keyword
MENU ▼
Read by QxMD icon Read
search

drug residue

keyword
https://www.readbyqxmd.com/read/28088282/conjugation-site-analysis-of-antibody-drug-conjugates-adcs-by-signature-ion-fingerprinting-and-normalized-area-quantitation-approach-using-nano-liquid-chromatography-coupled-to-high-resolution-mass-spectrometry
#1
Hua Sang, Gaoyuan Lu, Yazhong Liu, Qiyue Hu, Weifeng Xing, Dongbing Cui, Fang Zhou, Jingwei Zhang, Haiping Hao, Guangji Wang, Hui Ye
Trastuzumab-MCC-DM1 (T-DM1) is an antibody-drug conjugate (ADC) that consists of a monoclonal antibody (mAb) trastuzumab non-cleavably linked to a cytotoxic drug DM1. During production, the DM1 agents were conjugated to the lysine residues of the mAb in a non-specific manner, yielding a heterogeneous mixture of ADC molecules that differ with respect to both the number and the conjugation sites of DM1 per mAb molecule. Since drug conjugation sites of ADC can significantly impact properties such as stability and pharmacokinetic behaviors, a rapid and reliable approach for conjugation site analysis of ADCs is highly demanded...
February 22, 2017: Analytica Chimica Acta
https://www.readbyqxmd.com/read/28088045/uhplc-ms-ms-method-for-the-quantitation-of-penicillin-g-and-metabolites-in-citrus-fruit-using-internal-standards
#2
Daniele Canzani, Kevin Hsieh, Matthew Standland, Walter Hammack, Fadi Aldeek
Penicillin G has been applied to citrus trees as a potential treatment in the fight against Huanglongbing (HLB). Here, we have developed and validated a method to identify and quantitate penicillin G and two of its metabolites, penillic acid and penilloic acid, in citrus fruit using ultra high performance liquid chromatography-tandem mass spectrometry (UHPLC-MS/MS). This method improves upon a previous method by incorporating isotopically labeled internal standards, namely, penillic acid-D5, and penilloic acid-D5...
January 10, 2017: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
https://www.readbyqxmd.com/read/28087699/activation-of-c-abl-kinase-potentiates-the-anti-myeloma-drug-lenalidomide-by-promoting-dda1-recruitment-to-the-crl4-ubiquitin-ligase
#3
Shaobing Gao, Chenlu Geng, Tianyu Song, Xuanru Lin, Jiye Liu, Zhen Cai, Yong Cang
Cullin Ring Ligase 4 (CRL4), a complex of Cul4 and DDB1, regulates cell cycle, DNA damage repair, and chromatin replication by targeting a variety of substrates for ubiquitination. CRL4 is also hijacked by viral proteins or thalidomide-derived compounds to degrade host restriction factors. Here we report that the c-Abl non-receptor kinase phosphorylates DDB1 at residue Y316 to recruit a small regulatory protein DDA1, leading to increased substrate ubiquitination. Pharmacological inhibition or genetic ablation of the Abl-DDB1-DDA1 axis decreases the ubiquitination of CRL4 substrates, including IKZF1 and IKZF3 in lenalidomide-treated multiple myeloma cells...
January 13, 2017: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/28087281/mtuepa-trans-urethral-monopolar-enucleation-of-prostatic-adenoma-preliminary-report
#4
Vito Pansadoro, Paolo Emiliozzi, Gianluca Del Vecchio, Marco Martini, Paolo Scarpone, Francesco Del Giudice, Domenico Veneziano, Aldo Brassetti, Christophe Assenmacher
OBJECTIVES: To describe preliminary results of our monopolar Transurethral Enucleation of Prostatic Adenoma (mTUEPA). METHODS: A consecutive series of patient treated with mTUEPA, a retrograde enucleation of the prostatic adenoma performed by means of a standard monopolar resectoscope, were prospectively enrolled. Symptoms, uroflometry parmeters and post voiding residual (PVR) were assessed at baseline and 1, 6 and 12 months post-operatively. Prostate volume (PV) was evaluated at baseline by means of transrectal ultrasound...
January 10, 2017: Urology
https://www.readbyqxmd.com/read/28086782/in-vivo-antiplasmodial-activity-and-toxicological-assessment-of-hydroethanolic-crude-extract-of-ajuga-remota
#5
Aschalew Nardos, Eyasu Makonnen
BACKGROUND: Malaria is one of the most life-threatening health problems worldwide and treatment has been compromised by drug resistance. Identifying lead molecules from natural products might help to find better anti-malarial drugs, since those obtained from natural sources are still effective against malarial parasites. This study aimed at investigating the in vivo antiplasmodial activity of crude extract of the leaves of Ajuga remota together with its safety in mice models. METHODS: In vivo parasite growth inhibitory effect of crude extract was assessed in mice inoculated with Plasmodium berghei (ANKA strain)...
