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https://www.readbyqxmd.com/read/27912835/second-line-chemotherapy-and-beyond-for-non-small-cell-lung-cancer
#1
REVIEW
Greg Durm, Nasser Hanna
The landscape for the second- and third-line treatment of advanced non-small cell lung cancer has changed dramatically over the last two decades. Immunotherapeutic agents have become a preferred choice following progression on platinum-based first-line chemotherapy. However, there remains a role for cytotoxic chemotherapy and pemetrexed and docetaxel (with or without ramucirumab) are approved for single-agent use in the second-line setting. With the discovery of new genetic alterations and the development of novel targeted drugs, the treatment of advanced non-small cell lung cancer following progression on first-line therapy continues to become more complicated as new treatment algorithms evolve...
February 2017: Hematology/oncology Clinics of North America
https://www.readbyqxmd.com/read/27911112/treatment-of-alpha-and-beta-herpesvirus-infections-in-solid-organ-transplant-recipients
#2
C L Abad, R R Razonable
Human herpesviruses frequently cause infections in solid organ transplant (SOT) recipients. Areas covered: We provide an overview of the clinical impact of alpha and beta herpesviruses and highlight the mechanisms of action, pharmacokinetics, clinical indications, and adverse effects of antiviral drugs for the management of herpes simplex virus, varicella zoster virus and cytomegalovirus. We comprehensively evaluated key clinical trials that led to drug approval, and served as the foundation for management guidelines...
December 2, 2016: Expert Review of Anti-infective Therapy
https://www.readbyqxmd.com/read/27910768/pharmacological-properties-of-biocompounds-from-spores-of-the-lingzhi-or-reishi-medicinal-mushroom-ganoderma-lucidum-agaricomycetes-a-review
#3
Carlos Ricardo Soccol, Lucas Yamasaki Bissoqui, Cristine Rodrigues, Rosalia Rubel, Sandra R B R Sella, Fan Leifa, Luciana Porto de Souza Vandenberghe, Vanete Thomaz Soccol
Ganoderma lucidum is a well-known representative of mushrooms that have been used in traditional Chinese medicine for centuries. New discoveries related to this medicinal mushroom and its biological properties are frequently reported. However, only recently have scientists started to pay special attention to G. lucidum spores. This is in part because of the recent development of methods for breaking the spore wall and extracting biocompounds from the spore. Although some research groups are working with G. lucidum spores, data in the literature are still limited, and the methods used have not been systematized...
2016: International Journal of Medicinal Mushrooms
https://www.readbyqxmd.com/read/27910030/recurrent-cytogenetic-abnormalities-in-non-hodgkin-s-lymphoma-and-chronic-lymphocytic-leukemia
#4
Edmond S K Ma
Characteristic chromosomal translocations are found to be associated with subtypes of B-cell non-Hodgkin lymphoma (NHL), for example t(8;14)(q24;q32) and Burkitt lymphoma, t(14;18)(q32;q21) and follicular lymphoma, and t(11;14)(q13;q32) in mantle cell lymphoma. Only few recurrent cytogenetic aberrations have been identified in the T-cell NHL and the best known is the ALK gene translocation t(2;5)(p23;q35) in anaplastic large cell lymphoma. Since lymph node or other tissue is seldom submitted for conventional cytogenetics study, alternative approaches for translocation detection are polymerase chain reaction (PCR) or fluorescence in situ hybridization (FISH)...
2017: Methods in Molecular Biology
https://www.readbyqxmd.com/read/27908268/synthesis-of-new-fluoro-benzimidazole-derivatives-as-an-approach-towards-the-discovery-of-novel-intestinal-antiseptic-drug-candidates
#5
Ulviye Acar, Begüm Nurpelin Sağlık, Yusuf Özkay, Zerrin Cantürk, Juan Bueno, Fatih Demirci
In the present study, nineteen new fluoro-benzimidazole derivatives, including nifuroxazide analogues, were synthesized by microwave-supported reactions and tested against a panel of pathogenic microorganisms consisting of resistant strains. The synthesized compounds were characterised and identified by FT-IR, 1H- and 13C-NMR, mass spectroscopy, and elemental analyses, respectively. In vitro antimicrobial and cytotoxic effects of the synthesized compounds were determined by microdilution and by [3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] (MTT) assay...
