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https://www.readbyqxmd.com/read/29333270/lessons-from-ten-years-of-genome-wide-association-studies-of-asthma
#1
REVIEW
Cristina T Vicente, Joana A Revez, Manuel A R Ferreira
Twenty-five genome-wide association studies (GWAS) of asthma were published between 2007 and 2016, the largest with a sample size of 157242 individuals. Across these studies, 39 genetic variants in low linkage disequilibrium (LD) with each other were reported to associate with disease risk at a significance threshold of P<5 × 10-8, including 31 in populations of European ancestry. Results from analyses of the UK Biobank data (n=380 503) indicate that at least 28 of the 31 associations reported in Europeans represent true-positive findings, collectively explaining 2...
December 2017: Clinical & Translational Immunology
https://www.readbyqxmd.com/read/29333045/in-vitro-antiproliferative-effect-of-earthworm-coelomic-fluid-of-eudrilus-eugeniae-eisenia-foetida-and-perionyx-excavatus-on-squamous-cell-carcinoma-9-cell-line-a-pilot-study
#2
Dominic Augustine, Roopa S Rao, Jayaraman Anbu, K N Chidambara Murthy
Introduction: The earthworm coelomic fluid (ECF) has shown proven antiproliferative effect against breast, liver, gastrointestinal, and brain cancer, but it is least explored in oral cancer. The present in vitro study is an attempt to investigate the antiproliferative activity of ECF on oral cancer cell line squamous cell carcinoma (SCC)-9. Materials and Methods: ECF was collected from the species Eudrilus eugeniae (EE), Eisenia foetida (EF), and Perionyx excavatus (PE) stored at -80°C...
December 2017: Pharmacognosy Research
https://www.readbyqxmd.com/read/29332599/the-synthesis-of-chalcones-as-anticancer-prodrugs-and-their-bioactivation-in-cyp1-expressing-breast-cancer-cells
#3
Ketan Ruparelia, Keti Zeka, Randolph R Arroo, Kenneth J M Beresford
BACKGROUND: Although the expression levels of many P450s differ between tumour and corresponding normal tissue, CYP1B1 is one of the few CYP subfamilies which is significantly and consistently overexpressed in tumours. CYP1B1 has been shown to be active within tumours and is capable of metabolising a structurally diverse range of anticancer drugs. Because of this, and its role in the activation of procarcinogens, CYP1B1 is seen as an important target for anticancer drug development. OBJECTIVES: To synthesise a series of chalcone derivatives based on the chemopreventative agent DMU-135 and investigate their antiproliferative activities in human breast cancer cell lines which express CYP1B1 and CYP1A1...
January 12, 2018: Medicinal Chemistry
https://www.readbyqxmd.com/read/29330855/getting-innovative-therapies-faster-to-patients-at-the-right-dose-impact-of-quantitative-pharmacology-towards-first-registration-and-expanding-therapeutic-use
#4
Satyaprakash Nayak, Oliver Sander, Nidal Al-Huniti, Dinesh de Alwis, Anne Chain, Marylore Chenel, Soujanya Sunkaraneni, Shruti Agrawal, Neeraj Gupta, Sandra A G Visser
Quantitative pharmacology (QP) applications in translational medicine, drug-development, and therapeutic use were crowd-sourced by the ASCPT Impact and Influence initiative. Highlighted QP case studies demonstrated faster access to innovative therapies for patients through 1) rational dose selection for pivotal trials; 2) reduced trial-burden for vulnerable populations; or 3) simplified posology. Critical success factors were proactive stakeholder engagement, alignment on the value of model-informed approaches, and utilizing foundational clinical pharmacology understanding of the therapy...
January 13, 2018: Clinical Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/29330127/present-drug-likeness-filters-in-medicinal-chemistry-during-the-hit-and-lead-optimization-process-how-far-can-they-be-simplified
#5
REVIEW
Serge Mignani, João Rodrigues, Helena Tomas, Rachid Jalal, Parvinder Pal Singh, Jean-Pierre Majoral, Ram A Vishwakarma
During the past decade, decreasing the attrition rate of drug development candidates reaching the market has become one of the major challenges in pharmaceutical research and drug development (R&D). To facilitate the decision-making process, and to increase the probability of rapidly finding and developing high-quality compounds, a variety of multiparametric guidelines, also known as rules and ligand efficiency (LE) metrics, have been developed. However, what are the 'best' descriptors and how far can we simplify these drug-likeness prediction tools in terms of the numerous, complex properties that they relate to?...