January 13, 2017: Malaria Journal
https://www.readbyqxmd.com/read/28079981/inhibiting-solid-tumor-growth-in-vivo-by-non-tumor-penetrating-nanomedicine
#6
Shixian Lv, Zhaohui Tang, Wantong Song, Dawei Zhang, Mingqiang Li, Huaiyu Liu, Jianjun Cheng, Wu Zhong, Xuesi Chen
Nanomedicine (NM) cannot penetrate deeply into solid tumors, which is partly attributed to the heterogeneous microenvironment and high interstitial fluid pressure of solid tumors. To improve NM efficacy, there has been tremendous effort developing tumor-penetrating NMs by miniaturizing NM sizes or controlling NM surface properties. But progress along the direction of developing tumor penetrating nanoparticle has been slow and improvement of the overall antitumor efficacy has been limited. Herein, a novel strategy of inhibiting solid tumor with high efficiency by dual-functional, nontumor-penetrating NM is demonstrated...
January 12, 2017: Small
https://www.readbyqxmd.com/read/28079218/zinc-ion-induced-conformational-changes-in-new-delphi-metallo-%C3%AE-lactamase-1-probed-by-molecular-dynamics-simulations-and-umbrella-sampling
#7
Jianzhong Chen, Jinan Wang, Weiliang Zhu
The hydrolysis of a β-lactam core ring caused by new Delphi metallo-β-lactamase 1 (NDM-1) with the help of two zinc cofactors induces significant resistance toward β-lactam antibiotics. Molecular dynamics (MD) simulations and the umbrella sampling method are integrated to study the conformational change mechanism of NDM-1 mediated by zinc ion binding. The statistical analyses of interaction contacts of the antibiotic ampicillin (AMP) with residues based on MD trajectories suggest that two Zn ions are essential for maintaining the binding of AMP with NDM-1...
January 12, 2017: Physical Chemistry Chemical Physics: PCCP
https://www.readbyqxmd.com/read/28079013/natural-product-inhibitors-of-topoisomerases-review-and-docking-study
#8
L Scotti, F J B Mendonça Júnior, F F Ribeiro, J F Tavares, M S Da Silva, J M Barbosa Filho, M T Scotti
Since ancient times, natural products have been used in treating various diseases effectively and safely. Nowadays, these natural compounds are submitted to sophisticated methodologies from isolation, computing, analytical, and even serving as pharmacophore suggestions for synthesis. The substances extracted from marine species, plants, and microorganisms present activities beneficial to our health, including protection against malignant tumors. The topoisomerase enzymes play an important role in DNA metabolism, and searching for enzyme inhibitors is an important target in the search for new anticancer drugs...
January 11, 2017: Current Protein & Peptide Science
https://www.readbyqxmd.com/read/28077339/st20-a-new-venomous-animal-derived-natural-peptide-with-immunosuppressive-and-anti-inflammatory-activities
#9
Min Xiao, Li Ding, Weishan Yang, Lin Chai, Yuwen Sun, Xianyi Yang, Dandan Li, Hua Zhang, Wenxin Li, Zhijian Cao, Yingliang Wu, Jian Li, Shan Li, Zongyun Chen
Peptide toxins from venomous animals are natural resources with diverse biological functions and therapeutic potential towards human diseases. For venomous scorpions, many valuable peptide toxins have been discovered from Buthidae scorpions, but few works were done about non-buthidae scorpions. Here, we cloned and characterized the first disulfide-bridged toxin peptide St20 from the non-buthidae scorpion Scorpiops tibetanus. St20 has a putative 23-residue signal peptide, followed by a presumed 34-residue mature peptide including 8 cysteines...
January 8, 2017: Toxicon: Official Journal of the International Society on Toxinology
https://www.readbyqxmd.com/read/28076845/molecular-dynamics-simulation-reveals-how-phosphorylation-of-tyrosine-26-of-phosphoglycerate-mutase-1-upregulates-glycolysis-and-promotes-tumor-growth
#10
Yan Wang, Wen-Sheng Cai, Luonan Chen, Guanyu Wang
Phosphoglycerate mutase 1 (PGAM1) catalyzes the eighth step of glycolysis and is often found upregulated in cancer cells. To test the hypothesis that the phosphorylation of tyrosine 26 residue of PGAM1 greatly enhances its activity, we performed both conventional and steered molecular dynamics simulations on the binding and unbinding of PGAM1 to its substrates, with tyrosine 26 either phosphorylated or not. We analyzed the simulated data in terms of structural stability, hydrogen bond formation, binding free energy, etc...