December 1, 2016: Current Pharmaceutical Design
https://www.readbyqxmd.com/read/27908255/solid-state-concerns-during-drug-discovery-and-development-thermodynamic-and-kinetic-aspects-of-crystal-polymorphism-and-the-special-cases-of-concomitant-polymorphs-co-crystals-and-glasses
#6
Daniel Petrus Otto, Melgardt Melvin De Villiers
During drug discovery and development the thermodynamics and kinetics of crystal form transitions must be studied and the fundamental properties of polymorphs must be identified. However, despite the accumulation of knowledge and experimental evidence that support the understanding of crystallization, its predictability still presents significant challenges. With the continuous development of new drug delivery technologies, even more complex situations arise such as difficult cases of polymorph selection, co-crystallization of different molecules, and manipulation of the crystallization environment by for example amorphous solids...
December 1, 2016: Current Drug Discovery Technologies
https://www.readbyqxmd.com/read/27908220/pluripotent-stem-cells-the-last-10-years
#7
Erin A Kimbrel, Robert Lanza
Pluripotent stem cells (PSCs) can differentiate into virtually any cell type in the body, making them attractive for both regenerative medicine and drug discovery. Over the past 10 years, technological advances and innovative platforms have yielded first-in-man PSC-based clinical trials and opened up new approaches for disease modeling and drug development. Induced PSCs have become the foremost alternative to embryonic stem cells and accelerated the development of disease-in-a-dish models. Over the years and with each new discovery, PSCs have proven to be extremely versatile...
December 2, 2016: Regenerative Medicine
https://www.readbyqxmd.com/read/27905516/discovery-and-structural-characterisation-of-new-fold-type-iv-transaminases-exemplify-the-diversity-of-this-enzyme-fold
#8
Tea Pavkov-Keller, Gernot A Strohmeier, Matthias Diepold, Wilco Peeters, Natascha Smeets, Martin Schürmann, Karl Gruber, Helmut Schwab, Kerstin Steiner
Transaminases are useful biocatalysts for the production of amino acids and chiral amines as intermediates for a broad range of drugs and fine chemicals. Here, we describe the discovery and characterisation of new transaminases from microorganisms which were enriched in selective media containing (R)-amines as sole nitrogen source. While most of the candidate proteins were clearly assigned to known subgroups of the fold IV family of PLP-dependent enzymes by sequence analysis and characterisation of their substrate specificity, some of them did not fit to any of these groups...
December 1, 2016: Scientific Reports
https://www.readbyqxmd.com/read/27904012/new-trends-in-drug-discovery-and-development-by-constrained-peptides
#9
Keiichi Masuya
No abstract text is available yet for this article.
2016: Nihon Yakurigaku Zasshi. Folia Pharmacologica Japonica
https://www.readbyqxmd.com/read/27903430/minimizing-the-risk-of-chemically-reactive-metabolite-formation-of-new-drug-candidates-implications-for-preclinical-drug-design
#10
Andreas Brink, Axel Pähler, Christoph Funk, Franz Schuler, Simone Schadt
Many pharmaceutical companies aim to reduce reactive metabolite formation by chemical modification at early stages of drug discovery. A practice often applied is the detection of stable trapping products of electrophilic intermediates with nucleophilic trapping reagents to guide rational structure-based drug design. This contribution delineates this strategy to minimize the potential for reactive metabolite formation of clinical candidates during preclinical drug optimization, exemplified by the experience at Roche over the past decade...
