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https://www.readbyqxmd.com/read/28637676/editorial-focus-on-balance-between-s-nitrosylation-and-denitrosylation-modulates-myoblast-proliferation-independently-of-soluble-guanylyl-cyclase-activation
#1
Hugo P Monteiro, Fernando T Ogata
Myogenesis involves a complex series of signaling events that will result in the formation of muscle fibers. The participation of nitric oxide (NO) in myogenesis is well established. NO generation in skeletal muscle comes from the neuronal isoform of the NO synthase (nNOS). NO signals through cGMP production and s-nitrosylation of proteins in skeletal muscle. In skeletal muscle, nNOS interacts with two domains of caveolin-3 which is part of caveolae, and forms a signaling complex through additional interactions with Src kinase and p21Ras...
June 21, 2017: American Journal of Physiology. Cell Physiology
https://www.readbyqxmd.com/read/28629815/resveratrol-suppresses-pulmonary-tumor-metastasis-by-inhibiting-platelet-mediated-angiogenic-responses
#2
Liwei He, Fangtian Fan, Xianbang Hou, Cuixiang Gao, Li Meng, Shu Meng, Shiwen Huang, Hongyan Wu
BACKGROUND: To explore the impact of Resveratrol (RSV) on the angiogenic potential of activated platelets and to elucidate the underlying mechanism. METHODS: Vascular endothelial growth factor concentrations were measured by enzyme-linked immunosorbent assay. Capillary tube formation assay was used to examine the impact of RSV on the angiogenic potential of activated platelets. The levels of cyclic adenosine monophosphate and cyclic guanosine monophosphate (cGMP) in the supernatant were evaluated using corresponding enzyme-linked immunosorbent assay kits...
May 10, 2017: Journal of Surgical Research
https://www.readbyqxmd.com/read/28626572/optical-control-of-a-receptor-linked-guanylyl-cyclase-using-a-photoswitchable-peptidic-hormone
#3
Tom Podewin, Johannes Broichhagen, Christina Frost, Dieter Groneberg, Julia Ast, Helena Meyer-Berg, Nicholas H F Fine, Andreas Friebe, Martin Zacharias, David J Hodson, Dirk Trauner, Anja Hoffmann-Röder
The optical control over biological function with small photoswitchable molecules has gathered significant attention in the last decade. Herein, we describe the design and synthesis of a small library of photoswitchable peptidomimetics based upon human atrial natriuretic peptide (ANP), in which the photochromic amino acid [3-(3-aminomethyl)phenylazo]phenylacetic acid (AMPP) is incorporated into the peptide backbone. The endogeneous hormone ANP signals via the natriuretic peptide receptor A (NPR-A) through raising intracellular cGMP concentrations, and is involved in blood pressure regulation and sodium homeostasis, as well as lipid metabolism and pancreatic function...
June 1, 2017: Chemical Science
https://www.readbyqxmd.com/read/28626017/amyloid-beta-peptide-is-needed-for-cgmp-induced-long-term-potentiation-and-memory
#4
Agostino Palmeri, Roberta Ricciarelli, Walter Gulisano, Daniela Rivera, Claudia Rebosio, Elisa Calcagno, Maria Rosaria Tropea, Silvia Conti, Utpal Das, Subhojit Roy, Maria A Pronzato, Ottavio Arancio, Ernesto Fedele, Daniela Puzzo
High levels of amyloid-beta peptide (Aβ) have been related to Alzheimer's disease pathogenesis. However, in the healthy brain, low physiologically relevant concentrations of Aβ are necessary for long-term potentiation (LTP) and memory. Because cGMP plays a key role in these processes, here we investigated whether the cyclic nucleotide cGMP influences Aβ levels and function during LTP and memory. We demonstrate that the increase of cGMP levels by the phosphodiesterase-5 inhibitors (PDE5-Is) sildenafil and vardenafil induces a parallel release of Aβ due to a change in the approximation of amyloid precursor protein (APP) and the β-site APP cleaving enzyme 1 (BACE1)...