January 5, 2017: Oncotarget
https://www.readbyqxmd.com/read/28075591/discovery-of-potent-cyclophilin-inhibitors-based-on-structural-simplification-of-sanglifehrin-a
#11
Victoria A Steadman, Simon B Pettit, Karine G Poullennec, Linos Lazarides, Andrew J Keats, David K Dean, Steven J Stanway, Carol A Austin, Jonathan A Sanvoisin, Gregory M Watt, Hans G Fliri, Albert C Liclican, Debi Jin, Melanie H Wong, Stephanie A Leavitt, Yu-Jen Lee, Yang Tian, Christian R Frey, Todd C Appleby, Uli Schmitz, Petr Jansa, Richard L Mackman, Brian Edward Schultz
Cyclophilin inhibition has been a target for the treatment of hepatitis C and other diseases, but the generation of potent, drug-like molecules through chemical synthesis has been challenging. In this study, a set of macrocyclic cyclophilin inhibitors was synthesized based on the core structure of the natural product sanglifehrin A. Initial compound optimization identified the valine-m-tyrosine-piperazic acid tripeptide (Val-m-Tyr-Pip) in the sanglifehrin core, stereocenters at C14 and C15, and the hydroxyl group of the m-tyrosine (m-Tyr) residue as key contributors to compound potency...
January 11, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28075379/veterinary-compounding-regulation-challenges-and-resources
#12
REVIEW
Gigi Davidson
The spectrum of therapeutic need in veterinary medicine is large, and the availability of approved drug products for all veterinary species and indications is relatively small. For this reason, extemporaneous preparation, or compounding, of drugs is commonly employed to provide veterinary medical therapies. The scope of veterinary compounding is broad and focused primarily on meeting the therapeutic needs of companion animals and not food-producing animals in order to avoid human exposure to drug residues. As beneficial as compounded medical therapies may be to animal patients, these therapies are not without risks, and serious adverse events may occur from poor quality compounds or excipients that are uniquely toxic when administered to a given species...
January 10, 2017: Pharmaceutics
https://www.readbyqxmd.com/read/28074848/crystal-structure-of-stna-for-the-biosynthesis-of-antitumor-drug-streptonigrin-reveals-a-unique-substrate-binding-mode
#13
Tianle Qian, Jing Wo, Yan Zhang, Quanwei Song, Guoqiang Feng, Ray Luo, Shuangjin Lin, Geng Wu, Hai-Feng Chen
Streptonigrin methylesterase A (StnA) is one of the tailoring enzymes that modify the aminoquinone skeleton in the biosynthesis pathway of Streptomyces species. Although StnA has no significant sequence homology with the reported α/β-fold hydrolases, it shows typical hydrolytic activity in vivo and in vitro. In order to reveal its functional characteristics, the crystal structures of the selenomethionine substituted StnA (SeMet-StnA) and the complex (S185A mutant) with its substrate were resolved to the resolution of 2...
January 11, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28074337/economic-burden-of-rheumatoid-arthritis-in-italy-possible-consequences-on-anti-citrullinated-protein-antibody-positive-patients
#14
Francesco Saverio Mennini, Andrea Marcellusi, Lara Gitto, Florenzo Iannone
BACKGROUND: Rheumatoid arthritis (RA) is an autoimmune disease with a substantial medical and economic burden. In Italy, it affects approximately 280,000 people, therefore representing the musculoskeletal disease with the highest economic impact in terms of costs for the National Health Service and the social security system. OBJECTIVE: The aim of this study was to estimate the annual economic burden of RA in Italy and determine the potential cost reduction considering the most effective biologic treatment for early rapidly progressing RA (ERPRA) patients...
January 10, 2017: Clinical Drug Investigation
https://www.readbyqxmd.com/read/28072869/discovery-and-molecular-basis-of-a-diverse-set-of-polycomb-repressive-complex-2-inhibitors-recognition-by-eed
#15
Ling Li, Hailong Zhang, Man Zhang, Mengxi Zhao, Lijian Feng, Xiao Luo, Zhenting Gao, Ying Huang, Ophelia Ardayfio, Ji-Hu Zhang, Ying Lin, Hong Fan, Yuan Mi, Guobin Li, Lei Liu, Leying Feng, Fangjun Luo, Lin Teng, Wei Qi, Johannes Ottl, Andreas Lingel, Dirksen E Bussiere, Zhengtian Yu, Peter Atadja, Chris Lu, En Li, Justin Gu, Kehao Zhao
Polycomb repressive complex 2 (PRC2), a histone H3 lysine 27 methyltransferase, plays a key role in gene regulation and is a known epigenetics drug target for cancer therapy. The WD40 domain-containing protein EED is the regulatory subunit of PRC2. It binds to the tri-methylated lysine 27 of the histone H3 (H3K27me3), and through which stimulates the activity of PRC2 allosterically. Recently, we disclosed a novel PRC2 inhibitor EED226 which binds to the K27me3-pocket on EED and showed strong antitumor activity in xenograft mice model...