November 26, 2016: Drug Discovery Today
https://www.readbyqxmd.com/read/27903217/rational-drug-discovery-of-hcv-helicase-inhibitor-improved-docking-accuracy-with-multiple-seedings-of-autodock-vina-and-in-situ-minimization
#11
SeeKhai Lim, Rozana Othman, Rohana Yusof, ChoonHan Heh
BACKGROUND: Hepatitis C is a significant cause for end-stage liver diseases and liver transplantation which affects approximate 3% of the global populations. Despite the present of several direct antiviral agents in the treatment of hepatitis C, the standard treatment for HCV is accompanied by several drawbacks such as adverse side effects, high pricing of medications and the rapid emerging rate of resistant HCV variants. OBJECTIVES: To discover potential inhibitors for HCV helicase through an optimized in silico approach...
November 30, 2016: Current Computer-aided Drug Design
https://www.readbyqxmd.com/read/27902447/a-unique-type-of-gsk-3-inhibitor-brings-new-opportunities-to-the-clinic
#12
Avital Licht-Murava, Rom Paz, Lilach Vaks, Limor Avrahami, Batya Plotkin, Miriam Eisenstein, Hagit Eldar-Finkelman
Development of protein kinase inhibitors is a focus of many drug discovery programs. A major problem, however, is the limited specificity of the commonly used adenosine triphosphate-competitive inhibitors and the weak inhibition of the more selective substrate-competitive inhibitors. Glycogen synthase kinase-3 (GSK-3) is a promising drug target for treating neurodegenerative disorders, including Alzheimer's disease (AD), but most GSK-3 inhibitors have not reached the clinic. We describe a new type of GSK-3 inhibitor, L807mts, that acts through a substrate-to-inhibitor conversion mechanism that occurs within the catalytic site of the enzyme...
November 15, 2016: Science Signaling
https://www.readbyqxmd.com/read/27900785/a-tryptoline-ring-distortion-strategy-leads-to-complex-and-diverse-biologically-active-molecules-from-the-indole-alkaloid-yohimbine
#13
Nicholas Paciaroni, Ranjala Ratnayake, James Matthews, Verrill Norwood, Austin Arnold, Long Dang, Hendrik Luesch, Robert William Huigens Iii
High-throughput screening (HTS) is the primary driver to current drug discovery efforts. New therapeutic agents that enter the market are a direct reflection of the structurally simple compounds that make up screening libraries. Unlike medically relevant natural products (e.g., morphine), small molecules currently being screened have low fraction sp3 character and few, if any, stereogenic centers. Although simple compounds have been useful in drugging certain biological targets (e.g., protein kinases), more sophisticated targets (e...
November 29, 2016: Chemistry: a European Journal
https://www.readbyqxmd.com/read/27900588/modeling-informatics-at-vertex-pharmaceuticals-incorporated-our-philosophy-for-sustained-impact
#14
Georgia McGaughey, W Patrick Walters
Molecular modelers and informaticians have the unique opportunity to integrate cross-functional data using a myriad of tools, methods and visuals to generate information. Using their drug discovery expertise, information is transformed to knowledge that impacts drug discovery. These insights are often times formulated locally and then applied more broadly, which influence the discovery of new medicines. This is particularly true in an organization where the members are exposed to projects throughout an organization, such as in the case of the global Modeling & Informatics group at Vertex Pharmaceuticals...
November 29, 2016: Journal of Computer-aided Molecular Design
https://www.readbyqxmd.com/read/27899820/inhibition-of-hedgehog-dependent-tumors-and-cancer-stem-cells-by-a-newly-identified-naturally-occurring-chemotype
#15
Paola Infante, Romina Alfonsi, Cinzia Ingallina, Deborah Quaglio, Francesca Ghirga, Ilaria D'Acquarica, Flavia Bernardi, Laura Di Magno, Gianluca Canettieri, Isabella Screpanti, Alberto Gulino, Bruno Botta, Mattia Mori, Lucia Di Marcotullio
Hedgehog (Hh) inhibitors have emerged as valid tools in the treatment of a wide range of cancers. Indeed, aberrant activation of the Hh pathway occurring either by ligand-dependent or -independent mechanisms is a key driver in tumorigenesis. The smoothened (Smo) receptor is one of the main upstream transducers of the Hh signaling and is a validated target for the development of anticancer compounds, as underlined by the FDA-approved Smo antagonist Vismodegib (GDC-0449/Erivedge) for the treatment of basal cell carcinoma...