June 16, 2017: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/28625489/diosmin-reduces-chronic-constriction-injury-induced-neuropathic-pain-in-mice
#5
Mariana M Bertozzi, Ana C Rossaneis, Victor Fattori, Daniela T Longhi-Balbinot, Andressa Freitas, Fernando Q Cunha, José C Alves-Filho, Thiago M Cunha, Rubia Casagrande, Waldiceu A Verri
Injury or dysfunction of somatosensory system induces a complex syndrome called neuropathic pain, which still needs adequate pharmacological control. The current pharmacological treatments were in part developed from natural compounds. Flavonoids are natural polyphenolic molecules presenting varied biological activities and low toxicity. The flavonoid diosmin is a safe compound with good tolerability and low toxicity. This study evaluated the antinociceptive effect of diosmin in the sciatic nerve chronic constriction injury (CCI)-induced neuropathic pain model...
June 15, 2017: Chemico-biological Interactions
https://www.readbyqxmd.com/read/28619938/kilogram-scale-prexasertib-monolactate-monohydrate-synthesis-under-continuous-flow-cgmp-conditions
#6
Kevin P Cole, Jennifer McClary Groh, Martin D Johnson, Christopher L Burcham, Bradley M Campbell, William D Diseroad, Michael R Heller, John R Howell, Neil J Kallman, Thomas M Koenig, Scott A May, Richard D Miller, David Mitchell, David P Myers, Steven S Myers, Joseph L Phillips, Christopher S Polster, Timothy D White, Jim Cashman, Declan Hurley, Robert Moylan, Paul Sheehan, Richard D Spencer, Kenneth Desmond, Paul Desmond, Olivia Gowran
Advances in drug potency and tailored therapeutics are promoting pharmaceutical manufacturing to transition from a traditional batch paradigm to more flexible continuous processing. Here we report the development of a multistep continuous-flow CGMP (current good manufacturing practices) process that produced 24 kilograms of prexasertib monolactate monohydrate suitable for use in human clinical trials. Eight continuous unit operations were conducted to produce the target at roughly 3 kilograms per day using small continuous reactors, extractors, evaporators, crystallizers, and filters in laboratory fume hoods...
June 16, 2017: Science
https://www.readbyqxmd.com/read/28619367/the-vasoprotective-axes-of-the-renin-angiotensin-system-physiological-relevance-and-therapeutic-implications-in-cardiovascular-hypertensive-and-kidney-diseases
#7
REVIEW
Xiao C Li, Jianfeng Zhang, Jia L Zhuo
The renin-angiotensin system (RAS) is undisputedly one of the most prominent endocrine (tissue-to-tissue), paracrine (cell-to-cell) and intracrine (intracellular/nuclear) vasoactive systems in the physiological regulation of neural, cardiovascular, blood pressure, and kidney function. The importance of the RAS in the development and pathogenesis of cardiovascular, hypertensive and kidney diseases has now been firmly established in clinical trials and practice using renin inhibitors, angiotensin-converting enzyme (ACE) inhibitors, type 1 (AT1) angiotensin II (ANG II) receptor blockers (ARBs), or aldosterone receptor antagonists as major therapeutic drugs...
June 12, 2017: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
https://www.readbyqxmd.com/read/28615047/sensitivity-to-sevoflurane-anesthesia-is-decreased-in-mice-with-a-congenital-deletion-of-guanylyl-cyclase-1-alpha
#8
Yasuko Nagasaka, Martin Wepler, Robrecht Thoonen, Patrick Y Sips, Kaitlin Allen, Jan A Graw, Vincent Yao, Sara M Burns, Stefan Muenster, Peter Brouckaert, Keith Miller, Ken Solt, Emmanuel S Buys, Fumito Ichinose, Warren M Zapol
BACKGROUND: Volatile anesthetics increase levels of the neurotransmitter nitric oxide (NO) and the secondary messenger molecule cyclic guanosine monophosphate (cGMP) in the brain. NO activates the enzyme guanylyl cyclase (GC) to produce cGMP. We hypothesized that the NO-GC-cGMP pathway contributes to anesthesia-induced unconsciousness. METHODS: Sevoflurane-induced loss and return of righting reflex (LORR and RORR, respectively) were studied in wild-type mice (WT) and in mice congenitally deficient in the GC-1α subunit (GC-1(-/-) mice)...
