Read by QxMD icon Read


Wei Liu, Guanghui Han, Yalin Yin, Shuai Jiang, Guojun Yu, Qing Yang, Wenhui Yu, Xiangdong Ye, Yanting Su, Yajun Yang, Gerald W Hart, Hui Sun
O-linked N-acetylglucosamine (O-GlcNAcylation) is an important post-translational modification on serine or threonine of proteins, mainly observed in nucleus or cytoplasm. O-GlcNAcylation regulates many cell processes, including transcription, cell cycle, neural development, and nascent polypeptide chains stabilization. However, the facile identification of O-GlcNAc is a major bottleneck in O-GlcNAcylation research. Herein, we report that a lectin, AANL (Agrocybe aegerita GlcNAc specific lectin), also reported as AAL2, can be used as a powerful probe for O-GlcNAc identification...
March 19, 2018: Glycobiology
Junghyun L Suh, Brian Watts, Jacob I Stuckey, Jacqueline L Norris-Drouin, Stephanie H Cholensky, Bradley M Dickson, Yi An, Sebastian Mathea, Eidarus Salah, Stefan Knapp, Abid Khan, Alexander T Adams, Brian D Strahl, Cari A Sagum, Mark T Bedford, Lindsey I James, Dmitri B Kireev, Stephen V Frye
Multivalent binding is an efficient means to enhance the affinity and specificity of chemical probes targeting multi-domain proteins in order to study their function and role in disease. While the theory of multivalent binding is straightforward, physical and structural characterization of bivalent binding encounters multiple technical difficulties. We present a case study where a combination of experimental techniques and computational simulations was used to comprehensively characterize the binding and structure-affinity relationships for a series of Bromosporine-based bivalent bromodomain ligands with a bivalent protein, Transcription Initiation Factor TFIID subunit 1 (TAF1)...
March 20, 2018: Biochemistry
Qiaoxian Huang, Shengke Li, Yuan-Fu Ding, Hang Yin, Lian-Hui Wang, Ruibing Wang
Due to its outstanding capability to facilitate DNA condensation, transportation and endosomal escape, polyethylenimine (PEI) has been frequently studied for gene delivery. However, its molecular weight (M.W.) dependent transfection efficiency and cytotoxicity has severely limited its clinical application. To resolve this dilemma, a supramolecular strategy was developed for the first time, in which PEI with large M.W. (branched, 25 kDa) that has a satisfactory transfection efficiency, yet high non-specific cytotoxicity for gene delivery was wrapped with macrocyclic cucurbit[7]uril (CB[7])...
March 20, 2018: Biomaterials Science
Julie Eberle Davis, Ravi Kumar Gundampati, Srinivas Jayanthi, Joshua Anderson, Abigail Pickhardt, Bhanu Prasanth Koppolu, David A Zaharoff, Thallapuranam Krishnaswamy Suresh Kumar
Acidic human fibroblast growth factor (hFGF1) plays a key role in cell growth and proliferation. Activation of the cell surface FGF receptor is believed to involve the glycosaminoglycan, heparin. However, the exact role of heparin is a subject of considerable debate. In this context, in this study, the correlation between heparin binding affinity and cell proliferation activity of hFGF1 is examined by extending the heparin binding pocket through selective engineering via charge reversal mutations (D82R, D84R and D82R/D84R)...
March 2018: Biochemistry and Biophysics Reports
Dario Spigolon, D Travis Gallagher, Adrian Velazquez-Campoy, Donatella Bulone, Jatin Narang, Pier Luigi San Biagio, Francesco Cappello, Alberto J L Macario, Everly Conway de Macario, Frank T Robb
The human chaperonin complex is a ~ 1 MDa nanomachine composed of two octameric rings formed from eight similar but non-identical subunits called CCT. Here, we are elucidating the mechanism of a heritable CCT5 subunit mutation that causes profound neuropathy in humans. In previous work, we introduced an equivalent mutation in an archaeal chaperonin that assembles into two octameric rings like in humans but in which all subunits are identical. We reported that the hexadecamer formed by the mutant subunit is unstable with impaired chaperoning functions...
December 2017: Biochemistry and Biophysics Reports
Dipanwita Batabyal, Thomas L Poulos
We have compared the thermodynamics of substrate and redox partner binding of P450cam to its close homologue, CYP101D1, using isothermal titration calorimetry (ITC). CYP101D1 binds camphor about 10-fold more weakly than P450cam which is consistent with the inability of camphor to cause a complete low- to high-spin shift in CYP101D1. Even so molecular dynamics simulations show that camphor is very stable in the CYP101D1 active site similar to P450cam. ITC data on the binding of the CYP101D1 ferredoxin redox partner (abbreviated Arx) shows that the substrate-bound closed state of CYP101D1 binds Arx more tightly than the substrate-free open form...
