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https://www.readbyqxmd.com/read/28549582/crystal-structure-of-spsb2-in-complex-with-a-rational-designed-rgd-containing-cyclic-peptide-inhibitor-of-spsb2-inos-interaction
#1
Tingting You, Yuhui Wang, Kefa Li, Danting Zhang, Huan Wei, Yanhong Luo, Hua Li, Yongzhi Lu, Xunchen Su, Zhihe Kuang
SPRY domain-containing SOCS box protein 2 (SPSB2) is a negative regulator of inducible nitric oxide synthase (iNOS) that modulates the lifetime of iNOS and thus the levels of nitric oxide (NO) production. Inhibitors that can disrupt the endogenous SPSB2-iNOS interaction and augment NO production have potential as novel antimicrobial and anticancer drugs. In this study, we have designed a cyclic peptide (cR8), containing an RGD motif and the SPSB2 binding motif (DINNNV). ITC and chemical shift perturbation showed that cR8 binds to the iNOS binding site on SPSB2 with a Kd of 671 nM, and saturation transfer difference NMR showed that cR8 binds to αvβ3 integrin-expressing cells...
May 23, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/28546540/a-bioactive-chemical-markers-based-strategy-for-quality-assessment-of-botanical-drugs-xuesaitong-injection-as-a-case-study
#2
Zhenzhong Yang, Qing Shao, Zhiwei Ge, Ni Ai, Xiaoping Zhao, Xiaohui Fan
Current chemical markers based quality assessment methods largely fail to reflect intrinsic chemical complexity and multiple mechanisms of action of botanical drugs (BD). The development of novel quality markers is greatly needed. Here we propose bioactive chemical markers (BCM), defined as a group of chemo-markers that exhibit similar pharmacological activities comparable to the whole BD, which can therefore be used to effectively assess the quality of BD. As a proof-of-concept, a BCM-based strategy was developed and applied to Xuesaitong Injection (XST) for assessing the efficacy and consistency of different batches...
May 25, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28545238/epigenetic-strategies-to-boost-cancer-immunotherapies
#3
REVIEW
Maria J Barrero
Recently, immunotherapeutic approaches have shown impressive responses in a subset of cancer patients. However, the rate of success is low and a large percentage of treated patients do not experience clinical benefits. Therefore, additional strategies are needed to improve responses and select responsive patients. Emerging data suggest that epigenetic drugs can improve the responses to immunotherapy. Understanding the mechanisms of resistance to immunotherapy and the epigenetic events that take place during immune evasion is critical to providing a rational combined use of immunotherapies and epigenetic drugs...
May 23, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28544082/a-resource-of-potential-drug-targets-and-strategic-decision-making-for-obstructive-sleep-apnoea-pharmacotherapy
#4
REVIEW
Richard L Horner, Kevin P Grace, Andrew Wellman
There is currently no pharmacotherapy for obstructive sleep apnoea (OSA) but there is no principled a priori reason why there should not be one. This review identifies a rational decision-making strategy with the necessary logical underpinnings that any reasonable approach would be expected to navigate to develop a viable pharmacotherapy for OSA. The process first involves phenotyping an individual to quantify and characterize the critical predisposing factor(s) to their OSA pathogenesis and identify, a priori, if the patient is likely to benefit from a pharmacotherapy that targets those factors...
May 25, 2017: Respirology: Official Journal of the Asian Pacific Society of Respirology
https://www.readbyqxmd.com/read/28543088/3d-quantitative-structure-activity-relationship-and-docking-studies-of-coumarin-derivatives-as-tissue-kallikrein-7-inhibitors
#5
Xin Zheng, Mengxi He, Xiao Tan, Jun Zheng, Fangyu Wang, Sen Liu
OBJECTIVES: Kallikrein 7 (KLK7) is a secreted serine protease that plays important roles in skin desquamation and tumour progression, which makes it an attracting drug target. To guide the design of KLK7 inhibitors, a series of coumarin-based inhibitors were used to perform 3D-quantitative structure-activity relationship analysis. METHODS: 3D conformations of 37 inhibitors were generated and used to construct CoMFA and CoMSIA models. Then a complex model between the inhibitors and KLK7 was built with molecular docking...