January 9, 2018: Drug Discovery Today
https://www.readbyqxmd.com/read/29330093/designing-improved-active-peptides-for-therapeutic-approaches-against-infectious-diseases
#6
REVIEW
Bárbara Gomes, Marcelo T Augusto, Mário R Felício, Axel Hollmann, Octávio L Franco, Sónia Gonçalves, Nuno C Santos
Infectious diseases are one of the main causes of human morbidity and mortality. In the last few decades, pathogenic microorganisms' resistance to conventional drugs has been increasing, and it is now pinpointed as a major worldwide health concern. The need to search for new therapeutic options, as well as improved treatment outcomes, has therefore increased significantly, with biologically active peptides representing a new alternative. A substantial research effort is being dedicated towards their development, especially due to improved biocompatibility and target selectivity...
January 9, 2018: Biotechnology Advances
https://www.readbyqxmd.com/read/29328995/filter-base-a-web-accessible-chemical-database-for-small-compound-libraries
#7
Baban S Kolte, Sanjay R Londhe, Bhushan R Solanki, Rajesh N Gacche, Rohan J Meshram
Finding novel chemical agents for targeting disease associated drug targets often requires screening of large number of new chemical libraries. In silico methods are generally implemented at initial stages for virtual screening. Filtering of such compound libraries on physicochemical and substructure ground is done to ensure elimination of compounds with undesired chemical properties. Filtering procedure, is redundant, time consuming and requires efficient bioinformatics/computer manpower along with high end software involving huge capital investment that forms a major obstacle in drug discovery projects in academic setup...
January 6, 2018: Journal of Molecular Graphics & Modelling
https://www.readbyqxmd.com/read/29328990/the-amyloidogenicity-of-the-influenza-virus-pb1-derived-peptide-sheds-light-on-its-antiviral-activity
#8
Yana A Zabrodskaya, Dmitry V Lebedev, Marja A Egorova, Aram A Shaldzhyan, Alexey V Shvetsov, Alexander I Kuklin, Daria S Vinogradova, Nikolay V Klopov, Oleg V Matusevich, Taisiia A Cheremnykh, Rajeev Dattani, Vladimir V Egorov
The influenza virus polymerase complex is a promising target for new antiviral drug development. It is known that, within the influenza virus polymerase complex, the PB1 subunit region from the 1st to the 25th amino acid residues has to be is in an alpha-helical conformation for proper interaction with the PA subunit. We have previously shown that PB1(6-13) peptide at low concentrations is able to interact with the PB1 subunit N-terminal region in a peptide model which shows aggregate formation and antiviral activity in cell cultures...
January 8, 2018: Biophysical Chemistry
https://www.readbyqxmd.com/read/29328503/challenges-and-opportunities-with-oncology-drug-development-in-china
#9
REVIEW
Gaurav Bajaj, Manish Gupta, Hwei-Gene Heidi Wang, Jeffrey S Barrett, Matthew Tan, Katrin Rupalla, Richard Bertz, Jennifer Sheng
No abstract text is available yet for this article.
January 12, 2018: Clinical Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/29328380/role-of-the-pi3k%C3%A2-akt%C3%A2-mtor-pathway-in-hepatitis-b-virus-infection-and-replication
#10
Kunlun Xiang, Bin Wang
The replication of hepatitis B virus (HBV) may be modulated by a variety of cell signaling pathways, including the phosphatidylinositol 3‑kinase (PI3K)‑RAC‑α serine/threonine‑protein kinase (AKT)‑serine/threonine‑protein kinase mTOR (mTOR) pathway. The aim of the present study was to determine the regulatory effects of this pathway on the infection and replication of HBV. The results indicated that the HBV entry process may activate the AKT pathway, as demonstrated by AKT phosphorylation in HBV natural infection...
