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Prenylation

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https://www.readbyqxmd.com/read/29140585/timap-the-versatile-protein-phosphatase-1-regulator-in-endothelial-cells
#1
REVIEW
Anita Boratkó, Csilla Csortos
Transforming growth factor (TGF)-β inhibited membrane associated protein, TIMAP, is the member of the myosin phosphatase targeting protein (MYPT) family of protein phosphatase 1 (PP1) regulatory subunits. The N-terminal part of TIMAP has a typical MYPT family structure with a sequence element called MyPhone (myosin phosphatase N-terminal element), a putative bipartite nuclear localization signal, a PP1 catalytic subunit binding motif, and five ankyrin repeats. The C-terminal half of TIMAP is intrinsically disordered, but ends with a functional CAAX box for lipid modification which allows localization of TIMAP at the plasma membrane...
November 15, 2017: IUBMB Life
https://www.readbyqxmd.com/read/29140457/genistein-specific-g6dt-gene-for-the-inducible-production-of-wighteone-in-lotus-japonicus
#2
Jinyue Liu, Wenbo Jiang, Yaying Xia, Xuemin Wang, Guoan Shen, Yongzhen Pang
Prenylated isoflavonoids were found in several legume plants, and they possess various biological activities that play important roles in both plant defense and human health. However, it is still unknown whether prenylated isoflavonoids are present in the model legume plant L. japonicus. In the present study, we found that the prenylated isoflavonoid wighteone was produced in L. japonicus when the leaf was supplemented with genistein. Furthermore, a novel prenyltransferase gene LjG6DT was identified, which shared high similarity and was closely related with several known prenyltransferase genes involved in isoflavonoid biosynthesis...
November 10, 2017: Plant & Cell Physiology
https://www.readbyqxmd.com/read/29133041/design-synthesis-and-biological-evaluation-of-novel-aryldiketo-acids-with-enhanced-antibacterial-activity-against-multidrug-resistant-bacterial-strains
#3
Ilija N Cvijetić, Tatjana Ž Verbić, Pedro Ernesto de Resende, Paul Stapleton, Simon Gibbons, Ivan O Juranić, Branko J Drakulić, Mire Zloh
Antimicrobial resistance (AMR) is a major health problem worldwide, because of ability of bacteria, fungi and viruses to evade known therapeutic agents used in treatment of infections. Aryldiketo acids (ADK) have shown antimicrobial activity against several resistant strains including Gram-positive Staphylococcus aureus bacteria. Our previous studies revealed that ADK analogues having bulky alkyl group in ortho position on a phenyl ring have up to ten times better activity than norfloxacin against the same strains...
November 10, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29123952/mevalonate-metabolism-governs-cancer-immune-surveillance
#4
REVIEW
Georg Gruenbacher, Martin Thurnher
The metabolic reprogramming that drives immunity engages the mevalonate pathway for cholesterol biosynthesis and protein prenylation. The importance of tight regulation of this metabolic route is reflected by the fact that too low activity impairs cellular function and survival, whereas hyperactivity can lead to malignant transformation. Here, we first address how mevalonate metabolism drives immunity and then highlight ways of the immune system to respond to both, limited and uncontrolled flux through the mevalonate pathway...
2017: Oncoimmunology
https://www.readbyqxmd.com/read/29122977/a%C3%AE-inhibits-srebp-2-activation-through-akt-inhibition
#5
Amany Mohamed, Anissa Viveiros, Kathleen Williams, Elena Posse de Chaves
We previously demonstrated that oligomeric Aβ42 (oAβ42 ) inhibits the mevalonate pathway impairing cholesterol synthesis and protein prenylation. Enzymes of the mevalonate pathway are regulated by the transcription factor sterol regulatory element binding protein (SREBP) 2. Here, we show that in several neuronal types challenged with o Aβ42, SREBP-2 activation is reduced. Moreover, SREBP-2 activation is also decreased in brain cortex of the Alzheimer's disease (AD) mouse model TgCRND8, suggesting that SREBP-2 may be affected in vivo during disease...
November 9, 2017: Journal of Lipid Research
https://www.readbyqxmd.com/read/29121426/xanthohumol-inhibits-angiogenesis-by-suppressing-nuclear-factor-%C3%AE%C2%BAb-activation-in-pancreatic-cancer
#6
Kenta Saito, Yoichi Matsuo, Hiroyuki Imafuji, Tomotaka Okubo, Yuzo Maeda, Takafumi Sato, Tomoya Shamoto, Ken Tsuboi, Mamoru Morimoto, Hiroki Takahashi, Hideyuki Ishiguro, Shuji Takiguchi
Xantohumol, a prenylated chalcone from hops (Humulus lupulus L.), has been shown to inhibit proliferation in some cancers. However, little is known regarding the effects of xanthohumol in pancreatic cancer. We have previously reported that activation of the transcription factor nuclear factor-κB (NF-κB) plays a key role in angiogenesis in pancreatic cancer. In this study, we investigated whether xanthohumol inhibited angiogenesis by blocking NF-κB activation in pancreatic cancer in vitro and in vivo. We initially confirmed that xanthohumol significantly inhibited proliferation and NF-κB activation in pancreatic cancer cell lines...