2017: PloS One
https://www.readbyqxmd.com/read/28072827/comprehensive-n-glycan-profiling-of-cetuximab-biosimilar-candidate-by-np-hplc-and-maldi-ms
#16
Sheng Liu, Wenjie Gao, Yao Wang, Zhenyu He, Xiaojun Feng, Bi-Feng Liu, Xin Liu
Monitoring glycosylation of the mAbs have been emphasized and routinely characterized in biopharmaceutical industries because the carbohydrate components are closely related to the safety, efficacy, and consistency of the antibodies. In this study, the comprehensive glycan profiling of a biosimilar candidate of cetuximab was successfully characterized using Normal phase high-performance liquid chromatography (NP-HPLC) in combination with Matrix assisted laser desorption/ionization mass spectrometry (MALDI-MS)...
2017: PloS One
https://www.readbyqxmd.com/read/28072824/d19s-mutation-of-the-cationic-cysteine-rich-protein-paf-novel-insights-into-its-structural-dynamics-thermal-unfolding-and-antifungal-function
#17
Christoph Sonderegger, Ádám Fizil, Laura Burtscher, Dorottya Hajdu, Alberto Muñoz, Zoltán Gáspári, Nick D Read, Gyula Batta, Florentine Marx
The cysteine-rich, cationic, antifungal protein PAF is abundantly secreted into the culture supernatant of the filamentous Ascomycete Penicillium chrysogenum. The five β-strands of PAF form a compact β-barrel that is stabilized by three disulphide bonds. The folding of PAF allows the formation of four surface-exposed loops and distinct charged motifs on the protein surface that might regulate the interaction of PAF with the sensitive target fungus. The growth inhibitory activity of this highly stable protein against opportunistic fungal pathogens provides great potential in antifungal drug research...
2017: PloS One
https://www.readbyqxmd.com/read/28069228/cu-sns-sno2-nanoparticles-as-novel-sorbent-for-dispersive-micro-solid-phase-extraction-of-atorvastatin-in-human-plasma-and-urine-samples-by-high-performance-liquid-chromatography-with-uv-detection-application-of-central-composite-design-ccd
#18
Mehdi Dastkhoon, Mehrorang Ghaedi, Arash Asfaram, Maryam Arabi, Abbas Ostovan, Alireza Goudarzi
Separation and detection of residual drug in biological fluids has directly related to human health in term of their beneficial or side effects. In biological fluid samples (complex matrix which containing drug at very low level) conduction of preliminary efficient technique as good choice for pre-concentration and clean-up of real sample before their instrumental analysis is highly recommended. In this result technique, based on nano-structure material which poses higher available surface area and larger member of reactive sites led to significant improvement in characteristic performance of analytical method...
May 2017: Ultrasonics Sonochemistry
https://www.readbyqxmd.com/read/28068466/controlling-self-assembling-peptide-hydrogel-properties-through-network-topology
#19
Jie Gao, Claire Tang, Andrew M Smith, Aline Fiona Miller, Alberto Saiani
Self-assembling peptide based hydrogels have encountered increasing interest in the recent years as scaffolds for 3D cell culture or for controlled drug delivery. One of the main challenges is the fine control of the mechanical properties of these materials. The bulk properties of hydrogel not only depend on the intrinsic properties of the fibres but also on the network topology formed. In this work we show how fibre-fibre interactions can be manipulated by design to control the final hydrogels network topology and therefore control the final properties of the material...
January 9, 2017: Biomacromolecules
https://www.readbyqxmd.com/read/28067441/a-synthetic-hybrid-molecule-for-the-selective-removal-of-human-pluripotent-stem-cells-from-cell-mixtures
#20
Di Mao, Shin Ando, Shin-Ichi Sato, Ying Qin, Nao Hirata, Yousuke Katsuda, Eihachiro Kawase, Ting-Fang Kuo, Itsunari Minami, Yuji Shiba, Kazumitsu Ueda, Norio Nakatsuji, Motonari Uesugi
A major hurdle in stem cell therapy is the tumorigenic risk of residual undifferentiated stem cells. This report describes the design and evaluation of synthetic hybrid molecules that efficiently reduce the number of human induced pluripotent stem cells (hiPSCs) in cell mixtures. The design takes advantage of Kyoto probe 1 (KP-1), a fluorescent chemical probe for hiPSCs, and clinically used anticancer drugs. Among the KP-1-drug conjugates we synthesized, we found an exceptionally selective, chemically tractable molecule that induced the death of hiPSCs...
January 9, 2017: Angewandte Chemie
keyword
keyword
101794
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"