March 1, 2018: Journal of Inorganic Biochemistry
Bernd R Gardill, Ricardo E Rivera-Acevedo, Ching-Chieh Tung, Mark Okon, Lawrence P McIntosh, Filip Van Petegem
Voltage-gated sodium channels (NaV ) are responsible for the rapid depolarization of many excitable cells. They readily inactivate, a process where currents diminish after milliseconds of channel opening. They are also targets for a multitude of disease-causing mutations, many of which have been shown to affect inactivation. A cluster of disease mutations, linked to Long-QT and Brugada syndromes, is located in a C-terminal EF-hand like domain of NaV 1.5, the predominant cardiac sodium channel isoform. Previous studies have suggested interactions with the III-IV linker, a cytosolic element directly involved in inactivation...
March 14, 2018: Scientific Reports
Anthony Watts
Saturation transfer difference (STD) NMR constitutes one of the most popular ligand-based NMR techniques for the study of protein-ligand interactions. This is due to its robustness and the fact that it is focused on the signals of the ligand, without any need for NMR information of the macromolecular target. This technique is most commonly applied to systems involving different types of ligands (e.g. small organic molecules, carbohydrates, or lipids) and a protein as the target, where the latter is selectively saturated...
March 14, 2018: Chembiochem: a European Journal of Chemical Biology
Sergio Álvarez-Pérez, Marta E García, José L Blanco
Combination therapy has become popular in clinical practice, but limited data on the effects of combinations of antifungal agents is still available for most fungal pathogens. We studied the in vitro response of 30 genetically diverse clinical strains of the basidiomycetous lipophilic yeast Malassezia pachydermatis obtained from cases of canine otitis to several amphotericin B (AMB)-azole combinations. Broth microdilution checkerboard tests revealed that AMB antagonized the effects of itraconazole (ITC) and voriconazole (VRC) in 50% and 6...
March 8, 2018: Medical Mycology: Official Publication of the International Society for Human and Animal Mycology
Patricia Santofimia-Castaño, Bruno Rizzuti, Olga Abián, Adrián Velázquez-Campoy, Juan L Iovanna, José L Neira
BACKGROUND: NUPR1 is a multifunctional intrinsically disordered protein (IDP) involved, among other functions, in chromatin remodelling, and development of pancreatic ductal adenocarcinoma (PDAC). It interacts with several biomolecules through hydrophobic patches around residues Ala33 and Thr68. The drug trifluoperazine (TFP), which hampers PDAC development in xenografted mice, also binds to those regions. Because of the large size of the hot-spot interface of NUPR1, small molecules could not be adequate to modulate its functions...
March 9, 2018: Biochimica et Biophysica Acta
Liora Werber, Yitzhak Mastai
One of the most powerful techniques that are currently available to measure thermodynamic parameters such as enthalpy (ΔH), Gibbs free energy (ΔG), entropy changes (ΔS), and binding affinity in chemical reactions is isothermal titration calorimetry (ITC). Recent advances in instrumentation have facilitated the development of ITC as a very essential analytical tool in biology and chemistry. In this article, we will focus on a review of the literature on the application of ITC for the study of chiral systems and chiral interactions...
March 12, 2018: Chirality
Piman Pocasap, Natthida Weerapreeyakul, Kanjana Thumanu
The structure of the isothiocyanates (ITCs)-erucin, sulforaphane, erysolin, sulforaphene, and phenethyl isothiocyanate-were assessed as well as their respective in vitro anticancer activity on the hepatocellular carcinoma cell line HepG2. All of these ITCs induced both apoptotic and necrotic cell death. FTIR analysis indicated that the ITCs caused changes in cellular components comparable to vinblastine. Despite no observable effect on DNA, the ITCs all induced generation of intracellular reactive oxygen species (ROS) and suppressed microtubule polymerization...
March 6, 2018: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
Letizia Romeo, Renato Iori, Patrick Rollin, Placido Bramanti, Emanuela Mazzon
The use of plant-derived products as antimicrobial agents has been investigated in depth. Isothiocyanates (ITCs) are bioactive products resulting from enzymatic hydrolysis of glucosinolates (GLs), the most abundant secondary metabolites in the botanical order Brassicales. Although the antimicrobial activity of ITCs against foodborne and plant pathogens has been well documented, little is known about their antimicrobial properties against human pathogens. This review collects studies that focus on this topic...
March 9, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Jinling Xu, Luuk Koopal, Linchuan Fang, Juan Xiong, WenFeng Tan
Proton and copper (Cu) binding to soil and lignite-based humic acid (HA) was investigated by combining X-ray absorption fine structure (XAFS) spectroscopy, isothermal titration calorimetry (ITC) and non-ideal-competitive-adsorption (NICA) modeling. NICA model calculations and XAFS results showed that bidentate and monodentate inner-sphere complexation occurred for Cu binding to HA. The site-type specific thermodynamic parameters obtained by combining ITC measurements and NICA calculations revealed that copper binding to deprotonated carboxylic-type sites was entropically driven and that to deprotonated phenolic-type sites was driven by entropy and enthalpy...