November 9, 2017: Cancer Science
https://www.readbyqxmd.com/read/29112138/cytotoxic-and-antibacterial-compounds-from-the-coral-derived-fungus-aspergillus-tritici-sp2-8-1
#7
Weiyi Wang, Yanyan Liao, Chao Tang, Xiaomei Huang, Zhuhua Luo, Jianming Chen, Peng Cai
Three novel compounds, 4-methyl-candidusin A (1), aspetritone A (2) and aspetritone B (3), were obtained from the culture of a coral-derived fungus Aspergillus tritici SP2-8-1, together with fifteen known compounds (4-18). Their structures, including absolute configurations, were assigned based on NMR, MS, and time-dependent density functional theory (TD-DFT) ECD calculations. Compounds 2 and 5 exhibited better activities against methicillin-resistant strains of S. aureus (MRSA) ATCC 43300 and MRSA CGMCC 1...
November 7, 2017: Marine Drugs
https://www.readbyqxmd.com/read/29110479/synthesis-of-a-nonracemic-c2-symmetric-tetrahydro-1-4-azaborine-and-evaluation-of-hydroboration-enantioselectivity
#8
Robert-André F Rarig, John M Nelson, Edwin Vedejs
Tetrahydro-1,4-azaborines were accessed by hydroboration of N,N-di-prenyl-toluenesulfonamide 4. Conversion to the methylborinates 11 and 12 followed by heating with l alanine and crystallization afforded (R,R,S)-13 (27%). Hydrolysis to borinic acid (R,R) 18 and reduction with Soderquist's KH* gave the C2-symmetric borohydride (R,R) 19. Subsequent hydride abstraction by TMSCl in the presence of simple alkenes resulted in hydroboration. Promising enantioselectivity was seen with Z alkenes (84-86% ee, RT), but not with E alkenes or 1,1-disubstituted alkenes (<5% ee)...
November 7, 2017: Journal of Organic Chemistry
https://www.readbyqxmd.com/read/29110063/the-effect-of-icariin-on-bone-metabolism-and-its-potential-clinical-application
#9
REVIEW
Z Wang, D Wang, D Yang, W Zhen, J Zhang, S Peng
Osteoporosis is a bone disease characterized by reduced bone mass, which leads to increased risk of bone fractures, and poses a significant risk to public health, especially in the elderly population. The traditional Chinese medicinal herb Epimedii has been utilized for centuries to treat bone fracture and bone loss. Icariin is a prenylated flavonol glycoside isolated from Epimedium herb, and has been shown to be the main bioactive component. This review provides a comprehensive survey of previous studies on icariin, including its structure and function, effect on bone metabolism, and potential for clinical application...
November 6, 2017: Osteoporosis International
https://www.readbyqxmd.com/read/29089388/the-flavonol-glycoside-icariin-promotes-bone-formation-in-growing-rats-by-activating-the-camp-signaling-pathway-in-primary-cilia-of-osteoblasts
#10
Wengui Shi, Yuhai Gao, Yuanyuan Wang, Jian Zhou, Zhenlong Wei, Xiaoni Ma, Huiping Ma, Cory J Xian, Jufang Wang, Keming Chen
Icariin, a prenylated flavonol glycoside isolated from the herb Epimedium, has been considered as a potential alternative therapy for osteoporosis. Previous research has shown that unlike other flavonoids, icariin is unlikely to act via the estrogen receptor, but its exact mechanism of action is unknown. In this study, using rat calvarial osteoblast culture and rat bone growth models, we demonstrated that icariin promotes bone formation by activating the cAMP/protein kinase A (PKA)/cAMP response element-binding protein (CREB) pathway requiring functional primary cilia of osteoblasts...
October 31, 2017: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/29072465/two-prenyltransferases-govern-a-consecutive-prenylation-cascade-in-the-biosynthesis-of-echinulin-and-neoechinulin
#11
Viola Wohlgemuth, Florian Kindinger, Xiulan Xie, Bin-Gui Wang, Shu-Ming Li
Two prenyltransferases from Aspergillus ruber control the echinulin biosynthesis via exceptional sequential prenylations. EchPT1 catalyzes the first prenylation step, leading to preechinulin. The unique EchPT2 attaches, in a consecutive prenylation cascade, up to three dimethylallyl moieties to preechinulin and its dehydro forms neoechinulins A and B, resulting in the formation of at least 23 2- to 4-fold prenylated derivatives. Confirming these products in fungal extracts unravels the unprecedented catalytic relevance of EchPT2 for structural diversity...
