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https://www.readbyqxmd.com/read/28514875/identification-of-novel-nicotinamide-phosphoribosyltransferase-nampt-inhibitors-using-computational-approaches
#1
Manish Kesherwani, Sriram Raghavan, Krishnasamy Gunasekaran, Devadasan Velmurugan
Nicotinamide Phosphoribosyltransferase (NAMPT) is a rate-limiting enzyme in the biosynthesis of NAD. Cancer cells have elevated poly [ADP-Ribose] polymerase 1 (PARP) activity as well as the immense necessity of ATP: thereby consuming NAD at a higher rate than normal tissues. The perturbation of these intracellular processes is more sensitive and highly dependent on NAMPT to maintain the required NAD levels. Functional inhibition of NAMPT is, therefore, a promising drug target in therapeutic oncology. In this study, the importance of intermolecular contacts was realized based on contact occupancy and favorable energetic from molecular dynamic simulation to discern non-critical contacts of four different classes of potential NAMPT inhibitor bound complexes...
May 17, 2017: Journal of Biomolecular Structure & Dynamics
https://www.readbyqxmd.com/read/28507103/nicotinic-acid-phosphoribosyltransferase-regulates-cancer-cell-metabolism-susceptibility-to-nampt-inhibitors-and-dna-repair
#2
Francesco Piacente, Irene Caffa, Silvia Ravera, Giovanna Sociali, Mario Passalacqua, Valerio G Vellone, Pamela Becherini, Daniele Reverberi, Fiammetta Monacelli, Alberto Ballestrero, Patrizio Odetti, Antonia Cagnetta, Michele Cea, Aimable Nahimana, Michel A Duchosal, Santina Bruzzone, Alessio Nencioni
In the last decade, substantial efforts have been made to identify NAD+ biosynthesis inhibitors, specifically against nicotinamide phosphoribosyltransferase (NAMPT), as preclinical studies indicate their potential efficacy as cancer drugs. However, the clinical activity of NAMPT inhibitors has proven limited, suggesting that alternative NAD+ production routes exploited by tumors confer resistance. Here we show the gene encoding nicotinic acid phosphoribosyltransferase (NAPRT), a second NAD+ producing enzyme, is amplified and overexpressed in a subset of common types of cancer, including ovarian cancer, where NAPRT expression correlates with a BRCAness gene expression signature...
May 15, 2017: Cancer Research
https://www.readbyqxmd.com/read/28501332/inhibition-of-nicotinamide-phosphoribosyltransferase-and-depletion-of-nicotinamide-adenine-dinucleotide-contribute-to-arsenic-trioxide-suppression-of-oral-squamous-cell-carcinoma
#3
Xin Yue Wang, Jin Zhi Wang, Lu Gao, Fu Yin Zhang, Qi Wang, Ke Jian Liu, Bin Xiang
Emerging evidence suggests that increased nicotinamide phosphoribosyltransferase (NAMPT) expression is associated with the development and prognosis of many cancers, but it remains unknown regarding its role in oral squamous cell carcinoma (OSCC). In the present study, the results from tissue microarray showed that NAMPT was overexpressed in OSCC patients and its expression level was directly correlated with differential grades of cancer. Interestingly, treatment of OSCC cells with chemotherapy agent arsenic trioxide (ATO) decreased the levels of NAMPT protein and increased cellular death in an ATO dose- and time-dependent manner...
May 10, 2017: Toxicology and Applied Pharmacology
https://www.readbyqxmd.com/read/28482725/umbilical-cord-blood-and-maternal-visfatin-pbef-nampt-concentrations-in-preterm-birth-with-and-without-preterm-premature-rupture-of-membranes
#4
Tereza Pavlová, Filip Zlámal, Zbyněk Šplíchal, Josef Tomandl, Zuzana Hodická, Pavel Ventruba, Julie Bienertová-Vašků
OBJECTIVES: The aim of the study is to investigate differences in visfatin concentrations between mothers with term and preterm birth (PTB) and between mothers who delivered within 7 days and after more than 7 days following admission for PTB/preterm premature rupture of membranes (PPROM). METHODS: Maternal peripheral blood and cord blood was collected from 56 mothers with PTB (31 with PPROM) and 71 mothers with term delivery (3 with PPROM). RESULTS: Maternal visfatin concentration was significantly higher for given gestational age in PTBs compared to term deliveries (p = 0...
