keyword
MENU ▼
Read by QxMD icon Read
search

Molecular targeting

keyword
https://www.readbyqxmd.com/read/29054115/reversible-mono-adp-ribosylation-of-dna-breaks
#1
Deeksha Munnur, Ivan Ahel
ADP-ribosylation is a chemical modification of macromolecules that plays an important role in regulation of quintessential biological processes such as DNA repair, transcription, chromatin remodelling, stress response, apoptosis, bacterial metabolism and many others. ADP-ribosylation is carried out by ADP-ribosyltransferase proteins, such as poly(ADP-ribose) polymerases (PARPs) that transfer either monomer or polymers of ADP-ribose onto the molecular targets by using nicotinamide adenine dinucleotide (NAD(+) ) as a cofactor...
October 20, 2017: FEBS Journal
https://www.readbyqxmd.com/read/29054094/runx3-inhibits-the-proliferation-and-metastasis-of-gastric-cancer-through-regulating-mir-182-hoxa9
#2
Junyan Yu, Xiangyang Tian, Jianlan Chang, Ping Liu, Rong Zhang
OBJECTIVE: This study intended to explore the molecular mechanism of RUNX3 in inhibiting the process of migration and proliferation of gastric cancer (GC) cells. METHODS: The overexpressed plasmids of RUNX3 and the interfering siRNA of RUNX3 were transfected into GC cells. Then, qRT-PCR and western blot were performed to identify the expression level of RUNX3 and miR-182 in tumors and adjacent tissues respectively. ChIP and luciferase assay were performed to detect the relationship between RUNX3 and miR-182 as well as miR-182 and HOXA9...
October 17, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29054054/conformational-analysis-of-the-human-chemokine-receptor-cxcr3
#3
Raffaele Raucci, Andrea Polo, Alfredo Budillon, Giovanni Colonna, Susan Costantini
In the last years, some studies showed the patho-genetic role of CXCR3 bound to its ligands in many human inflammatory diseases and cancers. Thus, the blockage of the CXCR3 interaction site to its ligands is seen as a possible therapeutic target for the treatment of cancer. The presence of flexible regions in the chemokine receptors determines their capability to develop specific mechanisms of action. We have recently focused on the features of the N-terminal region of human CXCR3 free in solution, where we demonstrate the presence of numerous conformational ensembles, dynamically stabilized by H-bonds...
October 17, 2017: Molecular Immunology
https://www.readbyqxmd.com/read/29053971/a-gut-microbial-mimic-that-hijacks-diabetogenic-autoreactivity-to-suppress-colitis
#4
Roopa Hebbandi Nanjundappa, Francesca Ronchi, Jinguo Wang, Xavier Clemente-Casares, Jun Yamanouchi, Channakeshava Sokke Umeshappa, Yang Yang, Jesús Blanco, Helena Bassolas-Molina, Azucena Salas, Hamza Khan, Robyn M Slattery, Madeleine Wyss, Catherine Mooser, Andrew J Macpherson, Laura K Sycuro, Pau Serra, Derek M McKay, Kathy D McCoy, Pere Santamaria
The gut microbiota contributes to the development of normal immunity but, when dysregulated, can promote autoimmunity through various non-antigen-specific effects on pathogenic and regulatory lymphocytes. Here, we show that an integrase expressed by several species of the gut microbial genus Bacteroides encodes a low-avidity mimotope of the pancreatic β cell autoantigen islet-specific glucose-6-phosphatase-catalytic-subunit-related protein (IGRP206-214). Studies in germ-free mice monocolonized with integrase-competent, integrase-deficient, and integrase-transgenic Bacteroides demonstrate that the microbial epitope promotes the recruitment of diabetogenic CD8+ T cells to the gut...
October 19, 2017: Cell
https://www.readbyqxmd.com/read/29053842/differential-expression-of-water-channel-and-noncoding-rna-biogenesis-related-genes-in-three-lines-of-chickens-under-a-short-term-water-restriction
#5
S Orlowski, J Flees, N Anthony, S Dridi
Genetic selection for high growth rate has resulted in tremendous changes not only in feed efficiency, but also in water consumption between modern broilers and their ancestor jungle fowl (JF). However molecular mechanisms involved in water homeostasis are still not well defined. This study aimed, therefore, to determine the effect of short-term water restriction on the expression of water channel- and noncoding RNA biogenesis-related genes in the kidney and whole blood of JF, broiler population from the 1990s (RB1995), and modern broiler population developed in 2015 (ARB2015)...
