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Biochemical Pharmacology

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https://www.readbyqxmd.com/read/30236477/gain-of-affinity-for-vegf165-binding-within-the-vegfr2-nrp1-cellular-complex-detected-by-an-htrf-based-binding-assay
#1
Johanna Auriau, Clara Roujeau, Zakia Belaid Choucair, Atsuro Oishi, Carine Derviaux, Thomas Roux, Eric Trinquet, Olivier Hermine, Ralf Jockers, Julie Dam
Neuroplin 1 (NRP1), a transmembrane protein interacting with Vascular Endothelial Growth Factor VEGF-A165 (called here VEGF165) and the tyrosine kinase Receptor 2 (VEGFR2) promote angiogenesis and vascular homeostasis. In a pathophysiological context, several studies suggested that VEGFR2 and NRP1 mediate tumor development and progression. Given the involvement of the VEGF165 network in promoting tumor angiogenesis, NRP1, VEGFR2 and VEGF165 have been identified as targets for anti-angiogenic therapy. No binding assay exists to monitor specifically the binding of VEGF165 to the VEGFR2/NRP1 complex in intact cells...
September 17, 2018: Biochemical Pharmacology
https://www.readbyqxmd.com/read/30232037/the-potential-role-of-adenosine-signaling-in-the-pathogenesis-of-melanoma
#2
REVIEW
Amirhossein Bahreyni, Melika Rezaei, Majid Khazaei, Hamid Fuiji, Gordon A Ferns, Mikhail Ryzhikov, Amir Avan, Seyed Mahdi Hassanian
Melanoma cancer cell proliferation, motility, invasion, and tumor growth is affected by the adenosine pathway that consists of adenosine-synthesizing enzymes, receptors, and their respective agonists/antagonists. Accumulating evidence suggests that ischemia and inflammation, two conditions associated with melanoma, display dysregulated adenosine metabolism, which implicates it as the mechanism responsible for the pathogenesis of melanoma, thereby resulting in advanced diagnosis and therapy. Suppression of adenosine signaling by inhibiting adenosine receptors or adenosine-generating enzymes (CD39 and CD73) on melanoma cells presents a novel therapeutic target for patients with melanoma...
September 16, 2018: Biochemical Pharmacology
https://www.readbyqxmd.com/read/30222970/metformin-downregulates-the-mitochondrial-carrier-slc25a10-in-a-glucose-dependent-manner
#3
Qian Zhao, Xiaoshan Zhou, Sophie Curbo, Anna Karlsson
Metformin, a commonly used agent in the treatment of type 2 diabetes, is also associated with reduced risk of cancer development and improvement in cancer survival. Although much is known about metformin, the mechanisms behind its anti-cancer properties are not fully understood. In this study we addressed the role of a mitochondrial transporter commonly upregulated in cancer cells, SLC25A10, for cell survival and metabolism in the presence of metformin. SLC25A10 is a carrier in the mitochondrial inner membrane that transports malate and succinate out of the mitochondria, in exchange of phosphate and sulfate...
September 14, 2018: Biochemical Pharmacology
https://www.readbyqxmd.com/read/30222969/pancreatic-ductal-adenocarcinoma-cell-secreted-extracellular-vesicles-containing-ceramide-1-phosphate-promote-pancreatic-cancer-stem-cell-motility
#4
Norbert Kuc, Allison Doermann, Carolyn Shirey, Daniel D Lee, Chinn-Woan Lowe, Niranjan Awasthi, Roderich E Schwarz, Robert V Stahelin, Margaret A Schwarz
The high mortality rate associated with pancreatic ductal adenocarcinoma (PDAC) is in part due to lack of effective therapy for this highly chemoresistant tumor. Cancer stem cells, a subset of cancer cells responsible for tumor initiation and metastasis, are not targeted by conventional cytotoxic agents, which renders the identification of factors that facilitate cancer stem cell activation useful in defining targetable mechanisms. We determined that bioactive sphingolipid induced migration of pancreatic cancer stem cells (PCSC) and signaling was specific to ceramide-1-phosphate (C1P)...