June 14, 2017: BMC Anesthesiology
https://www.readbyqxmd.com/read/28614771/mantidis-ootheca-induces-vascular-relaxation-through-pi3k-akt-mediated-nitric-oxide-cyclic-gmp-protein-kinase-g-signaling-in-endothelial-cells
#9
H Y Kim, Y J Lee, B H Han, J J Yoon, Y M Ahn, M H Hong, R Tan, D G Kang, H S Lee
Mantidis ootheca (Sang Piao Xiao) is well known mantis eggs in a foamy pouch. The purpose of the present study was to investigate the underlying cellular mechanisms of the nitric oxide (NO)-releasing property of the aqueous extract of Mantidis ootheca (AMO) in rat aorta and vascular endothelial cells. AMO was examined for its vascular relaxant effect in isolated phenylephrine-precontracted rat thoracic aortic rings. The roles of the nitric oxide (NO) signaling in the AMO-induced effects were tested in human umbilical vein endothelial cells (HUVECs)...
April 2017: Journal of Physiology and Pharmacology: An Official Journal of the Polish Physiological Society
https://www.readbyqxmd.com/read/28611079/elevated-camp-improves-signal-to-noise-ratio-in-amphibian-rod-photoreceptors
#10
Luba A Astakhova, Darya A Nikolaeva, Tamara V Fedotkina, Victor I Govardovskii, Michael L Firsov
The absolute sensitivity of vertebrate retinas is set by a background noise, called dark noise, which originates from several different cell types and is generated by different molecular mechanisms. The major share of dark noise is produced by photoreceptors and consists of two components, discrete and continuous. Discrete noise is generated by spontaneous thermal activations of visual pigment. These events are undistinguishable from real single-photon responses (SPRs) and might be considered an equivalent of the signal...
June 13, 2017: Journal of General Physiology
https://www.readbyqxmd.com/read/28610481/efficacy-of-humanized-mesenchymal-stem-cell-cultures-for-bone-tissue-engineering-a-systematic-review-with-a-focus-on-platelet-derivatives
#11
Siddharth Shanbhag, Andreas Stavropoulos, Salwa Suliman, Tor Hervig, Kamal Mustafa
Fetal bovine serum (FBS) is the most commonly used supplement for ex vivo expansion of human mesenchymal stem cells (hMSCs) for bone tissue engineering applications. However, from a clinical standpoint, it is important to substitute animal-derived products according to current Good Manufacturing Practice (cGMP) guidelines. Humanized alternatives to FBS include three categories of products: human serum (HS), human platelet-derivatives (HPD) - including platelet lysate (PL) or releasate (PR), produced by freeze-/thawing or chemical activation of platelet concentrates, respectively; and chemically-defined media (CDM)...
June 13, 2017: Tissue Engineering. Part B, Reviews
https://www.readbyqxmd.com/read/28609666/the-hippeastrum-hybridum-pepr1-gene-hppepr1-encodes-a-functional-guanylyl-cyclase-and-is-involved-in-early-response-to-fungal-infection
#12
Brygida Świeżawska, Krzysztof Jaworski, Maria Duszyn, Agnieszka Pawełek, Adriana Szmidt-Jaworska
It is generally known that cyclic GMP widespread in prokaryotic and eukaryotic cells, is involved in essential cellular processes and stress signal transduction. However, in contrast to animals the knowledge about plant guanylyl cyclases (GCs) which catalyze the formation of cGMP from GTP is still quite obscure. Recent studies of plant GCs are focused on identification and functional analysis of a new family of membrane proteins called "moonlighting kinases with GC activity" with guanylyl cyclase catalytic center encapsulated within intracellular kinase domain...