May 23, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28542609/potent-and-selective-inhibition-of-pathogenic-viruses-by-engineered-ubiquitin-variants
#6
Wei Zhang, Ben A Bailey-Elkin, Robert C M Knaap, Baldeep Khare, Tim J Dalebout, Garrett G Johnson, Puck B van Kasteren, Nigel J McLeish, Jun Gu, Wenguang He, Marjolein Kikkert, Brian L Mark, Sachdev S Sidhu
The recent Middle East respiratory syndrome coronavirus (MERS-CoV), Ebola and Zika virus outbreaks exemplify the continued threat of (re-)emerging viruses to human health, and our inability to rapidly develop effective therapeutic countermeasures. Many viruses, including MERS-CoV and the Crimean-Congo hemorrhagic fever virus (CCHFV) encode deubiquitinating (DUB) enzymes that are critical for viral replication and pathogenicity. They bind and remove ubiquitin (Ub) and interferon stimulated gene 15 (ISG15) from cellular proteins to suppress host antiviral innate immune responses...
May 18, 2017: PLoS Pathogens
https://www.readbyqxmd.com/read/28541029/homochiral-mof-as-circular-dichroism-sensor-for-enantioselective-recognition-on-nature-and-chirality-of-unmodified-amino-acids
#7
Yan-Wu Zhao, Yan Wang, Xian-Ming Zhang
Self-assembly of zinc salt with rationally designed chiral ligand, (1R,2R)-2-(pyridine-4-yl carbamoyl) cyclohexanecarboxylic acid (RR-PCCH) generated 2D homochiral metal-organic framework [Zn(RR-PCCHC)2] (HMOF-1) that is composed of DNA-like right-handed double-helix structure. HMOF-1 shows high solvent and thermal stability and is also stable in neutral, weak acidic and weak basic aqueous solution. Emulsified HMOF-1 shows strong inherent circular dichroism (CD) signal in aqueous solution, which can show regular intensity change by induction of amino acids...
May 25, 2017: ACS Applied Materials & Interfaces
https://www.readbyqxmd.com/read/28540671/multidisciplinary-management-of-mycosis-fungoides-s%C3%A3-zary-syndrome
#8
REVIEW
Sara Berg, Jennifer Villasenor-Park, Paul Haun, Ellen J Kim
PURPOSE OF REVIEW: Diagnosis and management of mycosis fungoides and Sézary syndrome (MF/SS) require accurate clinicopathological correlation and a multidisciplinary approach. We reviewed major advances in the field regarding diagnostic and prognostic tools as well as skin-directed therapies (SDTs) and systemic agents for MF/SS published in the past 2 years. RECENT FINDINGS: Improved technology (T-cell receptor high-throughput sequencing) and increased multicenter collaboration (Cutaneous Lymphoma International Consortium) have led to diagnostic/prognostic advances...
May 24, 2017: Current Hematologic Malignancy Reports
https://www.readbyqxmd.com/read/28540638/in-silico-dose-prediction-for-long-acting-rilpivirine-and-cabotegravir-administration-to-children-and-adolescents
#9
Rajith K R Rajoli, David J Back, Steve Rannard, Caren Freel Meyers, Charles Flexner, Andrew Owen, Marco Siccardi
BACKGROUND AND OBJECTIVES: Long-acting injectable antiretrovirals represent a pharmacological alternative to oral formulations and an innovative clinical option to address adherence and reduce drug costs. Clinical studies in children and adolescents are characterised by ethical and logistic barriers complicating the identification of dose optimisation. Physiologically-based pharmacokinetic modelling represents a valuable tool to inform dose finding prior to clinical trials. The objective of this study was to simulate potential dosing strategies for existing long-acting injectable depot formulations of cabotegravir and rilpivirine in children and adolescents (aged 3-18 years) using physiologically-based pharmacokinetic modelling...
May 24, 2017: Clinical Pharmacokinetics
https://www.readbyqxmd.com/read/28539738/the-mealiness-and-quality-of-herbal-medicine-licorice-for-example
#10
Xueying Liu, Weilong Hou, Deqiang Dou
BACKGROUND: The morphological identification is an effective and simple quality evaluation method in Chinese drugs, and the traits of mealiness and color were widely used in the commercial market of Chinese drugs. OBJECTIVE: The objective of this study was to explore the correlation between mealiness of herbal drugs and its quality; licorice was selected as an example. MATERIALS AND METHODS: The mealiness of licorice was graded by its weight; meanwhile, the content of glycyrrhizic acid and liquiritin was determined by high-performance liquid chromatography-diode-array detection method; the content of polysaccharides, soluble sugars, pectin, total starch, amylose, and amylopectin was measured by colorimetric method; and the number and diameter of starch granule were observed by microscope...