May 9, 2017: Journal of Maternal-fetal & Neonatal Medicine
https://www.readbyqxmd.com/read/28478801/involvement-of-trpc1-in-nampt-induced-cardiomyocyte-hypertrophy-through-the-activation-of-er-stress
#5
J Li, W Wu, M Zhao, X Liu
Nicotinamide phosphoribosyltransferase (Nampt) is involved in the development of cardiac hypertrophy. Transient receptor potential canonical channel 1 (TRPC1) and endoplasmic reticulum stress (ER stress) are regarded as critical pathways in cardiac hypertrophy. Therefore, we hypothesizedthat TRPC1 might be associated with ER stress in Nampt-induced cardiac hypertrophy. CulturedH9c2cardiomyocyteswereexposed to Namptfor different timesand the expression of markers of cardiomyocyte hypertrophy and ER stress, as well as TRPC1 were detected...
April 29, 2017: Cellular and Molecular Biology
https://www.readbyqxmd.com/read/28468779/discovery-and-characterization-of-novel-non-substrate-and-substrate-nampt-inhibitors
#6
Julie L Wilsbacher, Min Cheng, Dong Cheng, Samuel A J Trammell, Yan Shi, Jun Guo, Stormy L Koeniger, Peter J Kovar, Yupeng He, Sujatha Selvaraju, H Robin Heyman, Bryan K Sorensen, Richard F Clark, T Matthew Hansen, Kenton L Longenecker, Diana Raich, Alla V Korepanova, Steven Cepa, Danli L Towne, Vivek C Abraham, Hua Tang, Paul L Richardson, Shaun M McLoughlin, Ilaria Badagnani, Michael L Curtin, Michael R Michaelides, David Maag, F Greg Buchanan, Gary G Chiang, Wenqing Gao, Saul H Rosenberg, Charles Brenner, Chris Tse
Cancer cells are highly reliant on nicotinamide adenine dinucleotide (NAD(+))-dependent processes including glucose metabolism, calcium signaling, DNA repair, and regulation of gene expression. Nicotinamide phosphoribosyltransferase (NAMPT), the rate-limiting enzyme for NAD(+) salvage from nicotinamide (NAM), has been investigated as a target for anti-cancer therapy. Known NAMPT inhibitors with potent cell activity are composed of a nitrogen-containing aromatic group, which is phosphoribosylated by the enzyme...
May 3, 2017: Molecular Cancer Therapeutics
https://www.readbyqxmd.com/read/28449683/inhibition-of-nampt-aggravates-high-fat-diet-induced-hepatic-steatosis-in-mice-through-regulating-sirt1-ampk%C3%AE-srebp1-signaling-pathway
#7
Ling-Fang Wang, Xiao-Nv Wang, Cong-Cong Huang, Long Hu, Yun-Fei Xiao, Xiao-Hui Guan, Yi-Song Qian, Ke-Yu Deng, Hong-Bo Xin
BACKGROUND: Nonalcoholic fatty liver disease is one of the most common liver diseases in the world and is a typical hepatic manifestation of metabolic syndrome which is characterized with lipid accumulation in liver. Nicotinamide phosphoribosyltransferase (NAMPT) has been recently identified as an enzyme involved in nicotinamide adenine dinucleotide (NAD(+)) biosynthesis and plays an important role in cellular metabolism in variety of organs in mammals. The aim of this study was to investigate the effects of NAMPT on high fat diet-induced hepatic steatosis...
April 27, 2017: Lipids in Health and Disease
https://www.readbyqxmd.com/read/28442350/extracellular-nampt-visfatin-induces-proliferation-through-erk1-2-and-akt-and-inhibits-apoptosis-in-breast-cancer-cells
#8
Zafar Gholinejad, Nejat Kheiripour, Mitra Nourbakhsh, Davod Ilbeigi, Kiarash Behroozfar, Zahra Hesari, Abolfazl Golestani, Mohammad Shabani, Nahid Einollahi
BACKGROUND: Visfatin is a novel adipokine and proinflammatory cytokine which is implicated in breast cancer progression. The exact proliferative and anti-apoptotic mechanisms of visfatin are still under debate. In this study, the effect of extracellular visfatin on proliferation and apoptosis of breast cancer cells were investigated considering key regulatory molecules in these procedures. METHODS: BrdU (Bromodeoxyuridine) experiment was used to assess cell proliferation in response to visfatin treatment...