June 1, 2017: Journal of Plant Physiology
https://www.readbyqxmd.com/read/28603044/relaxation-of-isolated-guinea-pig-trachea-by-apigenin-a-constituent-of-celery-via-inhibition-of-phosphodiesterase
#13
Junn-Lain Chen, Wun-Chang Ko
Apigenin, was reported to have vasodilatory effects by inhibiting Ca(2+) influx through both voltage- and receptor-operated calcium channels, but not by inhibiting cAMP- or cGMP-phosphodiesterases (PDEs) in rat thoracic aorta. However, apigenin was reported to inhibit PDE1, 2 and 3 in guinea-pig lung and heart. The aim of this study was to clarify that guinea-pig tracheal relaxation by apigenin whether via PDE inhibition. We isometrically recorded the tension of isolated guinea-pig tracheal segments on a polygraph...
June 9, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28599252/the-effect-of-microrna-328-antagomir-on-erectile-dysfunction-in-streptozotocin-induced-diabetic-rats
#14
Dong-Shui Li, Liang Feng, Long-Hua Luo, Zhi-Feng Duan, Xian-Long Li, Chun-Hua Yin, Xiang Sun
The study aimed at exploring the effect of microRNA-328 (miR-328) antagomir on erectile dysfunction (ED) in streptozotocin (STZ)-induced diabetic rats. A total of 120 male Sprague-Dawley (SD) rats were selected for this study. Fifteen rats were assigned as the diabetic control group and 75 out of the remaining rats (105 diabetic rat models) were divided into five groups with 15 rats in each group: diabetic ED, diabetic ED+negative control (NC), diabetic ED+miR-328 antagomir, diabetic ED+sildenafil and diabetic ED+miR-328 antagomir+sildenafil groups...
June 6, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28599060/evaluation-of-pharmacokinetic-and-pharmacodynamic-drug-drug-interaction-of-sacubitril-valsartan-lcz696-and-sildenafil-in-patients-with-mild-to-moderate-hypertension
#15
Hsiu-Ling Hsiao, Thomas H Langenickel, Jesika Petruck, Kiran Kode, Surya Ayalasomayajula, Uwe Schuehly, Michael Greeley, Parasar Pal, Wei Zhou, Margaret F Prescott, Gangadhar Sunkara, Iris Rajman
Sacubitril/valsartan (LCZ696) is indicated for the treatment of patients with heart failure and reduced ejection fraction (HFrEF). Since patients with HFrEF may receive sacubitril/valsartan and sildenafil, both increasing cGMP, the present study evaluated the pharmacokinetic and pharmacodynamic drug interaction potential between sacubitril/valsartan and sildenafil. In this open-label, 3-period, single sequence study, patients with mild-to-moderate hypertension (153.8±8.2 mm Hg mean SBP) received a single dose of sildenafil 50 mg, sacubitril/valsartan 400 mg once daily for 5 days, and sacubitril/valsartan and sildenafil co-administration...
June 9, 2017: Clinical Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/28596298/sex-differences-in-pulmonary-vascular-control-focus-on-the-nitric-oxide-pathway
#16
Daphne P M de Wijs-Meijler, A H Jan Danser, Irwin K M Reiss, Dirk J Duncker, Daphne Merkus
Although the incidence of pulmonary hypertension is higher in females, the severity and prognosis of pulmonary vascular disease in both neonates and adults have been shown to be worse in male subjects. Studies of sex differences in pulmonary hypertension have mainly focused on the role of sex hormones. However, the contribution of sex differences in terms of vascular signaling pathways regulating pulmonary vascular function remains incompletely understood. Consequently, we investigated pulmonary vascular function of male and female swine in vivo, both at rest and during exercise, and in isolated small pulmonary arteries in vitro, with a particular focus on the NO-cGMP-PDE5 pathway...
