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https://read.qxmd.com/read/30763886/anti-inflammatory-drug-approach-synthesis-and-biological-evaluation-of-novel-pyrazolo-3-4-d-pyrimidine-compounds
#1
Noor Atatreh, Amal M Youssef, Mohammad A Ghattas, Mohammad Al Sorkhy, Sara Alrawashdeh, Khaled B Al-Harbi, Ibrahim M El-Ashmawy, Tariq I Almundarij, Amani A Abdelghani, Alaa S Abd-El-Aziz
In this study, the acid chlorides of pyrazolo[3,4-d]pyrimidine compounds were prepared and reacted with a number of nucleophiles. The novel compounds were experimentally tested via enzyme assay and they showed cyclooxygenase-2 inhibition activity in the middle micro molar range (4b had a COX-1 IC50 of 26 µM and a COX-2 IC50 of 34 µM, 3b had a COX-1 IC50 of 19 µM and a COX-2 IC50 of 31 µM, 3a had a COX-2 IC50 of 42 µM). These compounds were analyzed via docking and were predicted to interact with some of the COX-2 key residues...
February 5, 2019: Bioorganic Chemistry
https://read.qxmd.com/read/30763788/an-evaluation-of-the-gliding-performance-of-solid-oral-dosage-form-film-coatings-using-an-artificial-mucous-layer
#2
Nélio Drumond, Sven Stegemann
Oral drug delivery technology is mainly provided in the form of solid oral dosage forms (SODF) that have to be swallowed intact and move throughout the oro-esophageal system to release the drug content in the stomach or intestine. As there is growing evidence for an increasing prevalence of impaired swallowing functions in certain diseases, multimorbidity and advanced age, predictive in vitro methods for the oro-esophageal gliding behavior of SODF would be very useful. The gliding performance of different SODF polymer films was investigated across an artificial mucous layer using a versatile in vitro gliding system...
February 6, 2019: Colloids and Surfaces. B, Biointerfaces
https://read.qxmd.com/read/30763772/scavenger-receptor-class-a1-mediates-uptake-of-morpholino-antisense-oligonucleotide-into-dystrophic-skeletal-muscle
#3
Shouta Miyatake, Yoshitaka Mizobe, Maria K Tsoumpra, Kenji Rowel Q Lim, Yuko Hara, Fazel Shabanpoor, Toshifumi Yokota, Shin'ichi Takeda, Yoshitsugu Aoki
Exon skipping using phosphorodiamidate morpholino oligomers (PMOs) is a promising treatment strategy for Duchenne muscular dystrophy (DMD). The most significant limitation of these clinically used compounds is their lack of delivery systems that target muscles; thus, cell-penetrating peptides are being developed to enhance uptake into muscles. Recently, we reported that uptake of peptide-conjugated PMOs into myofibers was mediated by scavenger receptor class A (SR-A), which binds negatively charged ligands...
January 25, 2019: Molecular Therapy. Nucleic Acids
https://read.qxmd.com/read/30763717/dynamic-in-vitro-models-for-tumor-tissue-engineering
#4
Daniel Karami, Nathan Richbourg, Vassilios Sikavitsas
Cancer research uses in vitro studies for controllable analysis of tumor behavior and preclinical testing of therapeutics. Shortcomings of basic cell culture systems in recreating in vivo interactions have driven the development of more efficient and biomimetic in vitro environments for cancer research. Assimilation of certain developments in tissue engineering will accelerate and improve the design of these environments. With the continual improvement of the tumor engineering field, the next step is towards macroscopic systems such as scaffold-supported, flow-perfused macroscale tumor bioreactors...
February 11, 2019: Cancer Letters
https://read.qxmd.com/read/30763201/managing-drug-interactions-with-oral-anticancer-agents-signals-noise-and-echoes
#5
R Donald Harvey
No abstract text is available yet for this article.
February 2019: Journal of Oncology Practice
https://read.qxmd.com/read/30763198/oral-anticancer-therapy-management-of-drug-interactions
#6
Britny G Rogala, Margaret M Charpentier, Michelle K Nguyen, Kaitlin M Landolf, Lamya Hamad, Kelly M Gaertner
Oral anticancer therapy is increasingly integrated into the care of patients with cancer. Recognition and management of drug-drug interactions (DDIs) is critical to providing efficacious and safe anticancer treatment. DDIs with QTc-prolonging agents, anticoagulants, enzyme inducers and inhibitors, antidepressants, and acid suppressants are commonly encountered with anticancer therapies. Here, we review frequently observed DDIs and outline literature-supported suggestions for their management.
