keyword
MENU ▼
Read by QxMD icon Read
search

New drug discovery

keyword
https://www.readbyqxmd.com/read/28922023/fatty-acid-synthase-fasn-as-a-therapeutic-target-in-breast-cancer
#1
Javier A Menendez, Ruth Lupu
Ten years ago, we put forward the metabolo-oncogenic nature of fatty acid synthase (FASN) in breast cancer. Since the conception of this hypothesis, which provided a model to explain how FASN is intertwined with various signaling networks to cell-autonomously regulate breast cancer initiation and progression, FASN has received considerable attention as a therapeutic target. However, despite the ever-growing evidence demonstrating the involvement of FASN as part of the cancer-associated metabolic reprogramming, translation of the basic science-discovery aspects of FASN blockade to the clinical arena remains a challenge...
September 18, 2017: Expert Opinion on Therapeutic Targets
https://www.readbyqxmd.com/read/28920461/discovery-and-development-of-tramadol-for-the-treatment-of-pain
#2
Lidia Bravo, Juan Antonio Mico, Esther Berrocoso
Tramadol is an opioid drug that, unlike classic opioids, also modulates the monoaminergic system by inhibiting noradrenergic and serotoninergic reuptake. For this reason, tramadol is considered an atypical opioid. These special pharmacological characteristics have made tramadol one of the most commonly prescribed analgesic drugs to treat moderate to severe pain. Areas covered: The aim of this review is to provide a historical description of the biochemistry, pharmacokinetics and particularly, the mechanisms of action of tramadol...
September 17, 2017: Expert Opinion on Drug Discovery
https://www.readbyqxmd.com/read/28920432/plk1-targeted-fluorescent-tumor-imaging-with-high-signal-background-ratio
#3
Ji-Ting Hou, Kyung-Phil Ko, Hu Shi, Wen Xiu Ren, Peter Verwilst, Seyoung Koo, Jin Yong Lee, Sung-Gil Chi, Jong Seung Kim
As significantly expressed during cell division, polo-like kinase 1 (PLK1) plays crucial roles in numerous mitotic events and has attracted interest as a potential therapeutic marker in oncological drug discovery. We prepared two small molecular fluorescent probes, 1 and 2, conjugated to SBE13 (a type II PLK1 inhibitor) to investigate the PLK1-targeted imaging of cancer cells and tumors. Enzymatic docking studies, molecular dynamics simulations, in vitro and in vivo imaging experiments, all supported the selective targeting and visualization of PLK1 expressing cells by probes 1 and 2, and probe 2 was successfully demonstrated to image PLK1-upregualted tumors with a remarkable signal to background ratios...
September 18, 2017: ACS Sensors
https://www.readbyqxmd.com/read/28919707/quantum-mechanics-implementation-in-drug-design-workflows-does-it-really-help
#4
REVIEW
Olayide A Arodola, Mahmoud Es Soliman
The pharmaceutical industry is progressively operating in an era where development costs are constantly under pressure, higher percentages of drugs are demanded, and the drug-discovery process is a trial-and-error run. The profit that flows in with the discovery of new drugs has always been the motivation for the industry to keep up the pace and keep abreast with the endless demand for medicines. The process of finding a molecule that binds to the target protein using in silico tools has made computational chemistry a valuable tool in drug discovery in both academic research and pharmaceutical industry...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28919040/heme-binding-biguanides-target-cytochrome-p450-dependent-cancer-cell-mitochondria
#5
Zhijun Guo, Irina F Sevrioukova, Ilia G Denisov, Xia Zhang, Ting-Lan Chiu, Dafydd G Thomas, Eric A Hanse, Rebecca A D Cuellar, Yelena V Grinkova, Vanessa Wankhede Langenfeld, Daniel S Swedien, Justin D Stamschror, Juan Alvarez, Fernando Luna, Adela Galván, Young Kyung Bae, Julia D Wulfkuhle, Rosa I Gallagher, Emanuel F Petricoin, Beverly Norris, Craig M Flory, Robert J Schumacher, M Gerard O'Sullivan, Qing Cao, Haitao Chu, John D Lipscomb, William M Atkins, Kalpna Gupta, Ameeta Kelekar, Ian A Blair, Jorge H Capdevila, John R Falck, Stephen G Sligar, Thomas L Poulos, Gunda I Georg, Elizabeth Ambrose, David A Potter
The mechanisms by which cancer cell-intrinsic CYP monooxygenases promote tumor progression are largely unknown. CYP3A4 was unexpectedly associated with breast cancer mitochondria and synthesized arachidonic acid (AA)-derived epoxyeicosatrienoic acids (EETs), which promoted the electron transport chain/respiration and inhibited AMPKα. CYP3A4 knockdown activated AMPKα, promoted autophagy, and prevented mammary tumor formation. The diabetes drug metformin inhibited CYP3A4-mediated EET biosynthesis and depleted cancer cell-intrinsic EETs...