September 14, 2018: Biochemical Pharmacology
https://www.readbyqxmd.com/read/30222968/about-canonical-non-canonical-and-immunogenic-cell-death-basic-mechanisms-and-translational-applications-a-meeting-report-of-the-international-cell-death-society
#5
EDITORIAL
Zahra Zakeri, Richard A Lockshin, Marc Diederich
International Cell Death Society held its 25th meeting, entitled "About canonical, non-canonical, and immunogenic cell death: basic mechanisms and translational applications" in Seoul, South Korea, May 31-June 2, 2018, addressed the most current issues in the field. Now that many types and pathways of cell death are recognized, attention has turned to how the threshold to death is maintained or surpassed, and how and what intracellular signals control the process. Most of the speakers addressed these topics, focusing on mitochondria and on new high-resolution techniques that promise to answer current questions...
September 14, 2018: Biochemical Pharmacology
https://www.readbyqxmd.com/read/30222967/lkb1-loss-is-associated-with-glutathione-deficiency-under-oxidative-stress-and-sensitivity-of-cancer-cells-to-cytotoxic-drugs-and-%C3%AE-irradiation
#6
E Zulato, F Ciccarese, V Agnusdei, M Pinazza, G Nardo, E Iorio, M Curtarello, M Silic-Benussi, E Rossi, C Venturoli, E Panieri, M M Santoro, V Di Paolo, L Quintieri, V Ciminale, S Indraccolo
The liver kinase B1 (LKB1) gene is a tumor suppressor associated with the hereditary Peutz-Jeghers syndrome and frequently mutated in non-small cell lung cancer and in cervical cancer. Previous studies showed that the LKB1/AMPK axis is involved in regulation of cell death and survival under metabolic stress. By using isogenic pairs of cancer cell lines, we report here that the genetic loss of LKB1 was associated with increased intracellular levels of total choline containing metabolites and, under oxidative stress, it impaired maintenance of glutathione (GSH) levels...
September 14, 2018: Biochemical Pharmacology
https://www.readbyqxmd.com/read/30222966/specific-tissue-factor-delivery-using-a-tumor-homing-peptide-for-inducing-tumor-infarction
#7
Quanwei Shi, Yinlong Zhang, Shaoli Liu, Guangna Liu, Junchao Xu, Xiao Zhao, Gregory J Anderson, Guangjun Nie, Suping Li
Targeting the human blood coagulation-inducing protein tissue factor (TF) to the tumor vasculature to induce infarction and disrupt the blood vessels has proven to be an effective approach for tumor therapy. In this study, we investigated the thrombogenic activity and anti-tumor potential of a novel fusion protein (tTF-CREKA) comprising the extracellular domain of human tissue factor (truncated TF, tTF) and a tumor targeting pentapeptide, Cys-Arg-Glu-Lys-Ala (CREKA). tTF is soluble and inactive in its free state, but when it is targeted to the plasma membrane of both tumor vessel endothelial cells and stromal cells by the CREKA peptide, its native coagulation-inducing activity is restored...
September 14, 2018: Biochemical Pharmacology
https://www.readbyqxmd.com/read/30222965/computational-systems-biology-approach-to-identify-novel-pharmacological-targets-for-diabetic-retinopathy
#8
Chiara Bianca Maria Platania, Gian Marco Leggio, Filippo Drago, Salvatore Salomone, Claudio Bucolo
Diabetic retinopathy was included by the World Health Organization in the eye disease priority list. Up to now, only proliferative diabetic retinopathy can be treated with approved drugs such as intravitreal anti-vascular endothelial growth factor (VEGF) agents or steroids. In this perspective, there is the urgent need to explore novel pharmacological targets for treatment of diabetic retinopathy. Drug discovery todays exploits the noticeable ability of computational systems biology methods to identify novel drug targets in complex pathologies bearing multifactorial etiology and wide and varying symptomatology...
