfusion and fetal growth. However, whether beneficial effects of sildenafil transcend onto the fetal heart and circulation in complicated development is unknown. We isolated the direct effects of sildenafil on the fetus using the chick embryo and hypothesised that sildenafil also protects fetal cardiovascular function in hypoxic development...
November 12, 2016: Journal of Physiology
https://www.readbyqxmd.com/read/27859531/increase-of-intracellular-cyclic-amp-by-pde4-inhibitors-affects-hepg2-cell-cycle-progression-and-survival
#12
Mara Massimi, Silvia Cardarelli, Francesca Galli, Maria Federica Giardi, Federica Ragusa, Nadia Panera, Benedetta Cinque, Maria Grazia Cifone, Stefano Biagioni, Mauro Giorgi
Type 4 cyclic nucleotide phosphodiesterases (PDE4) are major members of a superfamily of enzymes (PDE) involved in modulation of intracellular signaling mediated by cAMP. Broadly expressed in most human tissues and present in large amounts in the liver, PDEs have in the last decade been key therapeutic targets for several inflammatory diseases. Recently, a significant body of work has underscored their involvement in different kinds of cancer, but with no attention paid to liver cancer. The present study investigated the effects of two PDE4 inhibitors, rolipram and DC-TA-46, on the growth of human hepatoma HepG2 cells...
November 16, 2016: Journal of Cellular Biochemistry
https://www.readbyqxmd.com/read/27856658/new-targets-in-psoriatic-arthritis
#13
REVIEW
Juergen Braun
PsA is an immune-mediated chronic inflammatory disease that affects both skin and joints; it is a heterogeneous disease characterized by synovitis, enthesitis, dactylitis and spondylitis. The impact on patients and the burden of disease are substantial. For assessment of the disease, patient-reported outcomes are increasingly important. Conventional therapy consists of NSAIDs, local and systemic CSs, and synthetic and biological DMARDs. While MTX, LEF, SSZ and CYC are the synthetic drugs mainly used, TNF-α blocking agents have represented the majority of biologics used in the last decade (infliximab, etanercept, adalimumab, certolizumab and golimumab)...
December 2016: Rheumatology
https://www.readbyqxmd.com/read/27853102/cardiac-safety-profile-of-sildenafil-chronotropic-inotropic-and-coronary-vasodilator-effects-in-the-canine-isolated-blood-perfused-heart-preparations
#14
Nur Jaharat Lubna, Yuji Nakamura, Xin Cao, Takeshi Wada, Hiroko Izumi-Nakaseko, Kentaro Ando, Atsushi Sugiyama
Sildenafil is a phosphodiesterase type-5 inhibitor. We evaluated the effects of sildenafil on the sinoatrial rate, developed tension of the papillary muscle and coronary blood flow by using the canine isolated, blood-perfused sinoatrial node and papillary muscle preparations. The former preparation had a regular automaticity rate of 106 ± 1 beats/min (n = 4), whereas the latter showed a developed tension of 22 ± 4 mN (n = 4) and a coronary blood flow of 3.9 ± 0.1 mL/min (n = 4). Intracoronary injection of 10, 30 and 100 µg of sildenafil, which would provide about 20 to 200 times higher plasma drug concentrations than its therapeutic level, increased the automaticity rate by 4, 12 and 22%, the developed tension by 19, 55 and 118% and the coronary blood flow by 42, 95 and 142%, respectively...
2016: Journal of Toxicological Sciences
https://www.readbyqxmd.com/read/27846617/real-world-experience-with-apremilast-in-treating-psoriasis
#15
Julia N Mayba, Melinda J Gooderham
BACKGROUND: Clinical trial data have shown apremilast, an oral phosphodiesterase-4 inhibitor, to be efficacious and safe for the treatment of psoriasis. However, little real-world experience using apremilast in the community setting has been documented. OBJECTIVES: Many patients with psoriasis are often unresponsive to various treatment modalities, including topical, systemic, and biologic medications. The aim of this chart review was to assess the overall patient experience while using apremilast to treat psoriasis...