April 2017: Pharmacognosy Research
https://www.readbyqxmd.com/read/28537430/multifaceted-roles-of-glutathione-and-glutathione-based-systems-in-carcinogenesis-and-anticancer-drug-resistance
#11
Elie Hatem, Nadine El Banna, Meng-Er Huang
SIGNIFICANCE: Glutathione is the most abundant antioxidant molecule in living organisms and has multiple functions. Intracellular glutathione homeostasis, through its synthesis, consumption, and degradation is an intricately balanced process. Glutathione levels are often high in tumor cells prior to treatment and there is a strong correlation between elevated levels of intracellular glutathione/sustained glutathione-mediated redox activity and resistance to pro-oxidant anticancer therapy...
May 24, 2017: Antioxidants & Redox Signaling
https://www.readbyqxmd.com/read/28535898/treatment-of-postmenopausal-osteoporosis-a-literature-based-algorithm-for-use-in-the-public-health-care-system
#12
Ellen Luz Pereira Caires, Mailze Campos Bezerra, Ana Flávia Torquato de Araújo Junqueira, Sheila Márcia de Araújo Fontenele, Silvana Cristina de Albuquerque Andrade, Catarina Brasil d'Alva
Bisphosphonates are considered first-line agents in the treatment of postmenopausal osteoporosis based on extensive experience of use, safety, and proven efficacy in reducing vertebral, non-vertebral and femur fractures. However, post-marketing reports based on the treatment of millions of patients/year over lengthy periods of time have revealed the occurrence of initially unexpected adverse effects, such as osteonecrosis of the jaw and atypical femoral fracture, leading to the restriction of treatment duration with bisphosphonates by global regulatory agencies...
May 2017: Revista Brasileira de Reumatologia
https://www.readbyqxmd.com/read/28533225/multi-functional-effects-of-a-small-molecule-stat3-inhibitor-on-nash-and-hcc-in-mice
#13
Kwang Hwa Jung, Wonbeak Yoo, Heather L Stevenson, Dipti Deshpande, Hong Shen, Mihai Gagea, Suk-Young Yoo, Jing Wang, Thomas Kris Eckols, Uddalak Bharadwaj, David J Tweardy, Laura Beretta
The incidence of hepatocellular carcinoma (HCC) is increasing in the United States and liver cancer is the second leading cause of cancer-related mortality worldwide. Non-alcoholic steatohepatitis (NASH) is becoming an important risk for HCC and most patients with HCC have underlying liver cirrhosis and compromised liver function, which limit treatment options. Thus, novel therapeutic strategies to prevent or treat HCC in the context of NASH and cirrhosis are urgently needed. <br /><br />Experimental Design: Constitutive activation of signal transducer and activator of transcription 3 (STAT3) is frequently detected in HCC tumors...
May 22, 2017: Clinical Cancer Research: An Official Journal of the American Association for Cancer Research
https://www.readbyqxmd.com/read/28532474/detection-of-ikk%C3%AE%C2%B5-by-immunohistochemistry-in-primary-breast-cancer-association-with-egfr-expression-and-absence-of-lymph-node-metastasis
#14
Virginie Williams, Andrée-Anne Grosset, Natalia Zamorano Cuervo, Yves St-Pierre, Marie-Pierre Sylvestre, Louis Gaboury, Nathalie Grandvaux
BACKGROUND: IKKε is an oncogenic kinase that was found amplified and overexpressed in a substantial percentage of human breast cancer cell lines and primary tumors using genomic and gene expression analyses. Molecular studies have provided the rational for a key implication of IKKε in breast cancer cells proliferation and invasiveness through the phosphorylation of several substrates. METHODS: Here, we performed immunohistochemical detection of IKKε expression on tissue microarrays constituted of 154 characterized human breast cancer tumors...
May 22, 2017: BMC Cancer
https://www.readbyqxmd.com/read/28532298/ctbp-an-emerging-oncogene-and-novel-small-molecule-drug-target-advances-in-the-understanding-of-its-oncogenic-action-and-identification-of-therapeutic-inhibitors
#15
M Michael Dcona, Benjamin L Morris, Keith C Ellis, Steven R Grossman
C-terminal Binding Proteins (CtBP) 1 and 2 are oncogenic transcriptional co-regulators overexpressed in many cancer types, with their expression level correlating to worse prognostic outcomes and aggressive tumor features. CtBP negatively regulates the expression of many tumor suppressor genes, while coactivating genes that promote proliferation, epithelial-mesenchymal transition, and cancer stem cell self-renewal activity. In light of this evidence, the development of novel inhibitors that mitigate CtBP function may provide clinically actionable therapeutic tools...
