keyword
MENU ▼
Read by QxMD icon Read
search

Pipeline drugs

keyword
https://www.readbyqxmd.com/read/28933205/mass-spectrometry-methods-to-study-protein-metabolite-interactions
#1
Hongbo Guo, Hui Peng, Andrew Emili
To ​​​​understand and manipulate biochemical processes and signaling pathways, the knowledge of endogenous protein-metabolite interactions would be extremely helpful. Recent developments in precision mass spectrometry, high-throughput proteomics and sensitive metabolomic profiling are beginning to converge on a possible solution, heralding a new era of global metabolome-proteome 'interactome' studies that promise to change biomedical research and drug discovery. Areas covered: Here, we review innovative mass spectrometry-based methods and recent pioneering studies aimed at elucidating the physical associations of small molecule ligands with cellular proteins...
September 21, 2017: Expert Opinion on Drug Discovery
https://www.readbyqxmd.com/read/28931883/high-throughput-targeted-screening-in-triple-negative-breast-cancer-cells-identifies-wnt-inhibiting-activities-in-pacific-brittle-stars
#2
Artem Blagodatski, Vsevolod Cherepanov, Alexey Koval, Vladimir I Kharlamenko, Yuri S Khotimchenko, Vladimir L Katanaev
Pro-proliferative oncogenic signaling is one of the hallmarks of cancer. Specific targeting of such signaling pathways is one of the main approaches to modern anti-cancer drug discovery, as opposed to more traditional search for general cytotoxic agents. Natural products, especially from marine sources, represent a largely untapped source of chemical diversity, which so far have mostly been screened for cytotoxicity. Here we present a pioneering pipeline of high-throughput screening of marine-based activities targeted against the Wnt signaling pathway, which is one of the key factors in oncogenic transformation, growth and metastasis in different cancers, including the devastating triple-negative breast cancer (TNBC) currently lacking any targeted therapies...
September 20, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28930221/compounds-from-terminalia-mantaly-l-combretaceae-stem-bark-exhibit-potent-inhibition-against-some-pathogenic-yeasts-and-enzymes-of-metabolic-significance
#3
Marthe Aimée Tchuente Tchuenmogne, Thierry Ngouana Kammalac, Sebastian Gohlke, Rufin Marie Toghueo Kouipou, Abdulselam Aslan, Muslum Kuzu, Veysel Comakli, Ramazan Demirdag, Silvère Augustin Ngouela, Etienne Tsamo, Norbert Sewald, Bruno Ndjakou Lenta, Fabrice Fekam Boyom
Background: Pathogenic yeasts resistance to current drugs emphasizes the need for new, safe, and cost-effective drugs. Also, new inhibitors are needed to control the effects of enzymes that are implicated in metabolic dysfunctions such as cancer, obesity, and epilepsy. Methods: The anti-yeast extract from Terminalia mantaly (Combretaceae) was fractionated and the structures of the isolated compounds established by means of spectroscopic analysis and comparison with literature data. Activity was assessed against Candida albicans, C...
January 24, 2017: Medicines (Basel, Switzerland)
https://www.readbyqxmd.com/read/28929430/new-drugs-in-the-pipeline-for-the-treatment-of-hiv-a-review
#4
REVIEW
Leigh Anne Hylton Gravatt, Crystal R Leibrand, Sulay Patel, MaryPeace McRae
PURPOSE OF REVIEW: The purpose of this paper is to review therapies with new mechanisms of action for the treatment of HIV that are at least in phase 2 clinical trials. RECENT FINDINGS: There are several new mechanisms of action being represented within clinical development, including histone deacetylase (HDAC) inhibitors, gene therapies, broadly neutralizing anti-HIV antibodies, immune modulation, and drugs with new mechanisms to block HIV entry. The new therapies are being developed for both as add-on therapy to existing combination antiretroviral therapy and as agents to be used during treatment interruption...
September 19, 2017: Current Infectious Disease Reports
https://www.readbyqxmd.com/read/28925954/quantitative-structure-activity-relationship-modeling-of-kinase-selectivity-profiles
#5
Sandeepkumar Kothiwale, Corina Borza, Ambra Pozzi, Jens Meiler
The discovery of selective inhibitors of biological target proteins is the primary goal of many drug discovery campaigns. However, this goal has proven elusive, especially for inhibitors targeting the well-conserved orthosteric adenosine triphosphate (ATP) binding pocket of kinase enzymes. The human kinome is large and it is rather difficult to profile early lead compounds against around 500 targets to gain an upfront knowledge on selectivity. Further, selectivity can change drastically during derivatization of an initial lead compound...