September 14, 2018: Biochemical Pharmacology
https://www.readbyqxmd.com/read/30218916/corrigendum-to-induction-of-oxidative-stress-by-long-term-treatment-of-live-hek293-cells-with-therapeutic-concentration-of-lithium-is-associated-with-down-regulation-of-%C3%AE-opioid-receptor-amount-and-function-biochem-pharmacol-154-2018-452-463
#9
Miroslava Vosahlikova, Hana Ujcikova, Martina Hlouskova, Stanislav Musil, Lenka Roubalova, Martin Alda, Petr Svoboda
No abstract text is available yet for this article.
September 12, 2018: Biochemical Pharmacology
https://www.readbyqxmd.com/read/30217571/role-of-the-efflux-transporters-bcrp-and-mrp1-in-human-placental-bio-disposition-of-pravastatin
#10
Marjan Afrouzian, Rabab Al-Lahham, Svetlana Patrikeeva, Meixiang Xu, Valentina Fokina, Wayne G Fischer, Sherif Z Abdel-Rahman, Maged Costantine, Mahmoud S Ahmed, Tatiana Nanovskaya
The expression and activity of human placental transporters during pregnancy could be altered by several factors including pathological changes associated with preeclampsia. The aims of this study were to identify the placental efflux transporters involved in the bio-disposition of pravastatin, determine the protein expression of these transporters and their encoding genes as well as the activity of pravastatin uptake in placentas obtained from patients with preeclampsia. ATP-dependent uptake of [3H]-pravastatin by trophoblast tissue apical and basal membrane vesicles exhibited sigmoidal kinetics...
September 11, 2018: Biochemical Pharmacology
https://www.readbyqxmd.com/read/30217570/role-of-the-endocannabinoid-system-in-drug-addiction
#11
REVIEW
Jorge Manzanares, David Cabañero, Nagore Puente, María S García-Gutiérrez, Pedro Grandes, Rafael Maldonado
Drug addiction is a chronic relapsing disorder that produces a dramaticglobal health burden worldwide. Not effective treatment of drug addiction is currently available probably due to the difficulties to find an appropriate target to manage this complex disease raising the needs for further identification of novel therapeutic approaches.The endocannabinoid system has been found to play a crucial role in the neurobiological substrate underlying drug addiction. Endocannabinoids and cannabinoid receptors are widely expressed in the main areas of the mesocorticolimbic system that participate in the initiation and maintenance of drug consumption and in the development of compulsion and loss of behavioral control occurring during drug addiction...
September 11, 2018: Biochemical Pharmacology
https://www.readbyqxmd.com/read/30201214/functional-characterization-of-40-cyp2b6-allelic-variants-by-assessing-efavirenz-8-hydroxylation
#12
Takashi Watanabe, Takahiro Saito, Evelyn Marie Gutiérrez Rico, Eiji Hishinuma, Masaki Kumondai, Masamitsu Maekawa, Akifumi Oda, Daisuke Saigusa, Sakae Saito, Jun Yasuda, Masao Nagasaki, Naoko Minegishi, Masayuki Yamamoto, Hiroaki Yamaguchi, Nariyasu Mano, Noriyasu Hirasawa, Masahiro Hiratsuka
Genetic variations within cytochrome P450 2B6 (CYP2B6) contribute to inter-individual variation in the metabolism of clinically important drugs, including cyclophosphamide, bupropion, methadone and efavirenz (EFZ). In this study, we performed an in vitro analysis of 40 CYP2B6 allelic variant proteins including seven novel variants identified in 1070 Japanese individuals. Wild-type and 39 variant proteins were heterologously expressed in 293FT cells to estimate the kinetic parameters (Km , Vmax , and CLint ) of EFZ 8-hydroxylation and 7-ethoxy-4-trifluoromethylcoumarin (7-ETC) O-deethylation activities...