February 2019: Journal of Oncology Practice
https://read.qxmd.com/read/30763080/ranking-reversible-covalent-drugs-from-free-energy-perturbation-to-fragment-docking
#7
Han Zhang, Wenjuan Jiang, Payal Chatterjee, Yun Luo
Reversible covalent inhibitors have drawn increasing attention in drug design, as they are likely more potent than noncovalent inhibitors and less toxic than covalent inhibitors. Despite those advantages, the computational prediction of reversible covalent binding presents a formidable challenge because the binding process consists of multiple steps and quantum mechanics (QM) level calculation is needed to estimate the covalent binding free energy. It has been shown that the dissociation rates and the equilibrium dissociation constants vary significantly even with similar warheads, due to noncovalent interactions...
February 14, 2019: Journal of Chemical Information and Modeling
https://read.qxmd.com/read/30763071/nanovector-mediated-drug-delivery-in-spinal-cord-injury-a-multitarget-approach
#8
Simonetta Papa, Filippo Rossi, Irma Vismara, Gianluigi Forloni, Pietro Veglianese
Many pre-clinical studies seek cures for spinal cord injury (SCI) but when the results are translated to clinical trials they give scant efficacy. One possible reason is that most strategies use treatments directed toward a single pathological mechanism, while a multitherapeutic approach needs to be tested to significantly improve outcomes after SCI. Most of the pre-clinical reports gave better outcomes when a combination of different compounds was used instead of a single drug. This promising approach, however, must still be improved because it raises some criticism: i) the Blood-Spinal Cord barrier limits drug distribution, ii) it is hard to understand the interactions among the pharmacological components after systemic administration, iii) the timing of treatments is crucial: the spread of the lesion is a process finely regulated over time, so therapies must be scheduled at precise times during the post-injury course...
February 14, 2019: ACS Chemical Neuroscience
https://read.qxmd.com/read/30762518/influenza-virus-entry-via-the-gm3-ganglioside-mediated-platelet-derived-growth-factor-receptor-%C3%AE-signalling-pathway
#9
Pieter Vrijens, Sam Noppen, Talitha Boogaerts, Els Vanstreels, Roberto Ronca, Paola Chiodelli, Manon Laporte, Evelien Vanderlinden, Sandra Liekens, Annelies Stevaert, Lieve Naesens
The possible resistance of influenza virus against existing antiviral drugs calls for new therapeutic concepts. One appealing strategy is to inhibit virus entry, in particular at the stage of internalization. This requires a better understanding of virus-host interactions during the entry process, including the role of receptor tyrosine kinases (RTKs). To search for cellular targets, we evaluated a panel of 276 protein kinase inhibitors in a multicycle antiviral assay in Madin-Darby canine kidney cells. The RTK inhibitor Ki8751 displayed robust anti-influenza A and B virus activity and was selected for mechanistic investigations...
February 14, 2019: Journal of General Virology
https://read.qxmd.com/read/30762327/drug-interaction-is-the-cornerstone-of-modern-anaesthesia-practice
#10
Chien-Kun Ting
No abstract text is available yet for this article.
February 13, 2019: Minerva Anestesiologica
https://read.qxmd.com/read/30761756/carbon-dots-in-matrix-boosting-intriguing-luminescence-properties-and-applications
#11
REVIEW
Jiyang Li, Bolun Wang, Hongyue Zhang, Jihong Yu
As a new class of luminescent nanomaterials, carbon dots (CDs) have aroused significant interest because of their fascinating photoluminescence properties and potential applications in biological, optoelectronic, and energy-related fields. Strikingly, embedding CDs in host matrices endow them with intriguing luminescent properties, in particular, room temperature phosphorescence and thermally activated delayed fluorescence, due to the confinement effect of the host matrix and the H-bonding interactions between CDs and the matrix...