April 23, 2017: Peptides
https://www.readbyqxmd.com/read/28438162/targeting-of-nicotinamide-phosphoribosyltransferase-enzymatic-activity-ameliorates-lung-damage-induced-by-ischemia-reperfusion-in-rats
#9
Geng-Chin Wu, Wen-I Liao, Shu-Yu Wu, Hsin-Ping Pao, Shih-En Tang, Min-Hui Li, Kun-Lun Huang, Shi-Jye Chu
BACKGROUND: Emerging evidence reveals that nicotinamide phosphoribosyltransferase (NAMPT) has a significant role in the pathophysiology of the inflammatory process. NAMPT inhibition has a beneficial effect in the treatment of a variety of inflammatory diseases. However, it remains unclear whether NAMPT inhibition has an impact on ischemia-reperfusion (I/R)-induced acute lung injury. In this study, we examined whether NAMPT inhibition provided protection against I/R lung injury in rats...
April 24, 2017: Respiratory Research
https://www.readbyqxmd.com/read/28435063/regulation-of-nampt-expression-by-transcriptional-coactivator-ncoa6-in-pancreatic-%C3%AE-cells
#10
Jin Yoon, Kyung Jin Lee, Gyun-Sik Oh, Geun Hyang Kim, Seung-Whan Kim
Nuclear receptor coactivator 6 (NCOA6) is a transcriptional coactivator and crucial for insulin secretion and glucose metabolism in pancreatic β-cells. However, the regulatory mechanism of β-cell function by NCOA6 is largely unknown. In this study, we found that the transcript levels of nicotinamide phosphoribosyltransferase (Nampt) were decreased in islets of NCOA6(+/-) mice compared with NCOA6(+/+) mice. Moreover, NCOA6 overexpression increased the levels of Nampt transcripts in the mouse pancreatic β-cell line NIT-1...
April 20, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/28424540/mc-ppea-as-a-new-and-more-potent-inhibitor-of-clp-induced-sepsis-and-pulmonary-inflammation-than-fk866
#11
Peixin Huang, Mark W Lee, Keivan Sadrerafi, Daniel P Heruth, Li Q Zhang, Dev Maulik, Shui Qing Ye
Our previous study indicated that overexpression of nicotinamide phosphoribosyltransferase (NAMPT) aggravated acute lung injury, while knockdown of NAMPT expression attenuated ventilator-induced lung injury. Recently, we found that meta-carborane-butyl-3-(3-pyridinyl)-2E-propenamide (MC-PPEA, MC4), in which the benzoylpiperidine moiety of FK866 has been replaced by a carborane, displayed a 100-fold increase in NAMPT inhibition over FK866. Here, we determined the effects of MC4 and FK866 on cecal ligation and puncture (CLP) surgery-induced sepsis in C57BL/6J mice...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28416276/synthesis-and-degradation-of-adenosine-5-tetraphosphate-by-nicotinamide-and-nicotinate-phosphoribosyltransferases
#12
Adolfo Amici, Ambra A Grolla, Erika Del Grosso, Roberta Bellini, Michele Bianchi, Cristina Travelli, Silvia Garavaglia, Leonardo Sorci, Nadia Raffaelli, Silverio Ruggieri, Armando A Genazzani, Giuseppe Orsomando
Adenosine 5'-tetraphosphate (Ap4) is a ubiquitous metabolite involved in cell signaling in mammals. Its full physiological significance remains unknown. Here we show that two enzymes committed to NAD biosynthesis, nicotinamide phosphoribosyltransferase (NAMPT) and nicotinate phosphoribosyltransferase (NAPT), can both catalyze the synthesis and degradation of Ap4 through their facultative ATPase activity. We propose a mechanism for this unforeseen additional reaction, and demonstrate its evolutionary conservation in bacterial orthologs of mammalian NAMPT and NAPT...