October 5, 2017: Poultry Science
https://www.readbyqxmd.com/read/29053600/detection-and-management-of-mango-dieback-disease-in-the-united-arab-emirates
#6
Esam Eldin Saeed, Arjun Sham, Ayah AbuZarqa, Khawla A Al Shurafa, Tahra S Al Naqbi, Rabah Iratni, Khaled El-Tarabily, Synan F AbuQamar
Mango is affected by different decline disorders causing significant losses to mango growers. In the United Arab Emirates (UAE), the pathogen was isolated from all tissues sampled from diseased trees affected by Lasiodiplodia theobromae. Symptoms at early stages of the disease included general wilting appearance of mango trees, and dieback of twigs. In advanced stages, the disease symptoms were also characterized by the curling and drying of leaves, leading to complete defoliation of the tree and discolouration of vascular regions of the stems and branches...
October 20, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/29053416/imaging-of-integrin-%C3%AE-v%C3%AE-3-expression-in-lung-cancers-and-brain-tumors-using-single-photon-emission-computed-tomography-with-a-novel-radiotracer-99m-tc-ida-d-c-rgdfk-2
#7
Yoo Sung Song, Hyun Soo Park, Byung Chul Lee, Jae Ho Jung, Ho-Young Lee, Sang Eun Kim
Integrin αvβ3 is a molecular marker for the estimation of tumor angiogenesis and is an imaging target for radiolabeled Arg-Gly-Asp (RGD) peptides. In this study, the authors investigated the clinical efficacy and safety of a novel radiolabeled RGD peptide, (99m)Tc-IDA-D-[c(RGDfK)]2, for the imaging of integrin αvβ3 expression, as a measure of tumor angiogenesis in lung cancers and brain tumors. Five patients with lung cancers and seven with brain tumors underwent (99m)Tc-IDA-D-[c(RGDfK)]2 single-photon emission computed tomography (SPECT) imaging...
October 2017: Cancer Biotherapy & Radiopharmaceuticals
https://www.readbyqxmd.com/read/29053266/structure-activity-relationships-of-new-natural-product-based-diaryloxazoles-with-selective-activity-against-androgen-receptor-positive-breast-cancer-cells
#8
Andrew J Robles, Shelby McCowen, Shengxin Cai, Michaels Glassman, Francisco Ruiz, Robert H Cichewicz, Stanton F McHardy, Susan L Mooberry
Targeted therapies for ER+/PR+ and HER2-amplified breast cancers have improved patient survival, but there are no therapies for triple negative breast cancers (TNBC) that lack expression of estrogen and progesterone receptors (ER/PR), or amplification or overexpression of HER2. Gene expression profiling of TNBC has identified molecular subtypes and representative cell lines. An extract of the Texas native plant Amyris texana was found to have selective activity against MDA-MB-453 cells, a model of the luminal androgen receptor (LAR) subtype of TNBC...
October 20, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29053217/behavioral-control-by-striatal-a2a-dopamine-d2-receptor-heteromers
#9
Jaume Taura, Marta Valle-León, Kristoffer Sahlholm, Masahiko Watanabe, Katheleen Van Craenenbroeck, Víctor Fernández-Dueñas, Sergi Ferré, Francisco Ciruela
G protein-coupled receptors (GPCR) exhibit the ability to form receptor complexes that include molecularly different GPCR (i.e. GPCR heteromers), which endow them with singular functional and pharmacological characteristics. The relative expression of GPCR heteromers remains a matter of intense debate. Recent studies support that adenosine A2A receptors (A2A R) and dopamine D2 receptors (D2 R) predominantly form A2A R-D2 R heteromers in the striatum. The aim of the present study was evaluating the behavioral effects of pharmacological manipulation and genetic blockade of A2A R and D2 R within the frame of such a predominant striatal heteromeric population...
October 20, 2017: Genes, Brain, and Behavior
https://www.readbyqxmd.com/read/29053192/dissociation-of-nnos-from-psd-95-promotes-functional-recovery-after-cerebral-ischaemia-in-mice-through-reducing-excessive-tonic-gaba-release-from-reactive-astrocytes
#10
Yu-Hui Lin, Hai-Ying Liang, Ke Xu, Huan-Yu Ni, Jian Dong, Hui Xiao, Lei Chang, Hai-Yin Wu, Fei Li, Dong-Ya Zhu, Chun-Xia Luo
Mechanisms underlying functional recovery after stroke are little known, and effective drug intervention during the delayed stage is desirable. One potential drug target, the protein-protein interaction between neuronal nitric oxide synthase (nNOS) and postsynaptic density protein 95 (PSD-95), is critical to acute ischaemic damage and neurogenesis. We show that nNOS-PSD-95 dissociation induced by microinjection of a recombinant fusion protein Tat-nNOS-N1-133 or systemic administration of a small molecule ZL006 from days 4 to 10 after photothrombotic ischaemia in mice reduced excessive tonic inhibition in the peri-infarct cortex and ameliorated motor functional outcome...