June 2017: Physiological Reports
https://www.readbyqxmd.com/read/28596054/a-potent-and-selective-natriuretic-peptide-receptor-3-blocker-11-mer-peptide-created-by-hybridization-of-musclin-and-atrial-natriuretic-peptide
#17
Naoki Nishizawa, Goshi Nakamura, Yoko Noguchi, Hideyuki Nakagawa, Ayako Shimizu, Masaharu Nakayama, Shiro Takekawa, Taiji Asami
The natriuretic peptide (NP) system is a critical endocrine, autocrine, and paracrine system and has been investigated for potential use against cardiovascular and metabolic diseases. The clearance of NPs is regulated by the proteolysis of neutral endopeptidase (NEP) and by endocytosis via natriuretic peptide receptor-3 (NPR3). A linear NPR3-selective peptide, [Cha(8)]-ANP(7-16)-NH2 (1), showed potent binding affinity for NPR3 but poor predicted chemical stability due to its free thiol group. A 12-mer peptide (9) without a thiol group was designed by the hybridization of two NPR3-binding peptides: a linear ANP fragment peptide analog and musclin, a murine member of the bHLH family of transcription factors, possessed high binding affinity and strict selectivity for NPR3...
May 20, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28592882/ml290-is-a-biased-allosteric-agonist-at-the-relaxin-receptor-rxfp1
#18
Martina Kocan, Mohsin Sarwar, Sheng Y Ang, Jingbo Xiao, Juan J Marugan, Mohammed A Hossain, Chao Wang, Dana S Hutchinson, Chrishan S Samuel, Alexander I Agoulnik, Ross A D Bathgate, Roger J Summers
Activation of the relaxin receptor RXFP1 has been associated with improved survival in acute heart failure. ML290 is a small molecule RXFP1 agonist with simple structure, long half-life and high stability. Here we demonstrate that ML290 is a biased agonist in human cells expressing RXFP1 with long-term beneficial actions on markers of fibrosis in human cardiac fibroblasts (HCFs). ML290 did not directly compete with orthosteric relaxin binding and did not affect binding kinetics, but did increase binding to RXFP1...
June 7, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28592587/linaclotide-activates-guanylate-cyclase-c-cgmp-protein-kinase-ii-dependent-trafficking-of-cftr-in-the-intestine
#19
Md Kaimul Ahsan, Boris Tchernychev, Marco M Kessler, Robert M Solinga, David Arthur, Cristina I Linde, Inmaculada Silos-Santiago, Gerhard Hannig, Nadia A Ameen
The transmembrane receptor guanylyl cyclase-C (GC-C), expressed on enterocytes along the intestine, is the molecular target of the GC-C agonist peptide linaclotide, an FDA-approved drug for treatment of adult patients with Irritable Bowel Syndrome with Constipation and Chronic Idiopathic Constipation. Polarized human colonic intestinal cells (T84, CaCo-2BBe) rat and human intestinal tissues were employed to examine cellular signaling and cystic fibrosis transmembrane conductance regulator (CFTR)-trafficking pathways activated by linaclotide using confocal microscopy, in vivo surface biotinylation, and protein kinase-II (PKG-II) activity assays...
June 2017: Physiological Reports
https://www.readbyqxmd.com/read/28587776/pharmacological-characterization-of-a-novel-potent-selective-and-orally-active-phosphodiesterase-2a-inhibitor-pdm-631
#20
Shunsuke Maehara, Keita Arakawa, Kotaro Hoshida, Hiroshi Nagasue, Noboru Chida, Kazunari Nakao, Shoji Furusako
Recently, we identified a novel phosphodiesterase 2A (PDE2A) inhibitor, PDM-631 ((S)-3-cyclopropyl-6-methyl-1-(1-(4-(trifluoromethoxy)phenyl)propan-2-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one). PDM-631 showed potent inhibitory activities for human and rat PDE2A with IC50 values of 1.5 and 4.2nM, respectively and more than 2000-fold selectivity against other phosphodiesterases. In rat studies, PDM-631 showed oral bioavailability and good brain penetration, and increased the cGMP levels in the cortex...
June 3, 2017: European Journal of Pharmacology
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