October 26, 2017: Organic Letters
https://www.readbyqxmd.com/read/29057264/icariin-attenuates-synaptic-and-cognitive-deficits-in-an-a%C3%AE-1-42-induced-rat-model-of-alzheimer-s-disease
#12
Chenxia Sheng, Panpan Xu, Kexin Zhou, Dan Deng, Chunhu Zhang, Zhe Wang
Icariin (ICA), a prenylated flavanol glycoside present in abundant quantities in Epimedium sagittatum, has shown promise in the treatment and prevention of Alzheimer's disease. Damage to synaptic plasticity induced by amyloid-beta-mediated neurotoxicity is considered a main pathological mechanism driving the learning and memory deficits present in patients with Alzheimer's disease. This study investigated the neuroprotective effects of icariin in an Aβ1-42-induced rat model of Alzheimer's disease. Our results showed that Aβ1-42 injection induced loss of learning and memory behaviour in the Morris water maze, which could be reversed with intragastric administration of ICA...
2017: BioMed Research International
https://www.readbyqxmd.com/read/29055178/n-acetylborrelidin-b-a-new-bioactive-metabolite-from-streptomyces-mutabilis-sp-mii
#13
Abdelaaty Hamed, Ahmed S Abdel-Razek, Marcel Frese, Daniel Wibberg, Atef F El-Haddad, Tarek M A Ibrahim, Jörn Kalinowski, Norbert Sewald, Mohamed Shaaban
In the course of our screening program for new bioactive compounds, a naturally new 18-membered macrolide antibiotic, N-acetylborrelidin B (1) along with borrelidin (2) were obtained from the marine Streptomyces mutabilis sp. MII. The strain was isolated from a sediment sample collected in the Red Sea at the Hurghada Coast and characterized taxonomically. Additional nine diverse bioactive compounds were reported: 6-prenyl-indole-3-acetonitrile (3), sitosteryl-3β-d-glucoside, campesterol, ferulic acid, linoleic acid methyl ester, linoleic acid, N-acetylanthranilic acid, indole 3-acetic acid methyl ester, indole 3-carboxylic acid, and adenosine...
October 21, 2017: Zeitschrift Für Naturforschung. C, A Journal of Biosciences
https://www.readbyqxmd.com/read/29039247/high-throughput-in-silico-identification-and-characterization-of-plasmodium-falciparum-prl-phosphatase-inhibitors
#14
Rajan Pandey, Rakesh Kumar, Priya Gupta, Asif Mohmmed, Rita Tewari, Pawan Malhotra, Dinesh Gupta
Kinases and phosphatases are involved in many essential processes in Plasmodium life cycle. Among the identified 67 Plasmodium falciparum phosphatases, Phosphatase of Regenerating Liver (PRL) family protein homolog, PfPRL is an essential parasite tyrosine phosphatase. PfPRL is shown to be prenylated, secreted and involved in the host invasion process. In the present study, a structure based high throughput in-silico screening of PfPRL binders, using ChEMBL-NTD compounds lead to the identification of nine compounds based on binding energy, Lipinski rule of five and QED score...
October 17, 2017: Journal of Biomolecular Structure & Dynamics
https://www.readbyqxmd.com/read/29037945/enantioselective-inhibitory-abilities-of-enantiomers-of-notoamides-against-rankl-induced-formation-of-multinuclear-osteoclasts
#15
Hikaru Kato, Aika Kai, Tetsuro Kawabata, James D Sunderhaus, Timothy J McAfoos, Jennifer M Finefield, Yukihiko Sugimoto, Robert M Williams, Sachiko Tsukamoto
The marine-derived Aspergillus protuberus MF297-2 and the terrestrial A. amoenus NRRL 35600 produce enantiomeric prenylated indole alkaloids. Investigation of biological activities of the natural and synthetic derivatives revealed that (-)-enantiomers of notoamides A and B, 6-epi-notoamide T, and stephacidin A inhibited receptor activator of nuclear factor-κB (NF-κB) ligand (RANKL)-induced osteoclastogenic differentiation of murine RAW264 cells more strongly than their respective (+)-enantiomers. Among them, (-)-6-epi-notoamide T was the most potent inhibitor with an IC50 value of 1...