May 22, 2017: Cancer Biology & Therapy
https://www.readbyqxmd.com/read/28530543/using-properties-of-tumor-microenvironments-for-controlling-local-on-demand-delivery-from-biopolymer-based-nanocarriers
#16
Abdullah K Alshememry, Suleiman S El-Tokhy, Larry D Unsworth
BACKGROUND: The 'tumor microenvironment' comprised of tumor cells, non-malignant stromal tissues, signaling molecules and the extracellular matrix. Tumor microenvironment has unique physical and physiological characteristics including vascular abnormalities, hypoxia, acidic pH, specific enzymes and growth factors upregulation and high reducing potential. It is these endogenous properties of the tumor environment that can be used to trigger the release of cancer therapeutics both locally and as a function of disease state...
May 21, 2017: Current Pharmaceutical Design
https://www.readbyqxmd.com/read/28530401/rational-design-of-mof-nanocarrier-based-co-delivery-system-of-doxorubicin-hydrochloride-verapamil-hydrochloride-for-overcoming-multidrug-resistance-with-efficient-targeted-cancer-therapy
#17
Huiyuan Zhang, Wei Jiang, Ruiling Liu, Jing Zhang, Di Zhang, Zhonghao Li, Yuxia Luan
Conventional organic and inorganic drug nanocarriers suffer from serious drawbacks, such as low drug-storage capacity and uncontrolled release. Moreover, multidrug resistance (MDR) has been one of the primary causes leading to chemotherapy failure for cancers. The main reason of MDR is the overexpressed active efflux transporters such as P-glycoprotein. Here, zeolitic imidazolate framework ZIF-8, as one of the biocompatible metal organic frameworks (MOFs), is reported for the first time as the multidrug carrier to realize the efficient co-delivery of verapamil hydrochloride (VER) as the P-glycoprotein inhibitor as well as doxorubicin hydrochloride (DOX) as an anticancer drug to overcome the MDR in addition to realizing the active targeted ability for an efficient anticancer effect...
May 22, 2017: ACS Applied Materials & Interfaces
https://www.readbyqxmd.com/read/28528519/il-6-blockade-in-the-management-of-non-infectious-uveitis
#18
Giuseppe Lopalco, Claudia Fabiani, Jurgen Sota, Orso Maria Lucherini, Gian Marco Tosi, Bruno Frediani, Florenzo Iannone, Mauro Galeazzi, Rossella Franceschini, Donato Rigante, Luca Cantarini
Several pathogenetic studies have paved the way for a newer more rational therapeutic approach to non-infectious uveitis, and treatment of different forms of immune-driven uveitis has drastically evolved in recent years after the advent of biotechnological drugs. Tumor necrosis factor-α targeted therapies, the first-line recommended biologics in uveitis, have certainly led to remarkable results in patients with non-infectious uveitis. Nevertheless, the decision-making process turns out to be extremely difficult in anti-tumor necrosis factor or multidrug-resistant cases...
May 20, 2017: Clinical Rheumatology
https://www.readbyqxmd.com/read/28528286/assessing-the-stable-conformations-of-ibuprofen-in-solution-by-means-of-residual-dipolar-couplings
#19
Maria Enrica Di Pietro, Giorgio Celebre, Christie Aroulanda, Denis Merlet, Giuseppina De Luca
Detailing the conformational equilibria between global and local minimum energy structures of anti-inflammatory α-arylpropionic acids directly in solution is of the utmost importance for a better understanding of the structure-activity relationships, hence providing valuable clues for rational structure-based drug design studies. Here the conformational preferences of the widely used pharmaceutical ibuprofen were investigated in solution by NMR spectroscopy in weakly ordering phases. A thorough theoretical treatment of the anisotropic interactions that are relevant for NMR spectra led to a conformational model characterized by six pairs of symmetry-related conformers, in particular four couples of gauche structures, with a total probability of 93%, and 2 couples of trans structures, counting for the remaining 7%...
May 17, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28526836/characterisation-of-antibiotic-prescriptions-for-acute-respiratory-tract-infections-in-danish-general-practice-a-retrospective-registry-based-cohort-study
#20
Rune Aabenhus, Malene Plejdrup Hansen, Laura Trolle Saust, Lars Bjerrum
Inappropriate use of antibiotics is contributing to the increasing rates of antimicrobial resistance. Several Danish guidelines on antibiotic prescribing for acute respiratory tract infections in general practice have been issued to promote rational prescribing of antibiotics, however it is unclear if these recommendations are followed. We aimed to characterise the pattern of antibiotic prescriptions for patients diagnosed with acute respiratory tract infections, by means of electronic prescriptions, labeled with clinical indications, from Danish general practice...
May 19, 2017: NPJ Primary Care Respiratory Medicine
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