August 29, 2017: Cell Chemical Biology
https://www.readbyqxmd.com/read/28917974/cross-cultural-analysis-of-medicinal-plants-commonly-used-in-ethnoveterinary-practices-at-south-waziristan-agency-and-bajaur-agency-federally-administrated-tribal-areas-fata-pakistan
#6
Muhammad Abdul Aziz, Muhammad Adnan, Amir Hasan Khan, Muhammad Sufyan, Shahid Niaz Khan
ETHNOPHARMACOLOGICAL RELEVANCE: In remote areas, medicinal plants have an imperative role in curing various livestock's ailments. In Pakistan, people residing in remote areas including South Waziristan Agency and Bajaur Agency depend on traditional herbal remedies for treating their domestic animals. Medicinal plants are an important part of the medical system in these Agencies. The prime goal of the current study is to explore the ethnoveterinary practices in the two regions and discuss cross-cultural consensus on the use of medicinal plants...
September 13, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/28917310/screening-of-a-small-well-curated-natural-product-based-library-identifies-two-rotenoids-with-potent-nematocidal-activity-against-haemonchus-contortus
#7
H M P Dilrukshi Herath, Sarah Preston, Andreas Hofmann, Rohan A Davis, Anson V Koehler, Bill C H Chang, Abdul Jabbar, Robin B Gasser
The control of parasitic roundworms (nematodes) is heavily reliant on the use of a limited number of anthelmintic drugs. However, drug resistance is now very widespread and no vaccines are available, such that the discovery of new chemical entities is crucial. Within this context, we screened a library of pure natural products (n=400) against exsheathed third-stage (xL3) larvae of the parasitic nematode Haemonchus contortus using a whole-organism screening method. We identified two plant-derived rotenoids, deguelin and rotenone, with inhibitory activity on xL3 motility...
September 15, 2017: Veterinary Parasitology
https://www.readbyqxmd.com/read/28916303/high-throughput-flow-cytometry-for-drug-discovery-principles-applications-and-case-studies
#8
REVIEW
Mei Ding, Karin Kaspersson, David Murray, Catherine Bardelle
Flow cytometry is a technology providing multiparametric analysis of single cells or other suspension particles. High-throughput (HT) flow cytometry has become an attractive screening platform for drug discovery. In this review, we highlight the recent HT flow cytometry applications, and then focus on HT flow cytometry deployment at AstraZeneca (AZ). Practical considerations for successful HT flow cytometry assay development and screening are provided based on experience from four project case studies at AZ...
September 12, 2017: Drug Discovery Today
https://www.readbyqxmd.com/read/28915805/antibiotic-resistance-it-s-bad-but-why-isn-t-it-worse
#9
REVIEW
Nicholas Waglechner, Gerard D Wright
Antibiotic natural products are ancient and so is resistance. Consequently, environmental bacteria harbor numerous and varied antibiotic resistance elements. Nevertheless, despite long histories of antibiotic production and exposure, environmental bacteria are not resistant to all known antibiotics. This means that there are barriers to the acquisition of a complete resistance armamentarium. The sources, distribution, and movement of resistance mechanisms in different microbes and bacterial populations are mosaic features that act as barriers to slow this movement, thus moderating the emergence of bacterial pan-resistance...
September 15, 2017: BMC Biology
https://www.readbyqxmd.com/read/28915268/large-scale-cross-species-chemogenomic-platform-proposes-a-new-drug-discovery-strategy-of-veterinary-drug-from-herbal-medicines
#10
Chao Huang, Yang Yang, Xuetong Chen, Chao Wang, Yan Li, Chunli Zheng, Yonghua Wang
Veterinary Herbal Medicine (VHM) is a comprehensive, current, and informative discipline on the utilization of herbs in veterinary practice. Driven by chemistry but progressively directed by pharmacology and the clinical sciences, drug research has contributed more to address the needs for innovative veterinary medicine for curing animal diseases. However, research into veterinary medicine of vegetal origin in the pharmaceutical industry has reduced, owing to questions such as the short of compatibility of traditional natural-product extract libraries with high-throughput screening...
2017: PloS One
https://www.readbyqxmd.com/read/28915003/the-evolution-of-dna-templated-synthesis-as-a-tool-for-materials-discovery
#11
Rachel K O'Reilly, Andrew J Turberfield, Thomas R Wilks
Precise control over reactivity and molecular structure is a fundamental goal of the chemical sciences. Billions of years of evolution by natural selection have resulted in chemical systems capable of information storage, self-replication, catalysis, capture and production of light, and even cognition. In all these cases, control over molecular structure is required to achieve a particular function: without structural control, function may be impaired, unpredictable, or impossible. The search for molecules with a desired function is often achieved by synthesizing a combinatorial library, which contains many or all possible combinations of a set of chemical building blocks (BBs), and then screening this library to identify "successful" structures...