October 20, 2017: Journal of Pathology
https://www.readbyqxmd.com/read/29053159/proximity-hybridization-triggered-rolling-circle-amplification-for-sensitive-electrochemical-homogeneous-immunoassay
#11
Fenglei Gao, Fuyi Zhou, Songjie Chen, Yao Yao, Jing Wu, Dengyang Yin, Deqin Geng, Po Wang
A new homogeneous electrochemical immunoassay strategy was developed for ultrasensitive detection of carcinoembryonic antigen (CEA) based on target-induced proximity hybridization coupled with rolling circle amplification (RCA). The immobilization-free detection of CEA was realized by the use of an uncharged peptide nucleic acid (PNA) probe labeled with ferrocene (Fc) as the electroactive indicator on a negatively charged indium tin oxide (ITO) electrode. In the presence of a target protein and two DNA-labeled antibodies, the proximate complex formed in homogeneous solution could unfold the molecular beacon, and a part of the unfolded molecular beacon as a primer hybridized with the RCA template to initiate the RCA process...
October 20, 2017: Analyst
https://www.readbyqxmd.com/read/29052968/non-steroidal-estrogen-receptor-isoform-selective-biphenyls
#12
Seema Bhatnagar, Anjali Soni, Swati Kaushik, Megha Rikhi, T R Santhosh Kumar, B Jayaram
Estrogen receptor (ER) has been a therapeutic target to treat ER positive breast cancer, most notably by agents known as selective estrogen receptor modulators (SERMs). However, resistance and severe adverse effects of known drugs gave impetus to the search for newer agents with better therapeutic profile. ERα and ERβ are two isoforms sharing 56% identity, and having different physiological functions and expressions in various tissues. Only two residues differ in the active sites of the two isoforms motivating us to design isoform selective ligands...
October 20, 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/29052959/peptide-ligands-for-targeting-the-extracellular-domain-of-egfr-comparison-between-linear-and-cyclic-peptides
#13
Tyrslai M Williams, Rushikesh Sable, Sitanshu Singh, M Graça H Vicente, Seetharama Jois
Colorectal cancer (CRC) is the third most common solid internal malignancy among cancers. Early detection of cancer is key to increasing the survival rate of colorectal cancer patients. Overexpression of the EGFR protein is associated with CRC. We have designed a series of peptides that are highly specific for the extracellular domain of EGFR, based on our earlier studies on linear peptides. The previously reported linear peptide LARLLT, known to bind to EGFR, was modified with the goals of increasing its stability and its specificity towards EGFR...
October 20, 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/29052792/prediction-of-binding-poses-to-fxr-using-multi-targeted-docking-combined-with-molecular-dynamics-and-enhanced-sampling
#14
Soumendranath Bhakat, Emil Åberg, Pär Söderhjelm
Advanced molecular docking methods often aim at capturing the flexibility of the protein upon binding to the ligand. In this study, we investigate whether instead a simple rigid docking method can be applied, if combined with multiple target structures to model the backbone flexibility and molecular dynamics simulations to model the sidechain and ligand flexibility. The methods are tested for the binding of 35 ligands to FXR as part of the first stage of the Drug Design Data Resource (D3R) Grand Challenge 2 blind challenge...
October 20, 2017: Journal of Computer-aided Molecular Design
https://www.readbyqxmd.com/read/29052680/progressive-structural-modification-to-a-zinc-actuated-photoinduced-electron-transfer-pet-switch-in-the-context-of-intracellular-zinc-imaging
#15
Miguel Macias-Contreras, Kirsten L Daykin, J Tyler Simmons, John R Allen, Zachary S Hooper, Michael W Davidson, Lei Zhu
Photoinduced electron transfer (PeT)-type fluorescent molecular switches are often applied in ion-selective sensors. Zinc-targeting sensors that contain an anilino-based electron donor (aka, the PeT 'switch') have multiple advantages over those with an aliphatic amino switch. In addition to the lower pKa value of an aniline than that of a comparably substituted aliphatic amine, which reduces the interference of pH on the spectral properties of the attached fluorophore, the oxidation potentials of anilino groups are lower than those of aliphatic amino counterparts, which make them better electron donors in PeT...