January 8, 2018: Molecular Medicine Reports
https://www.readbyqxmd.com/read/29326962/emerging-issues-in-aav-mediated-in%C3%A2-vivo-gene-therapy
#11
REVIEW
Pasqualina Colella, Giuseppe Ronzitti, Federico Mingozzi
In recent years, the number of clinical trials in which adeno-associated virus (AAV) vectors have been used for in vivo gene transfer has steadily increased. The excellent safety profile, together with the high efficiency of transduction of a broad range of target tissues, has established AAV vectors as the platform of choice for in vivo gene therapy. Successful application of the AAV technology has also been achieved in the clinic for a variety of conditions, including coagulation disorders, inherited blindness, and neurodegenerative diseases, among others...
March 16, 2018: Molecular Therapy. Methods & Clinical Development
https://www.readbyqxmd.com/read/29326425/unified-understanding-of-ms-course-is-required-for-drug-development
#12
Timothy Coetzee, Alan J Thompson
No abstract text is available yet for this article.
January 12, 2018: Nature Reviews. Neurology
https://www.readbyqxmd.com/read/29326078/ncp7-targeting-a-multitask-protein-for-next-generation-anti-hiv-drug-development-part-2-noncovalent-inhibitors-and-nucleic-acid-binders
#13
REVIEW
Nunzio Iraci, Oriana Tabarrini, Claudio Santi, Luca Sancineto
Nucleocapsid protein 7 (NCp7) represents a viable target not yet reached by the currently available antiretrovirals. It is a small and highly basic protein, which is essential for multiple stages of the viral replicative cycle, with its structure preserved in all viral strains, including clinical isolates. NCp7 can be inhibited covalently, noncovalently and by shielding the nucleic acid (NA) substrates of its chaperone activity. Although covalent NCp7 inhibitors have already been detailed in the first part of this review series, the focus here is based on noncovalent and NA-binder inhibitors and on the analysis of the NCp7 3D structure to deliver fruitful insights for future drug design strategies...
January 8, 2018: Drug Discovery Today
https://www.readbyqxmd.com/read/29326019/isolation-of-a-peptide-containing-d-amino-acid-residues-that-inhibits-the-%C3%AE-helix-mediated-p53-mdm2-interaction-from-a-one-bead-one-compound-library
#14
Jumpei Morimoto, Yuki Hosono, Shinsuke Sando
α-Helix-mediated protein-protein interactions (PPIs) are important targets in biological research and drug development. Peptides containing d-amino acid residues are attractive molecules for inhibiting α-helix-mediated PPIs because of their wide surface area and high protease resistance. In this study, a peptide library was constructed using a one-bead one-compound format designed to isolate left-handed α-helical peptides, which are promising molecules as inhibitors of α-helix-mediated PPIs. Screening of the library against an α-helix-mediated PPI between MDM2 and p53 yielded an inhibitor of the PPI...
January 2, 2018: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/29325508/mesh-nebulizers-have-become-the-first-choice-for-new-nebulized-pharmaceutical-drug-developments
#15
John N Pritchard, Ross Hm Hatley, John Denyer, Dirk von Hollen
In the 24 years since first being marketed, the mesh nebulizer has been developed by five main manufacturers into a viable solution for the delivery of high-value nebulized drugs. Mesh nebulizers provide increased portability, convenience and energy efficiency along with similar lung deposition and increased ease of use compared with jet nebulizers. An analysis of EU and US clinical trial databases has shown that mesh nebulizers are now preferred over jet nebulizers for clinical trials sponsored by pharmaceutical companies...