November 15, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/29030460/hmg-coa-reductase-inhibition-delays-dna-repair-and-promotes-senescence-after-tumor-irradiation
#16
Elena V Efimova, Natalia Ricco, Edwardine Labay, Helena J Mauceri, Amy C Flor, Aishwarya Ramamurthy, Harold G Sutton, Ralph R Weichselbaum, Stephen J Kron
Despite significant advances in combinations of radiotherapy and chemotherapy, altered fractionation schedules and image-guided radiotherapy, many cancer patients fail to benefit from radiation. A prevailing hypothesis is that targeting repair of DNA double strand breaks (DSBs) can enhance radiation effects in the tumor and overcome therapeutic resistance without incurring off-target toxicities. Unrepaired DSBs can block cancer cell proliferation, promote cancer cell death and induce cellular senescence. Given the slow progress to date translating novel DSB repair inhibitors as radiosensitizers, we have explored drug repurposing, a proven route to improving speed, costs and success rates of drug development...
October 13, 2017: Molecular Cancer Therapeutics
https://www.readbyqxmd.com/read/29027991/n6-isopentenyladenosine-dual-targeting-of-ampk-and-rab7-prenylation-inhibits-melanoma-growth-through-the-impairment-of-autophagic-flux
#17
Roberta Ranieri, Elena Ciaglia, Giuseppina Amodio, Paola Picardi, Maria Chiara Proto, Patrizia Gazzerro, Chiara Laezza, Paolo Remondelli, Maurizio Bifulco, Simona Pisanti
Targeting the autophagic process is considered a promising therapeutic strategy in cancer since a great number of tumors, including melanoma, show high basal levels of protective autophagy that contributes to tumor progression and chemoresistance. Here, exploiting both in vitro and in vivo approaches, we identified N6-isopentenyladenosine (iPA), an end product of the mevalonate pathway, as a novel autophagy inhibitor with an interesting anti-melanoma activity. iPA, after being phosphorylated by adenosine kinase into 5'-iPA-monophosphate, induces autophagosome accumulation through AMPK activation, measured by increased fluorescent GFP-LC3 puncta and enhanced conversion into the lipidated autophagosome-associated LC3-II...
October 13, 2017: Cell Death and Differentiation
https://www.readbyqxmd.com/read/29024217/use-of-the-target-of-rapamycin-fatc-domain-as-a-general-membrane-anchor-the-fkbp-12-like-domain-of-fkbp38-as-a-case-study
#18
Maristella De Cicco, Lech-G Milroy, Sonja A Dames
Increased efforts have been undertaken to better understand the formation of signaling complexes at cellular membranes. Since the preparation of proteins containing a transmembrane domain or a prenylation motif is generally challenging an alternative membrane anchoring unit that is easy to attach, water-soluble and binds to different membrane mimetics would find broad application. The 33-residue long FATC domain of yeast TOR1 (y1fatc) fulfills these criteria and binds to neutral and negatively charged micelles, bicelles and liposomes...
October 12, 2017: Protein Science: a Publication of the Protein Society
https://www.readbyqxmd.com/read/28993794/antitrypanosomal-and-antileishmanial-activity-of-prenyl-1-2-3-triazoles
#19
Exequiel O J Porta, Sebastián N Jäger, Isabel Nocito, Galina I Lepesheva, Esteban C Serra, Babu L Tekwani, Guillermo R Labadie
A series of prenyl 1,2,3-triazoles were prepared from isoprenyl azides and different alkynes. The dipolar cycloaddition reaction provided exclusively primary azide products as regioisomeric mixtures that were separated by column chromatography and fully characterized. Most of the compounds displayed antiparasitic activity against Trypanosoma cruzi and Leishmania donovani. The most active compounds were assayed as potential TcCYP51 inhibitors.
May 1, 2017: MedChemComm
https://www.readbyqxmd.com/read/28990465/statins-induce-apoptosis-through-inhibition-of-ras-signaling-pathways-and-enhancement-of-bim-and-p27-expression-in-human-hematopoietic-tumor-cells
#20
Daichiro Fujiwara, Masanobu Tsubaki, Tomoya Takeda, Yoshika Tomonari, Yu-Ichi Koumoto, Katsuhiko Sakaguchi, Shozo Nishida
Recently, statins have been demonstrated to improve cancer-related mortality or prognosis in patients of various cancers. However, the details of the apoptosis-inducing mechanisms remain unknown. This study showed that the induction of apoptosis by statins in hematopoietic tumor cells is mediated by mitochondrial apoptotic signaling pathways, which are activated by the suppression of mevalonate or geranylgeranyl pyrophosphate biosynthesis. In addition, statins decreased the levels of phosphorylated extracellular signal-regulated kinase 1/2 and mammalian target of rapamycin through suppressing Ras prenylation...
October 2017: Tumour Biology: the Journal of the International Society for Oncodevelopmental Biology and Medicine
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