May 18, 2017: Cell Chemical Biology
https://www.readbyqxmd.com/read/28408371/leukocyte-overexpression-of-intracellular-nampt-attenuates-atherosclerosis-by-regulating-ppar%C3%AE-dependent-monocyte-differentiation-and-function
#13
Beatriz Bermudez, Tuva B Dahl, Indira Medina, Mathijs Groeneweg, Sverre Holm, Sergio Montserrat-de la Paz, Mat Rousch, Jeroen J T Otten, Veronica Herias, Lourdes M Varela, Trine Ranheim, Arne Yndestad, Almudena Ortega-Gomez, Rocio Abia, Laszlo Nagy, Pal Aukrust, Francisco J G Muriana, Bente Halvorsen, Erik A L Biessen
OBJECTIVE: Extracellular nicotinamide phosphoribosyltransferase (eNAMPT) mediates inflammatory and potentially proatherogenic effects, whereas the role of intracellular NAMPT (iNAMPT), the rate limiting enzyme in the salvage pathway of nicotinamide adenine dinucleotide (NAD)(+) generation, in atherogenesis is largely unknown. Here we investigated the effects of iNAMPT overexpression in leukocytes on inflammation and atherosclerosis. APPROACH AND RESULTS: Low-density lipoprotein receptor-deficient mice with hematopoietic overexpression of human iNAMPT (iNAMPT(hi)), on a western type diet, showed attenuated plaque burden with features of lesion stabilization...
April 13, 2017: Arteriosclerosis, Thrombosis, and Vascular Biology
https://www.readbyqxmd.com/read/28382091/inhibition-of-nicotinamide-phosphoribosyltransferase-induces-apoptosis-in-estrogen-receptor-positive-mcf-7-breast-cancer-cells
#14
Mohammad Alaee, Shahnaz Khaghani, Kiarash Behroozfar, Zahra Hesari, Seyedeh Sara Ghorbanhosseini, Mitra Nourbakhsh
PURPOSE: Tumor cells have increased turnover of nicotinamide adenine dinucleotide (NAD(+)), the main coenzyme in processes including adenosine diphosphate-ribosylation, deacetylation, and calcium mobilization. NAD(+) is predominantly synthesized in human cells via the salvage pathway, with the first component being nicotinamide. Nicotinamide phosphoribosyltransferase (NAMPT) is the key enzyme in this pathway, and its chemical inhibition by FK866 has elicited antitumor effects in several preclinical models of solid and hematologic cancers...
March 2017: Journal of Breast Cancer
https://www.readbyqxmd.com/read/28370493/melatonin-administration-to-wild-type-mice-and-non-treated-nlrp3-mutant-mice-share-similar-inhibition-of-the-inflammatory-response-during-sepsis
#15
Ibtissem Rahim, Bahia Djerdjouri, Ramy K Sayed, Marisol Fernández-Ortiz, Beatriz Fernández-Gil, Agustín Hidalgo-Gutiérrez, Luis C López, Germaine Escames, Russel J Reiter, Dario Acuna-Castroviejo
The NLRP3 inflammasome is involved in the innate immune response during inflammation. Moreover, melatonin blunts the NF-κB/NLRP3 connection during sepsis. Thus, we compared the roles of the NLRP3 inflammasome and/or melatonin treatment in the septic response of wild-type and NLRP3(-/-) mice. Mouse myocardial tissue was used for this purpose. The nuclear turnover of NF-κB was enhanced during sepsis, with an increase in TNFα, iNOS, and pro-IL-1β. The lack of inflammasome in NLRP3(-/-) mice significantly reduced that response and blunted IL-1β maturation due to the lack of caspase-1...
March 31, 2017: Journal of Pineal Research
https://www.readbyqxmd.com/read/28356339/nicotinamide-phosphoribosyltransferase-in-smooth-muscle-cells-maintains-genome-integrity-resists-aortic-medial-degeneration-and-is-suppressed-in-human-thoracic-aortic-aneurysm-disease
#16
Alanna Watson, Zengxuan Nong, Hao Yin, Caroline O'Neil, Stephanie Fox, Brittany Balint, Ray Guo, Oberdan Leo, Michael W Chu, Robert Gros, J G Pickering
Rationale: The thoracic aortic wall can degenerate over time with catastrophic consequences. Vascular smooth muscle cells (SMCs) can resist and repair artery damage but their capacities decline with age and stress. Recently, cellular production of NAD(+) via nicotinamide phosphoribosyltransferase (Nampt) has emerged as a mediator of cell vitality. However, a role for Nampt in aortic SMCs in vivo is unknown. Objective: To determine if a Nampt-NAD(+) control system exists within the aortic media and is required for aortic health...