February 13, 2019: Small
https://read.qxmd.com/read/30761294/cancer-cell-targeting-with-functionalized-quantum-dot-encoded-polyelectrolyte-microcapsules
#12
Galina Nifontova, Fernanda Ramos-Gomes, Maria Baryshnikova, Frauke Alves, Igor Nabiev, Alyona Sukhanova
Imaging agents and drug carriers are commonly targeted toward cancer cell through functionalization with specific recognition molecules. Quantum dots (QDs) are fluorescent semiconductor nanocrystals whose extraordinary brightness and photostability make them attractive for direct fluorescent labeling of biomolecules or optical encoding of the membranes and cells. Here, we analyse the cytotoxicity of QD-encoded microcapsules, validate an approach to the activation of the microcapsule's surface for further functionalization with monoclonal antibody Trastuzumab, a humanized monoclonal antibody targeting the extracellular domain of the human epidermal growth factor receptor 2 (HER2) and already in clinical use for the treatment of HER2 positive breast cancer...
2019: Frontiers in Chemistry
https://read.qxmd.com/read/30761293/insight-into-the-binding-mechanism-of-p53-pdiq-mdmx-mdm2-with-the-interaction-entropy-method
#13
Mengxin Li, Yalong Cong, Yuchen Li, Susu Zhong, Ran Wang, Hao Li, Lili Duan
The study of the p53-MDMX/MDM2 binding sites is a research hotspot for tumor drug design. The inhibition of p53-targeted MDMX/MDM2 has become an effective approach in anti-tumor drug development. In this paper, a theoretically rigorous and computationally accurate method, namely, the interaction entropy (IE) method, combined with the polarized protein-specific charge (PPC) force field, is used to explore the difference in the binding mechanism between p53-MDMX and p53-MDM2. The interaction of a 12mer peptide inhibitor (pDIQ), which is similar to p53 in structure, with MDMX/MDM2 is also studied...
2019: Frontiers in Chemistry
https://read.qxmd.com/read/30760870/runx-proteins-desensitize-multiple-myeloma-to-lenalidomide-via-protecting-ikzfs-from-degradation
#14
Nan Zhou, Alvaro Gutierrez-Uzquiza, Xiang Yu Zheng, Renxu Chang, Dan T Vogl, Alfred L Garfall, Luca Bernabei, Anita Saraf, Laurence Florens, Michael P Washburn, Anuradha Illendula, John H Bushweller, Luca Busino
Ikaros family zinc finger protein 1 and 3 (IKZF1 and IKZF3) are transcription factors that promote multiple myeloma (MM) proliferation. The immunomodulatory imide drug (IMiD) lenalidomide promotes myeloma cell death via Cereblon (CRBN)-dependent ubiquitylation and proteasome-dependent degradation of IKZF1 and IKZF3. Although IMiDs have been used as first-line drugs for MM, the overall survival of refractory MM patients remains poor and demands the identification of novel agents to potentiate the therapeutic effect of IMiDs...
February 13, 2019: Leukemia: Official Journal of the Leukemia Society of America, Leukemia Research Fund, U.K
https://read.qxmd.com/read/30760838/synthesis-and-antibiotic-activity-of-novel-acylated-phloroglucinol-compounds-against-methicillin-resistant-staphylococcus-aureus
#15
Navriti Mittal, Haben H Tesfu, Andrew M Hogan, Silvia T Cardona, John L Sorensen
The rise in antibiotic resistance among pathogenic microorganisms has created an imbalance in the drugs available for treatment, in part due to the slow development of new antibiotics. Cystic fibrosis (CF) patients are highly susceptible to antibiotic-resistant pathogens, including methicillin-resistant Staphylococcus aureus (MRSA). Phloroglucinols and related polyketide natural products have demonstrated antimicrobial activity against a number of Gram-positive bacteria including S. aureus. In this study, we investigated a series of acylated phloroglucinol derivatives to determine their potential as lead compounds for the design of novel therapeutics...
February 13, 2019: Journal of Antibiotics
https://read.qxmd.com/read/30760803/the-cyclic-peptide-labaditin-does-not-alter-the-outer-membrane-integrity-of-salmonella-enterica-serovar-typhimurium
#16
Simone C Barbosa, Thatyane M Nobre, Diogo Volpati, Eduardo M Cilli, Daniel S Correa, Osvaldo N Oliveira
Antimicrobial peptides are a promising class of new antibiotics with the ability to kill bacteria by disrupting their cell membrane, which is especially difficult for Gram-negative bacteria whose cell wall contains an outer layer of lipopolysaccharides (LPS). Here we show that the cyclic decapeptide Labaditin (Lo), with proven activity against the Gram-positive Staphylococcus aureus and Streptococcus mutans, is not able to kill the Gram-negative Salmonella enterica serovar Typhimurium (S.e.s. Typhimurium). We found that Lo induced significant changes in the surface pressure isotherms of Langmuir monolayers representing the Salmonella enterica serovar Typhimurium inner membrane (S...