March 9, 2018: Environmental Science & Technology
Nancy L Fleischer, Paula Lozano, Yun-Hsuan Wu, James W Hardin, Gang Meng, Angela D Liese, Geoffrey T Fong, James F Thrasher
OBJECTIVE: To examine how point-of-sale (POS) display bans, tobacco retailer density and tobacco retailer proximity were associated with smoking cessation and relapse in a cohort of smokers in Canada, where provincial POS bans were implemented differentially over time from 2004 to 2010. METHODS: Data from the 2005 to 2011 administrations of the International Tobacco Control (ITC) Canada Survey, a nationally representative cohort of adult smokers, were linked via residential geocoding with tobacco retailer data to derive for each smoker a measure of retailer density and proximity...
March 8, 2018: Tobacco Control
Raimunda Sâmia Nogueira Brilhante, Edmilson Emanuel Monteiro Correia, Glaucia Morgana de Melo Guedes, Jonathas Sales de Oliveira, Débora de Souza Collares Maia Castelo-Branco, Rossana de Aguiar Cordeiro, Adriana de Queiroz Pinheiro, Lúcio Jackson Queiroz Chaves, Waldemiro de Aquino Pereira Neto, José Júlio Costa Sidrim, Marcos Fábio Gadelha Rocha
BACKGROUND: As shown by recent researches, most of the clinically relevant fungi, including dermatophytes, form biofilms in vitro and in vivo, which may present antimicrobial tolerance favoring recurrent infections. OBJECTIVES: The aim of this study was to determine the minimum inhibitory concentrations (MICs) of itraconazole (ITC), voriconazole (VCZ) and griseofulvin (GRI) against Trichophyton rubrum, Trichophyton tonsurans, Trichophyton mentagrophytes, Microsporum canis and Microsporum gypseum, in planktonic and biofilm growth...
March 8, 2018: Mycoses
Anne Meyer, Hannah R Holt, Farikou Oumarou, Kalinga Chilongo, William Gilbert, Albane Fauron, Chisoni Mumba, Javier Guitian
BACKGROUND: Animal African trypanosomiasis (AAT) and its tsetse vector are responsible for annual losses estimated in billions of US dollars ($). Recent years have seen the implementation of a series of multinational interventions. However, actors of AAT control face complex resource allocation decisions due to the geographical range of AAT, diversity of ecological and livestock systems, and range of control methods available. METHODS: The study presented here integrates an existing tsetse abundance model with a bio-economic herd model that captures local production characteristics as well as heterogeneities in AAT incidence and breed...
March 7, 2018: Parasites & Vectors
Jonathan T Caranfa, Elaine Nguyen, Rafay Ali, Iregi Francis, Albert Zichichi, Elliott Bosco, Craig I Coleman, William L Baker, Christine G Kohn
BACKGROUND: Randomized controlled trials (RCTs) have compared mechanical endovascular therapy (MET) in addition to intravenous tissue plasminogen activator (IVtPA) to IVtPA alone for the management of acute ischemic stroke (AIS). Direct comparative studies between individual METs are not available. In lieu of head-to-head randomized control trials, we performed an adjusted indirect treatment comparison (ITC) meta-analysis to assess the comparative efficacy and safety of different METs, Solitaire+IVtPA and Penumbra+IVtPA in AIS patients...
2018: PloS One
Shumaila Afrin, Yusra Rahman, Mohammad Tabish
Ticlopidine is an anti-platelet drug that functions as a P2Y12 receptor antagonist. The present study provides a detailed characterization of interaction of ticlopidine with a model transport protein, bovine serum albumin (BSA) as well as an assessment of its bilirubin displacing ability using a multi-spectroscopic approach in combination with isothermal titration calorimetry. The value of binding constant determined using ITC studies was found to be 3.03 x 103 M-1 with a binding stoichiometry of approximately 1:1...
March 7, 2018: Journal of Biomolecular Structure & Dynamics
Franko Burčul, Ivana Generalić Mekinić, Mila Radan, Patrick Rollin, Ivica Blažević
Finding a new type of cholinesterase inhibitor that would overcome the brain availability and pharmacokinetic parameters or hepatotoxic liability has been a focus of investigations dealing with the treatment of Alzheimer's disease. Isothiocyanates have not been previously investigated as potential cholinesterase inhibitors. These compounds can be naturally produced from their glucosinolate precursors, secondary metabolites widely distributed in our daily Brassica vegetables. Among 11 tested compounds, phenyl isothiocyanate and its derivatives showed the most promising inhibitory activity...
December 2018: Journal of Enzyme Inhibition and Medicinal Chemistry
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"