March 29, 2017: Circulation Research
https://www.readbyqxmd.com/read/28333382/regulation-and-function-of-extracellular-nicotinamide-phosphoribosyltransferase-visfatin
#17
Federico Carbone, Luca Liberale, Aldo Bonaventura, Alessandra Vecchiè, Matteo Casula, Michele Cea, Fiammetta Monacelli, Irene Caffa, Santina Bruzzone, Fabrizio Montecucco, Alessio Nencioni
Nicotinamide phosphoribosyltransferase (NAMPT) is an adipokine-enzyme, which was described as to play bioactivities both in the intracellular and in the extracellular environment. However, while the functions of intracellular NAMPT (iNAMPT) are well known, much less is known on extracellular NAMPT (eNAMPT), also called visfatin or pre-B cell colony-enhancing factor. iNAMPT catalyzes the rate-limiting step in the NAD+ biosynthesis pathway from nicotinamide. Its inhibition severely reduces intracellular NAD+ levels, achieving anti-inflammatory and anti-cancer effects...
March 16, 2017: Comprehensive Physiology
https://www.readbyqxmd.com/read/28333140/metabolic-and-molecular-insights-into-an-essential-role-of-nicotinamide-phosphoribosyltransferase
#18
Li Q Zhang, Leon Van Haandel, Min Xiong, Peixin Huang, Daniel P Heruth, Charlie Bi, Roger Gaedigk, Xun Jiang, Ding-You Li, Gerald Wyckoff, Dmitry N Grigoryev, Li Gao, Linheng Li, Min Wu, J Steven Leeder, Shui Qing Ye
Nicotinamide phosphoribosyltransferase (NAMPT) is a pleiotropic protein implicated in the pathogenesis of acute respiratory distress syndrome, aging, cancer, coronary heart diseases, diabetes, nonalcoholic fatty liver disease, obesity, rheumatoid arthritis, and sepsis. However, the underlying molecular mechanisms of NAMPT in these physiological and pathological processes are not fully understood. Here, we provide experimental evidence that a Nampt gene homozygous knockout (Nampt(-/-)) resulted in lethality at an early stage of mouse embryonic development and death within 5-10 days in adult mice accompanied by a 25...
March 23, 2017: Cell Death & Disease
https://www.readbyqxmd.com/read/28330719/nicotinamide-mononucleotide-inhibits-jnk-activation-to-reverse-alzheimer-disease
#19
Zhiwen Yao, Wenhao Yang, Zhiqiang Gao, Peng Jia
Amyloid-β (Aβ) oligomers have been accepted as major neurotoxic agents in the therapy of Alzheimer's disease (AD). It has been shown that the activity of nicotinamide adenine dinucleotide (NAD+) is related with the decline of Aβ toxicity in AD. Nicotinamide mononucleotide (NMN), the important precursor of NAD+, is produced during the reaction of nicotinamide phosphoribosyl transferase (Nampt). This study aimed to figure out the potential therapeutic effects of NMN and its underlying mechanisms in APPswe/PS1dE9 (AD-Tg) mice...
March 19, 2017: Neuroscience Letters
https://www.readbyqxmd.com/read/28322315/quantitative-proteomic-analysis-on-activated-hepatic-stellate-cells-reversion-reveal-stat1-as-a-key-regulator-between-liver-fibrosis-and-recovery
#20
Hongyu Zhang, Fangyan Chen, Xu Fan, Cong Lin, Yunwei Hao, Handong Wei, Weiran Lin, Ying Jiang, Fuchu He
Understanding the changes of activated HSCs reversion is an essential step toward clarifying the potential roles of HSCs in the treatment of liver fibrosis. In this study, we chose adipocyte differentiation mixture to induce LX-2 cells for 2 days in vitro as reversion phase, comparing with normal cultured LX-2 cells as activation phase. Mass spectrometric-based SILAC technology was adopted to study differentially expressed proteome of LX-2 cells between reversion and activation. Compared with activated HSCs, 273 proteins showed significant differences in reverted HSCs...
March 21, 2017: Scientific Reports
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