October 21, 2016: Journal of Cutaneous Medicine and Surgery
https://www.readbyqxmd.com/read/27843073/off-target-effect-of-sildenafil-on-postsurgical-erectile-dysfunction-alternate-pathways-and-localized-delivery-system
#16
Amirali Salmasi, Geun Taek Lee, Neal Patel, Ritu Goyal, Michael Dinizo, Young Suk Kwon, Part K Modi, Izak Faiena, Nara Lee, Johanna L Hannan, Joachim Kohn, Isaac Yi Kim
INTRODUCTION: There is no consensus on the best oral phosphodiesterase type 5 inhibitor (PDE5I) for patients undergoing penile rehabilitation after surgical nerve injury. AIM: To determine the mechanism of PDE5I on cultured neuronal cells and the effectiveness of local drug delivery using nanospheres (NSPs) to sites of nerve injury in a rat model of bilateral cavernous nerve injury (BCNI). METHODS: The effects of sildenafil, tadalafil, and vardenafil on cyclic adenosine monophosphate, cyclic guanosine monophosphate, and cell survival after exposure to hypoxia and H2O2 were measured in PC12, SH-SY5Y, and NTERA-2 (NT2) cell cultures...
November 11, 2016: Journal of Sexual Medicine
https://www.readbyqxmd.com/read/27836567/management-of-psoriatic-arthritis-early-diagnosis-monitoring-of-disease-severity-and-cutting-edge-therapies
#17
REVIEW
Siba P Raychaudhuri, Reason Wilken, Andrea C Sukhov, Smriti K Raychaudhuri, Emanual Maverakis
Psoriatic arthritis (PsA) is a heterogeneous disease that can involve a variety of distinct anatomical sites including a patient's peripheral and axial joints, entheses, skin and nails. Appropriate management of PsA requires early diagnosis, monitoring of disease activity, and utilization of cutting edge therapies. To accomplish the former there are a variety of PsA-specific tools available to screen, diagnose, and assess patients. This review will outline the recently developed PsA screening tools, including the Toronto Psoriatic Arthritis Screening Questionnaire (TOPAS), the Psoriasis Epidemiology Screening Tool (PEST), the Psoriatic Arthritis Screening and Evaluation (PASE), and the Psoriasis and Arthritis Screening Questionnaire (PASQ)...
November 8, 2016: Journal of Autoimmunity
https://www.readbyqxmd.com/read/27833852/molecular-cloning-heterologous-expression-and-enzymatic-characterization-of-lysoplasmalogen-specific-phospholipase-d-from-thermocrispum-sp
#18
Yusaku Matsumoto, Nana Kashiwabara, Takayuki Oyama, Kazutaka Murayama, Hideyuki Matsumoto, Shin-Ich Sakasegawa, Daisuke Sugimori
: Lysoplasmalogen (LyPls)-specific phospholipase D (LyPls-PLD) is an enzyme that catalyses the hydrolytic cleavage of the phosphoester bond of LyPls, releasing ethanolamine or choline, and 1-(1-alkenyl)-sn-glycero-3-phosphate (lysoplasmenic acid). Little is known about LyPls-PLD and metabolic pathways of plasmalogen (Pls). Reportedly, Pls levels in human serum/plasma correlate with several diseases such as Alzheimer's disease and arteriosclerosis as well as a variety of biological processes including apoptosis and cell signaling...
November 2016: FEBS Open Bio
https://www.readbyqxmd.com/read/27826996/treatment-of-psoriatic-arthritis-with-traditional-dmard-s-and-novel-therapies-approaches-and-recommendations
#19
Ajesh B Maharaj, Vinod Chandran
Recent advances in the therapeutics of psoriatic arthritis (PsA) have provided more options to clinicians managing PsA. The purpose of this review is to update the reader on treatment options for PsA using conventional synthetic disease modifying agents (csDMARDs) and novel therapies including tumour necrosis factor alpha inhibitors, interleukin 12/23 inhibitor (ustekinumab), the interleukin 17 antagonists including secukinumab, brodalumab, ixekizumab, and the phosphodiesterase-4 inhibitor, apremilast. Areas covered: We reviewed published articles on the treatment of PsA...
November 18, 2016: Expert Review of Clinical Immunology
https://www.readbyqxmd.com/read/27821246/erratum-to-effect-of-roflumilast-novel-phosphodiesterase-4-inhibitor-on-lung-chronic-graft-versus-host-disease-in-mice
#20
Sei Won Kim, Ji Young Lim, Chin Kook Rhee, Ji Hye Kim, Chan Kwon Park, Tae Jung Kim, Chul Soo Cho, Chang Ki Min, Hyoung Kyu Yoon
No abstract text is available yet for this article.
November 4, 2016: Experimental Hematology
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