October 20, 2017: Organic & Biomolecular Chemistry
https://www.readbyqxmd.com/read/29052679/oligonucleotide-modifications-enhance-probe-stability-for-single-cell-transcriptome-in-vivo-analysis-tiva
#16
S B Yeldell, B K Ruble, I J Dmochowski
Single cell transcriptomics provides a powerful discovery tool for identifying new cell types and functions as well as a means to probe molecular features of the etiology and treatment of human diseases, including cancer. However, such analyses are limited by the difficulty of isolating mRNA from single cells within biological samples. We recently introduced a photochemical method for isolating mRNA from single living cells, Transcriptome In Vivo Analysis (TIVA). The TIVA probe is a "caged" polyU : polyA oligonucleotide hairpin designed to enter live tissue, where site-specific activation with 405 nm laser reveals the polyU-biotin strand to bind mRNA in a target cell, enabling subsequent mRNA isolation and sequencing...
October 20, 2017: Organic & Biomolecular Chemistry
https://www.readbyqxmd.com/read/29052618/a-role-for-prefrontal-cortical-nmda-receptors-in-murine-alcohol-heightened-aggression
#17
Emily L Newman, Miho Terunuma, Tiffany Wang, Nishani Hewage, Matthew B Bicakci, Stephen J Moss, Joseph F DeBold, Klaus A Miczek
Alcohol is associated with nearly half of all violent crimes committed in the United States; yet, a potential neural basis for this type of pathological aggression remains elusive. Alcohol may act on NMDA receptors (NMDARs) within cortical circuits to impede processing and to promote aggression. Here, male mice were characterized as alcohol-heightened (AHAs) or alcohol non-heightened aggressors (ANAs) during resident-intruder confrontations after self-administering 1.0 g/kg alcohol (6% w/v) or water. Alcohol produced a pathological-like pattern of aggression in AHAs; these mice shifted their bites to more vulnerable locations on the body of a submissive animal, including the anterior back and ventrum after consuming alcohol...
October 20, 2017: Neuropsychopharmacology: Official Publication of the American College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/29052616/pregenual-anterior-cingulate-dysfunction-associated-with-depression-in-ocd-an-integrated-multimodal-fmri-1-h-mrs-study
#18
Reza Tadayonnejad, Rangaprakash Deshpande, Olusola Ajilore, Teena Moody, Francesca Morfini, Ronald Ly, Joseph O'Neill, Jamie D Feusner
Depression is a commonly-occurring symptom in obsessive-compulsive disorder (OCD), and is associated with worse functional impairment, poorer quality of life, and poorer treatment response. Understanding the underlying neurochemical and connectivity-based brain mechanisms of this important symptom domain in OCD is necessary for development of novel, more globally effective treatments. To investigate biopsychological mechanisms of comorbid depression in OCD, we examined effective connectivity and neurochemical signatures in the pregenual anterior cingulate cortex (pACC), a structure known to be involved in both OCD and depression...
October 20, 2017: Neuropsychopharmacology: Official Publication of the American College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/29052609/neuro-ophthalmic-side-effects-of-molecularly-targeted-cancer-drugs
#19
REVIEW
M T Bhatti, A K S Salama
The past two decades has been an amazing time in the advancement of cancer treatment. Molecularly targeted therapy is a concept in which specific cellular molecules (overexpressed, mutationally activated, or selectively expressed proteins) are manipulated in an advantageous manner to decrease the transformation, proliferation, and/or survival of cancer cells. In addition, increased knowledge of the role of the immune system in carcinogenesis has led to the development of immune checkpoint inhibitors to restore and enhance cellular-mediated antitumor immunity...
October 20, 2017: Eye
https://www.readbyqxmd.com/read/29052591/targeting-thermogenesis-in-brown-fat-and-muscle-to-treat-obesity-and-metabolic-disease
#20
REVIEW
Matthias J Betz, Sven Enerbäck
Brown fat is emerging as an interesting and promising target for therapeutic intervention in obesity and metabolic disease. Activation of brown fat in humans is associated with marked improvement in metabolic parameters such as levels of free fatty acids and insulin sensitivity. Skeletal muscle is another important organ for thermogenesis, with the capacity to induce energy-consuming futile cycles. In this Review, we focus on how these two major thermogenic organs - brown fat and muscle - act and cooperate to maintain normal body temperature...
October 23, 2017: Nature Reviews. Endocrinology
keyword
keyword
93715
1
2
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read
×

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"