September 19, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28924171/a-network-integration-approach-for-drug-target-interaction-prediction-and-computational-drug-repositioning-from-heterogeneous-information
#6
Yunan Luo, Xinbin Zhao, Jingtian Zhou, Jinglin Yang, Yanqing Zhang, Wenhua Kuang, Jian Peng, Ligong Chen, Jianyang Zeng
The emergence of large-scale genomic, chemical and pharmacological data provides new opportunities for drug discovery and repositioning. In this work, we develop a computational pipeline, called DTINet, to predict novel drug-target interactions from a constructed heterogeneous network, which integrates diverse drug-related information. DTINet focuses on learning a low-dimensional vector representation of features, which accurately explains the topological properties of individual nodes in the heterogeneous network, and then makes prediction based on these representations via a vector space projection scheme...
September 18, 2017: Nature Communications
https://www.readbyqxmd.com/read/28922445/position-paper-on-treatment-of-hepatitis-c-in-romania-2017-part-two
#7
Liana Gheorghe, Ioan Sporea, Speranta Iacob, Roxana Sirli, Anca Trifan, Mircea Diculescu, Carol Stanciu, Oliviu Pascu, Monica Acalovschi, Ciprian Brisc, Cristina Cijevschi, Cristian Gheorghe, Zeno Spârchez, Ion Rogoveanu, Daniela Dobru, Dan L Dumitrascu
BACKGROUND AND AIMS: Hepatitis C virus (HCV) infection is a common condition with endemic prevalence in some areas of the world. In Romania, the mean prevalence is about 3%. New treatments have become available on the market in recent years and new drugs are in the pipeline. A re-evaluation of HCV therapy was considered mandatory. The Romanian Society of Gastroenterology and Hepatology undertook this task for the practitioners of this country. METHODOLOGY: A group of recognized experts was created who screened the available literature and the major available guidelines...
September 2017: Journal of Gastrointestinal and Liver Diseases: JGLD
https://www.readbyqxmd.com/read/28919062/progress-and-challenges-in-anti-obesity-pharmacotherapy
#8
REVIEW
Daniel H Bessesen, Luc F Van Gaal
Obesity is a serious and growing worldwide health challenge. Healthy lifestyle choices are the foundation of obesity treatment. However, weight loss can lead to physiological adaptations that promote weight regain. As a result, lifestyle treatment alone typically produces only modest weight loss that is difficult to sustain. In other metabolic diseases, pharmacotherapy is an accepted adjunct to lifestyle. Several anti-obesity drugs have been approved in the USA, European Union, Australia, and Japan including sympathomimetics, pancreatic lipase inhibitors, GABAA receptor activators, a serotonin 2C receptor agonist, opioid antagonist, dopamine-norepinephrine reuptake inhibitor, and glucagon-like peptide-1 (GLP-1) receptor agonists...
September 14, 2017: Lancet Diabetes & Endocrinology
https://www.readbyqxmd.com/read/28918303/decoding-noises-in-hiv-computational-genotyping
#9
MingRui Jia, Timothy Shaw, Xing Zhang, Dong Liu, Ye Shen, Amara E Ezeamama, Chunfu Yang, Ming Zhang
Lack of a consistent and reliable genotyping system can critically impede HIV genomic research on pathogenesis, fitness, virulence, drug resistance, and genomic-based healthcare and treatment. At present, mis-genotyping, i.e., background noises in molecular genotyping, and its impact on epidemic surveillance is unknown. For the first time, we present a comprehensive assessment of HIV genotyping quality. HIV sequence data were retrieved from worldwide published records, and subjected to a systematic genotyping assessment pipeline...
September 14, 2017: Virology
https://www.readbyqxmd.com/read/28898695/identification-of-gpc2-as-an-oncoprotein-and-candidate-immunotherapeutic-target-in-high-risk-neuroblastoma
#10
Kristopher R Bosse, Pichai Raman, Zhongyu Zhu, Maria Lane, Daniel Martinez, Sabine Heitzeneder, Komal S Rathi, Nathan M Kendsersky, Michael Randall, Laura Donovan, Sorana Morrissy, Robyn T Sussman, Doncho V Zhelev, Yang Feng, Yanping Wang, Jennifer Hwang, Gonzalo Lopez, Jo Lynne Harenza, Jun S Wei, Bruce Pawel, Tricia Bhatti, Mariarita Santi, Arupa Ganguly, Javed Khan, Marco A Marra, Michael D Taylor, Dimiter S Dimitrov, Crystal L Mackall, John M Maris
We developed an RNA-sequencing-based pipeline to discover differentially expressed cell-surface molecules in neuroblastoma that meet criteria for optimal immunotherapeutic target safety and efficacy. Here, we show that GPC2 is a strong candidate immunotherapeutic target in this childhood cancer. We demonstrate high GPC2 expression in neuroblastoma due to MYCN transcriptional activation and/or somatic gain of the GPC2 locus. We confirm GPC2 to be highly expressed on most neuroblastomas, but not detectable at appreciable levels in normal childhood tissues...