September 8, 2018: Biochemical Pharmacology
https://www.readbyqxmd.com/read/30195733/glucagon-like-peptide-1-receptor-internalisation-controls-spatiotemporal-signalling-mediated-by-biased-agonists
#13
Madeleine M Fletcher, Michelle L Halls, Peishen Zhao, Lachlan Clydesdale, Arthur Christopoulos, Patrick M Sexton, Denise Wootten
The glucagon-like peptide-1 receptor (GLP-1R) is a major therapeutic target in the treatment of type 2 diabetes due to its roles in regulating blood glucose and in promoting weight loss. Like many GPCRs, it is pleiotropically coupled, can be activated by multiple ligands and is subject to biased agonism. The GLP-1R undergoes agonist mediated receptor internalisation that may be associated with spatiotemporal control of signalling and biased agonism, although to date, this has not been extensively explored. Here, we investigate GLP-1R trafficking and its importance with regard to signalling, including the localisation of key signalling molecules, mediated by biased peptide agonists that are either endogenous GLP-1R ligands or are used clinically...
September 7, 2018: Biochemical Pharmacology
https://www.readbyqxmd.com/read/30195732/the-activity-of-brain-and-liver-cytochrome-p450-2d-cyp2d-is-differently-affected-by-antidepressants-in-the-chronic-mild-stress-cms-model-of-depression-in-the-rat
#14
Anna Haduch, Marta Rysz, Mariusz Papp, Władysława A Daniel
The effect of two second-generation antidepressants escitalopram and venlafaxine on the activity of brain and liver cytochrome P450 2D (CYP2D) involved in the metabolism of psychotropics and neurotransmitters was determined in the chronic mild stress (CMS) model of depression. Escitalopram or venlafaxine (10 mg/kg ip/day each) were administered to control and CMS rats for 5 weeks. The activity of CYP2D was studied by measurement of the rate of bufuralol 1'-hydroxylation in microsomes derived from the liver or different brain structures...
September 7, 2018: Biochemical Pharmacology
https://www.readbyqxmd.com/read/30195730/rifampicin-ameliorates-lithium-pilocarpine-induced-seizures-consequent-hippocampal-damage-and-memory-deficit-in-rats-impact-on-oxidative-inflammatory-and-apoptotic-machineries
#15
Alaa E Ali, Heba M Mahdy, Doaa M Elsherbiny, Samar S Azab
Epilepsy is one of the serious neurological sequelae of bacterial meningitis. Rifampicin, the well-known broad spectrum antibiotic, is clinically used for chemoprophylaxis of meningitis. Besides its antibiotic effects, rifampicin has been proven to be an effective neuroprotective candidate in various experimental models of neurological diseases. In addition, rifampicin was found to have promising antioxidant, anti-inflammatory and anti-apoptotic effects. Herein, we investigated the anticonvulsant effect of rifampicin at experimental meningitis dose (20 mg/kg, i...
September 7, 2018: Biochemical Pharmacology
https://www.readbyqxmd.com/read/30195736/targeting-glioma-initiating-cells-with-a-combined-therapy-of-cannabinoids-and-temozolomide
#16
Israel López-Valero, Cristina Sáiz-Ladera, Sofía Torres, Sonia Hernández Tiedra, Elena García-Taboada, Fátima Rodríguez-Fornés, Marina Barba, David Dávila de León, Nélida Salvador-Tormo, Manuel Guzmán, Juan M Sepúlveda, Pilar Sánchez, Mar Lorente, Guillermo Velasco
Glioblastoma multiforme (GBM) is the most frequent and aggressive type of brain tumor due, at least in part, to its poor response to current anticancer treatments. These features could be explained, at least partially, by the presence within the tumor mass of a small population of cells termed Glioma Initiating Cells (GICs) that has been proposed to be responsible for the relapses occurring in this disease. Thus, the development of novel therapeutic approaches (and specifically those targeting the population of GICs) is urgently needed to improve the survival of the patients suffering this devastating disease...