February 2018: Therapeutic Delivery
https://www.readbyqxmd.com/read/29324919/synchrotron-fourier-transform-infrared-maps-of-ovalbumin-induced-murine-chronic-allergic-airways-disease-correlation-with-conventional-histology
#16
Nadia Mazarakis, Jitraporn Vongsvivut, Keith R Bambery, Kenneth J Snibson, Simon G Royce, Tom C Karagiannis
Asthma is a chronic respiratory disease characterised by airway inflammation, remodeling and hyperresponsiveness. The ability to replicate these asthma traits in the well-established ovalbumin induced chronic model of allergic airways disease is an important tool for asthma research and preclinical drug development. Here, spectra derived from focal plane array and Synchrotron-Fourier transform infrared maps were used to analyse biochemical changes in lung tissue from an ovalbumin-induced murine chronic allergic airways disease model...
September 2017: Hellenic Journal of Nuclear Medicine
https://www.readbyqxmd.com/read/29324783/sirt3-activator-honokiol-attenuates-%C3%AE-amyloid-by-modulating-amyloidogenic-pathway
#17
Sindhu Ramesh, Manoj Govindarajulu, Tyler Lynd, Gwyneth Briggs, Danielle Adamek, Ellery Jones, Jake Heiner, Mohammed Majrashi, Timothy Moore, Rajesh Amin, Vishnu Suppiramaniam, Muralikrishnan Dhanasekaran
Honokiol (poly-phenolic lignan from Magnolia grandiflora) is a Sirtuin-3 (SIRT3) activator which exhibit antioxidant activity and augment mitochondrial functions in several experimental models. Modern evidence suggests the critical role of SIRT3 in the progression of several metabolic and neurodegenerative diseases. Amyloid beta (Aβ), the precursor to extracellular senile plaques, accumulates in the brains of patients with Alzheimer's disease (AD) and is related to the development of cognitive impairment and neuronal cell death...
2018: PloS One
https://www.readbyqxmd.com/read/29324237/dna-induction-of-mdm2-promotes-proliferation-of-human-renal-mesangial-cells-and-alters-peripheral-b-cells-subsets-in-pediatric-systemic-lupus-erythematosus
#18
Chen-Xing Zhang, Ji Chen, Li Cai, Jing Wu, Jia-Yuan Wang, Lan-Fang Cao, Wei Zhou, Tong-Xin Chen
The study is aimed to investigate the role of MDM2 in the pathogenesis of lupus nephritis (LN) in pediatric SLE (pSLE). We confirmed that MDM2 expression was increased in peripheral blood mononuclear cells (PBMCs) as well as renal specimen of SLE compared with that of controls by western blot and immunofluorescence staining. Percentage of apoptotic and necrotic CD4+T, CD8+T and B cells were detected by flow cytometry respectively and levels of plasma cell free DNA (cfDNA) were quantified in SLE and healthy controls (HC)...
January 8, 2018: Molecular Immunology
https://www.readbyqxmd.com/read/29324183/technologies-for-measuring-pharmacokinetic-profiles
#19
A A Heller, S Y Lockwood, T M Janes, D M Spence
The creation of a pharmacokinetic (PK) curve, which follows the plasma concentration of an administered drug as a function of time, is a critical aspect of the drug development process and includes such information as the drug's bioavailability, clearance, and elimination half-life. Prior to a drug of interest gaining clearance for use in human clinical trials, research is performed during the preclinical stages to establish drug safety and dosing metrics from data obtained from the PK studies. Both in vivo animal models and in vitro platforms have limitations in predicting human reaction to a drug due to differences in species and associated simplifications, respectively...
January 11, 2018: Annual Review of Analytical Chemistry
https://www.readbyqxmd.com/read/29323575/phase-ii-investigational-oral-drugs-for-the-treatment-of-radio-chemotherapy-induced-oral-mucositis
#20
Stephen T Sonis, Alessandro Villa
Oral mucositis is a significant unmet clinical need for many cancer patients. The biological complexity of mucositis' pathogenesis provides a number of mechanistic targets suitable as pharmacologic targets. The diversity of targets has stimulated drug development in search of an effective intervention. In this paper, we review a range of agents that are currently being evaluated. Areas covered: Drugs for management of oral mucositis vary in formulation, route of administration and biological target. Most propose to interrupt the initiation of injury by suppressing activation of the innate immune response or countering oxidative stress, or minimizing downstream inflammatory responses...
January 11, 2018: Expert Opinion on Investigational Drugs
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