September 11, 2017: Cancer Cell
https://www.readbyqxmd.com/read/28898593/biosimilars-implications-for-clinical-practice
#11
Robert M Rifkin, Susan R Peck
In 2015, the United States Food and Drug Administration (FDA) approved the first biosimilar, filgrastim-sndz, a biosimilar of the granulocyte colony-stimulating factor filgrastim. Since that time, the FDA has approved four additional biosimilar tumor necrosis factor α inhibitors, and, in May 2017, the Oncology Drug Advisory Committee voted in favor of approval of an epoetin alfa biosimilar. The patents of several widely used biologic cancer therapies (including trastuzumab, rituximab, bevacizumab, cetuximab, and pegfilgrastim) are recently expired or due to expire in the near future, so the introduction of biosimilars into the oncology treatment armamentarium is imminent...
September 2017: Journal of Oncology Practice
https://www.readbyqxmd.com/read/28892308/targeting-epidermal-growth-factor-receptor-co-dependent-signaling-pathways-in-glioblastoma
#12
Feng Liu, Paul S Mischel
The epidermal growth factor receptor (EGFR) is a transmembrane receptor tyrosine kinase (RTK) that is critical for normal development and function. EGFR is also amplified or mutated in a variety of cancers including in nearly 60% of cases of the highly lethal brain cancer glioblastoma (GBM). EGFR amplification and mutation reprogram cellular metabolism and broadly alter gene transcription to drive tumor formation and progression, rendering EGFR as a compelling drug target. To date, brain tumor patients have yet to benefit from anti-EGFR therapy due in part to an inability to achieve sufficient intratumoral drug levels in the brain, cultivating adaptive mechanisms of resistance...
September 11, 2017: Wiley Interdisciplinary Reviews. Systems Biology and Medicine
https://www.readbyqxmd.com/read/28882020/non-antibiotic-treatment-for-infectious-diseases
#13
REVIEW
J Ruiz, I Castro, E Calabuig, M Salavert
The abuse and uncontrolled use of antibiotics has resulted in the emergence and spread of resistant bacteria. The utility of conventional antibiotics for the treatment of bacterial infections has become increasingly strained due to increased rates of resistance coupled with reduced rates of development of new agents. As a result, multidrug-resistant, extensively drug-resistant, and pan-drug-resistant bacterial strains are now frequently encountered. This has led to fears of a "post-antibiotic era" in which many bacterial infections could be untreatable...
September 2017: Revista Española de Quimioterapia: Publicación Oficial de la Sociedad Española de Quimioterapia
https://www.readbyqxmd.com/read/28879787/moving-forward-with-treatment-options-for-hiv-infected-children
#14
Jean-Christophe Beghin, Jean Cyr Yombi, Jean Ruelle, Dimitri Van der Linden
Current international guidelines recommend to treat all HIV-1 infected patients regardless of CD4 cell count. Despite the remarkable worldwide progress for universal access to antiretroviral during the last decade, the pediatric population remains fragile due to lack of randomized studies, inappropriate antiretroviral formulations, adherence difficulties, drug toxicity and development of resistance. Areas covered: This review summarizes the latest recommendations and advances for the treatment of HIV-infected children and highlights the potential complications of a lifelong antiretroviral treatment initiated early in life...
September 7, 2017: Expert Opinion on Pharmacotherapy
https://www.readbyqxmd.com/read/28869864/immunopegliposomes-for-the-targeted-delivery-of-novel-lipophilic-drugs-to-red-blood-cells-in-a-falciparum-malaria-murine-model
#15
Ernest Moles, Silvia Galiano, Ana Gomes, Miguel Quiliano, Cátia Teixeira, Ignacio Aldana, Paula Gomes, Xavier Fernàndez-Busquets
Most drugs currently entering the clinical pipeline for severe malaria therapeutics are of lipophilic nature, with a relatively poor solubility in plasma and large biodistribution volumes. Low amounts of these compounds do consequently accumulate in circulating Plasmodium-infected red blood cells, exhibiting limited antiparasitic activity. These drawbacks can in principle be satisfactorily dealt with by stably encapsulating drugs in targeted nanocarriers. Here this approach has been adapted for its use in immunocompetent mice infected by the Plasmodium yoelii 17XL lethal strain, selected as a model for human blood infections by Plasmodium falciparum...