February 13, 2019: Scientific Reports
https://read.qxmd.com/read/30760797/phencynonate-s-isomer-as-a-eutomer-is-a-novel-central-anticholinergic-drug-for-anti-motion-sickness
#17
Pingxiang Xu, Ying Liu, Liyun Wang, Yi Wu, Xuelin Zhou, Junhai Xiao, Jianquan Zheng, Ming Xue
To compare and evaluate the differences of stereoselective activity, the binding affinity, metabolism, transport and molecular docking of phencynonate isomers to muscarinic acetylcholine receptor (mAChR) were investigated in this study. The rotation stimulation and locomotor experiments were used to evaluate anti-motion sickness effects. The competitive affinity with [3 H]-QNB and molecular docking were used for studying the interactions between the two isomers and mAChR. The stereoselective mechanism of isomers was investigated by incubation with rat liver microsomes, a protein binding assay and membrane permeability assay across a Caco-2 cell monolayer using a chiral column HPLC method...
February 13, 2019: Scientific Reports
https://read.qxmd.com/read/30760721/improvement-of-antibody-functionality-by-structure-guided-paratope-engraftment
#18
Qingbo Liu, Yen-Ting Lai, Peng Zhang, Mark K Louder, Amarendra Pegu, Reda Rawi, Mangaiarkarasi Asokan, Xuejun Chen, Chen-Hsiang Shen, Gwo-Yu Chuang, Eun Sung Yang, Huiyi Miao, Yuge Wang, Anthony S Fauci, Peter D Kwong, John R Mascola, Paolo Lusso
Broadly neutralizing antibodies (bNAbs) represent a promising alternative to antiretroviral drugs for HIV-1 prevention and treatment. Selected antibodies to the CD4-binding site bolster envelope trimer binding via quaternary contacts. Here, we rationally engraft a new paratope, i.e., the extended heavy-chain framework region 3 (FR3) loop of VRC03, which mediates quaternary interaction, onto several potent bNAbs, enabling them to reach an adjacent gp120 protomer. The interactive quaternary surface is delineated by solving the crystal structure of two FR3 loop-chimeric antibodies...
February 13, 2019: Nature Communications
https://read.qxmd.com/read/30760618/oral-treatment-with-bt-11-ameliorates-inflammatory-bowel-disease-by-enhancing-regulatory-t-cell-responses-in-the-gut
#19
Andrew Leber, Raquel Hontecillas, Victoria Zoccoli-Rodriguez, Jyoti Chauhan, Josep Bassaganya-Riera
Inflammatory bowel disease (IBD) is an expanding autoimmune disease afflicting millions that remains difficult to treat due to the accumulation of multiple immunological changes. BT-11 is an investigational new drug for IBD that is orally active, gut restricted, and targets the lanthionine synthetase C-like 2 immunometabolic pathway. CD25+ FOXP3+ CD4+ T cells are increased locally within the colon of BT-11-treated mice in Citrobacter rodentium and IL-10-/- mouse models of colitis. The maintained efficacy of BT-11 in the absence of IL-10 combined with the loss of efficacy when direct cell-cell interactions are prevented suggest that the regulatory T cell (Treg)-related elements of suppression are cell contact-mediated...
February 13, 2019: Journal of Immunology: Official Journal of the American Association of Immunologists
https://read.qxmd.com/read/30760577/hiv-1-subtype-c-with-pyxe-insertion-has-enhanced-binding-of-gag-p6-to-host-cell-protein-alix-and-increased-replication-fitness
#20
Robert van Domselaar, Duncan T Njenda, Rohit Rao, Anders Sönnerborg, Kamalendra Singh, Ujjwal Neogi
Human immunodeficiency virus type 1 subtype C (HIV-1C) has a natural deletion of a YPxL motif in its Gag-p6 late domain. This domain mediates the binding of Gag to host cell protein ALIX and subsequently facilitates viral budding. In a subset of HIV-1C infected individuals, the tetrapeptide insertion PYxE has been identified at the deleted YPxL motif site. Here, we report the consequences of PYxE insertion on the interaction with ALIX and the relevance regarding replication fitness and drug sensitivity. In our three HIV-1C cohorts, PYKE and PYQE were most prevalent among PYxE variants...
February 13, 2019: Journal of Virology
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