September 22, 2016: Cell Death & Disease
https://www.readbyqxmd.com/read/27899599/pubchem-bioassay-2017-update
#16
Yanli Wang, Stephen H Bryant, Tiejun Cheng, Jiyao Wang, Asta Gindulyte, Benjamin A Shoemaker, Paul A Thiessen, Siqian He, Jian Zhang
PubChem's BioAssay database (https://pubchem.ncbi.nlm.nih.gov) has served as a public repository for small-molecule and RNAi screening data since 2004 providing open access of its data content to the community. PubChem accepts data submission from worldwide researchers at academia, industry and government agencies. PubChem also collaborates with other chemical biology database stakeholders with data exchange. With over a decade's development effort, it becomes an important information resource supporting drug discovery and chemical biology research...
November 29, 2016: Nucleic Acids Research
https://www.readbyqxmd.com/read/27897041/novel-antifungal-agents-a-patent-review-2013-present
#17
María Victoria Castelli, Marcos Gabriel Derita, Silvia Noelí López
Superficial infections involving the skin and mucosa are the most common fungal disease in humans. Fungi can also produce invasive infections (IFI), which are increasing in incidence among the growing population of immunocompromised patients, and are characterized by a high mortality rate. Amphotericin B, new triazoles and echinocandins have improved treatment options in IFI. However, the frequency of less common and more resistant fungi, the limited activity of available antifungal drugs and their undesirable side effects reflect the urgent need for the development of new therapeutic strategies...
November 29, 2016: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/27897001/differential-pathway-dependency-discovery-associated-with-drug-response-across-cancer-cell-lines
#18
Gil Speyer, Divya Mahendra, Hai J Tran, Jeff Kiefer, Stuart L Schreiber, Paul A Clemons, Harshil Dhruv, Michael Berens, Seungchan Kim
The effort to personalize treatment plans for cancer patients involves the identification of drug treatments that can effectively target the disease while minimizing the likelihood of adverse reactions. In this study, the gene-expression profile of 810 cancer cell lines and their response data to 368 small molecules from the Cancer Therapeutics Research Portal (CTRP) are analyzed to identify pathways with significant rewiring between genes, or differential gene dependency, between sensitive and non-sensitive cell lines...
2016: Pacific Symposium on Biocomputing
https://www.readbyqxmd.com/read/27896985/a-new-relevance-estimator-for-the-compilation-and-visualization-of-disease-patterns-and-potential-drug-targets
#19
Modest VON Korff, Tobias Fink, Thomas Sander
A new computational method is presented to extract disease patterns from heterogeneous and text-based data. For this study, 22 million PubMed records were mined for co-occurrences of gene name synonyms and disease MeSH terms. The resulting publication counts were transferred into a matrix Mdata. In this matrix, a disease was represented by a row and a gene by a column. Each field in the matrix represented the publication count for a co-occurring disease-gene pair. A second matrix with identical dimensions Mrelevance was derived from Mdata...
2016: Pacific Symposium on Biocomputing
https://www.readbyqxmd.com/read/27896216/recent-advances-in-immunotherapy-in-metastatic-nsclc
#20
REVIEW
Pranshu Bansal, Diaa Osman, Gregory N Gan, George R Simon, Yanis Boumber
Non-small cell lung cancer (NSCLC) is one of most common malignancies and the leading cause of cancer deaths worldwide. Despite advances in targeted therapies, majority of NSCLC patients do not have targetable genomic alterations. Nevertheless, recent discovery that NSCLC is an immunogenic tumor type, and several breakthroughs in immunotherapies have led to rapid expansion of this new treatment modality in NSCLC with recent FDA approvals of programed death receptor-1 inhibitors, such as nivolumab and pembrolizumab...
2016: Frontiers in Oncology
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