August 15, 2017: Biomaterials
https://www.readbyqxmd.com/read/28857064/implementation-of-g6pd-testing-and-primaquine-for-p-vivax-radical-cure-operational-perspectives-from-thailand-and-cambodia
#16
Suravadee Kitchakarn, Dysoley Lek, Sea Thol, Chantheasy Hok, Aungkana Saejeng, Rekol Huy, Nipon Chinanonwait, Krongthong Thimasarn, Chansuda Wongsrichanalai
Following progressive success in reducing the burden of malaria over the past two decades, countries of the Asia Pacific are now aiming for elimination of malaria by 2030. Plasmodium falciparum and Plasmodium vivax are the two main malaria species that are endemic in the region. P. vivax is generally perceived to be less severe but will be harder to eliminate, owing partly to its dormant liver stage (known as a hypnozoite) that can cause multiple relapses following an initial clinical episode caused by a mosquito-borne infection...
September 2017: WHO South-East Asia Journal of Public Health
https://www.readbyqxmd.com/read/28852193/an-enhanced-c-elegans-based-platform-for-toxicity-assessment
#17
Huajiang Xiong, Catherine Pears, Alison Woollard
There is a well-defined regulatory framework governing the approval of chemicals for use as pharmaceuticals or release into the environment. Toxicity assessment is thus a major hurdle in the compound discovery pipeline, currently involving large scale animal testing. The search for alternative testing platforms is therefore an important priority. We have developed a convenient, low cost assay utilising the nematode Caenorhabditis elegans, to rapidly assess both acute toxicity and developmental and reproductive toxicity (DART)...
August 29, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28851378/in-silico-prediction-of-novel-therapeutic-targets-using-gene-disease-association-data
#18
Enrico Ferrero, Ian Dunham, Philippe Sanseau
BACKGROUND: Target identification and validation is a pressing challenge in the pharmaceutical industry, with many of the programmes that fail for efficacy reasons showing poor association between the drug target and the disease. Computational prediction of successful targets could have a considerable impact on attrition rates in the drug discovery pipeline by significantly reducing the initial search space. Here, we explore whether gene-disease association data from the Open Targets platform is sufficient to predict therapeutic targets that are actively being pursued by pharmaceutical companies or are already on the market...
August 29, 2017: Journal of Translational Medicine
https://www.readbyqxmd.com/read/28831944/biological-factors-that-impinge-on-chagas-disease-drug-development
#19
Amanda F Francisco, Shiromani Jayawardhana, Michael D Lewis, Martin C Taylor, John M Kelly
Chagas disease is caused by infection with the insect-transmitted protozoan Trypanosoma cruzi, and is the most important parasitic infection in Latin America. The current drugs, benznidazole and nifurtimox, are characterized by limited efficacy and toxic side-effects, and treatment failures are frequently observed. The urgent need for new therapeutic approaches is being met by a combined effort from the academic and commercial sectors, together with major input from not-for-profit drug development consortia...
August 23, 2017: Parasitology
https://www.readbyqxmd.com/read/28829118/bioactive-natural-products-prioritization-using-massive-multi-informational-molecular-networks
#20
Florent Olivon, Pierre-Marie Allard, Alexey Koval, Davide Righi, Gregory Genta-Jouve, Johan Neyts, Cécile Apel, Christophe Pannecouque, Louis-Félix Nothias, Xavier Cachet, Laurence Marcourt, Fanny Roussi, Vladimir L Katanaev, David Touboul, Jean-Luc Wolfender, Marc Litaudon
Natural products represent an inexhaustible source of novel therapeutic agents. Their complex and constrained three-dimensional structures endow these molecules with exceptional biological properties, thereby giving them a major role in drug discovery programs. However, the search for new bioactive metabolites is hampered by the chemical complexity of the biological matrices in which they are found. The purification of single constituents from such matrices requires such a significant amount of work that it should be ideally performed only on molecules of high potential value (i...
September 15, 2017: ACS Chemical Biology
keyword
keyword
42476
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"