September 6, 2018: Biochemical Pharmacology
https://www.readbyqxmd.com/read/30195735/ppar%C3%AE-cb1-receptor-dual-ligands-as-a-novel-therapy-for-alcohol-use-disorder-evaluation-of-a-novel-oleic-acid-conjugate-in-preclinical-rat-models
#17
Francisco Alen, Juan Decara, Gloria Brunori, Zhi-Bing You, Kora-Mareen Bühler, Jose Antonio López-Moreno, Andrea Cippitelli, Francisco Javier Pavon, Juan Suárez, Eliot L Gardner, Rafael de la Torre, Roberto Ciccocioppo, Antonia Serrano, Fernando Rodríguez de Fonseca
Recent studies have demonstrated the utility of drugs modulating the endogenous cannabinoid system to control excessive alcohol intake. Among them, drugs interacting with acylethanolamide receptors including cannabinoid CB1 receptor antagonists/inverse agonists, peroxisome proliferator-activated receptor alpha (PPARα) agonists or peroxisome proliferator-activated receptor gamma (PPARγ) agonists have demonstrated utility in the reduction of alcohol intake in animal models. However, few studies have addressed the potential utility of combining these classes of drugs, especially because of expected safety problems...
September 6, 2018: Biochemical Pharmacology
https://www.readbyqxmd.com/read/30195734/the-endocannabinoid-2-arachidonoylglycerol-regulates-oligodendrocyte-progenitor-cell-migration
#18
Maria A Sanchez-Rodriguez, Oscar Gomez, Pedro F Esteban, Daniel Garcia-Ovejero, Eduardo Molina-Holgado
While the endocannabinoid 2-arachidonoylglycerol (2-AG) is thought to enhance the proliferation and differentiation of oligodendrocyte progenitor cells (OPCs) in vitro, less is known about how endogenous 2-AG may influence the migration of these cells. When we assessed this in Agarose drop and Boyden chemotaxis chamber assays, inhibiting the sn-1-diacylglycerol lipases α and β (DAGLs) that are responsible for 2-AG synthesis significantly reduced the migration of OPCs stimulated by platelet-derived growth factor-AA (PDGF) and basic fibroblast growth factor (FGF)...
September 6, 2018: Biochemical Pharmacology
https://www.readbyqxmd.com/read/30195731/smiglaside-a-ameliorates-lps-induced-acute-lung-injury-by-modulating-macrophage-polarization-via-ampk-ppar%C3%AE-pathway
#19
Yurong Wang, Yuan Xu, Pingping Zhang, Wenchen Ruan, Luyong Zhang, Shengtao Yuan, Tao Pang, Ai-Qun Jia
Macrophages, which have various phenotypes and diverse functions, are becoming the target cells in inflammatory diseases. In this study, we evaluated the effects of the natural product smiglaside A, a phenylpropanoid glycoside isolated from the traditional Chinese medicinal herb Smilax riparia, on macrophage polarization and investigated the underlying mechanisms. We found that smiglaside A promoted M2 polarization and reduced M1 polarization in LPS-stimulated RAW264.7 cells and primary mouse peritoneal macrophages...
September 6, 2018: Biochemical Pharmacology
https://www.readbyqxmd.com/read/30195729/role-of-interleukin-1-beta-in-the-inflammatory-response-in-a-fatty-acid-amide-hydrolase-knockout-mouse-model-of-alzheimer-s-disease
#20
Noelia Aparicio, M Teresa Grande, Samuel Ruiz de Martín Esteban, Alicia López, Gonzalo Ruiz-Pérez, Mario Amores, Carmen Vázquez, Ana M Martínez-Relimpio, M Ruth Pazos, Benjamin F Cravatt, Rosa M Tolón, Julián Romero
The search for novel therapies for the treatment of Alzheimer's disease is an urgent need, due to the current paucity of available pharmacological tools and the recent failures obtained in clinical trials. Among other strategies, the modulation of amyloid-triggered neuroinflammation by the endocannabinoid system seems of relevance. Previous data indicate that the enhancement of the endocannabinoid tone through the inhibition of the enzymes responsible for the degradation of their main endogenous ligands may render beneficial effects...
September 6, 2018: Biochemical Pharmacology
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