September 15, 2017: Accounts of Chemical Research
https://www.readbyqxmd.com/read/28914188/a-retrospect-study-on-thiazole-derivatives-as-the-potential-antidiabetic-agents-in-drug-discovery-amp-developments
#12
Gopal L Khatik, Ashok Kumar Datusalia, Waquar Ahsan, Paranjeet Kaur, Manish Vyas, Amit Mittal, Surendra Kumar Nayak
BACKGROUND: Heterocycles containing thiazole, a moiety with sulfur and nitrogen is a core structure which found in a number of biologically active compounds. The thiazole ring is notable as a component of the certain natural products, such as vitamin B1 (thiamine) and penicillins. Thiazole is also known as wonder nucleus and has versatile in different biological fields. A number of new compounds contain heterocycle thiazole moieties, thus it is one of the important areas of research. METHODS: We searched the scientific database using relevant keywords...
September 15, 2017: Current Drug Discovery Technologies
https://www.readbyqxmd.com/read/28911817/natural-neuro-inflammatory-inhibitors-from-caragana-turfanensis
#13
Yan Song, Lan Pan, Wenjie Li, Yingying Si, Di Zhou, Chengjian Zheng, Xiaofang Hao, Xinyue Jia, Yuemei Jia, Minghui Shi, Xiaoguang Jia, Ning Li, Yue Hou
Because of the critical role of over-activated microglia in the progress of neurodegenerative diseases, it has been selected as a potential therapeutic target for drug discovery. In order to find natural neuroinflammatory inhibitors, we carried out a bioactivity-oriented phytochemical research of Caragana turfanensis Kom. (Krassn.), which is a folk medicine widely distributed in Xinjiang. As a result, a new coumarin lactone caraganolide A (1) and 35 known components were characterized from the effective extract of C...
August 23, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28911725/which-patient-with-thyroid-cancer-deserves-systemic-therapy-and-when
#14
REVIEW
Furio Pacini
Distant metastases from differentiated thyroid cancer (DTC) are a rare event, occurring in less than 10% of patients with persistent or recurrent clinical disease. About 50% of these patients do respond to radioiodine (RAI) therapy, either with complete remission or stabilization of the disease on a long term period. Unfortunately, another 50% of these patients are refractory to the treatment with RAI, either from the first appearance of distant metastases or during follow-up. Overall, these patients represent 4-5 new cases/year/million...
June 2017: Best Practice & Research. Clinical Endocrinology & Metabolism
https://www.readbyqxmd.com/read/28904183/the-tb-portals-an-open-access-web-based-platform-for-global-drug-resistant-tuberculosis-data-sharing-and-analysis
#15
Alex Rosenthal, Andrei Gabrielian, Eric Engle, Darrell E Hurt, Sofia Alexandru, Valeriu Crudu, Eugene Sergueev, Valery Kirichenko, Vladzimir Lapitskii, Eduard Snezhko, Vassili Kovalev, Andrei Astrovko, Alena Skrahina, Jessica Taaffe, Michael Harris, Alyssa Long, Kurt Wollenberg, Irada Akhundova, Sharafat Ismayilova, Aliaksandr Skrahin, Elcan Mammadbayov, Hagigat Gadirova, Rafik Abuzarov, Mehriban Seyfaddinova, Zaza Avaliani, Irina Strambu, Dragos Zaharia, Alexandru Muntean, Eugenia Ghita, Miron Bogdan, Roxana Mindru, Victor Spinu, Alexandra Sora, Catalina Ene, Sergo Vashakidze, Natalia Shubladze, Ucha Nanava, Alexander Tuzikov, Michael Tartakovsky
The TB Portals Program is an international consortium of physicians, radiologists, and microbiologists from countries with a heavy burden of drug-resistant tuberculosis working with data scientists and IT professionals. Together, we have built the TB Portals, a repository of socioeconomic/geographic, clinical, laboratory, radiological, and genomic data from patient cases of drug-resistant tuberculosis and backed by shareable, physical samples. Currently, there are 1,299 total cases from five country sites (Azerbaijan, Belarus, Moldova, Georgia, and Romania), of which 976 (75...
September 13, 2017: Journal of Clinical Microbiology
https://www.readbyqxmd.com/read/28903573/crispr-in-research-and-treatment-of-multiple-myeloma
#16
M M Simicek, K Growkova, R Hájek
In the recent years, there was a remarkable advance in research and clinical implementation of the genome editing technologies. The most remarkable was a discovery of the bacterial adaptive immune system called CRISPR and its rapid transformation into a robust and broadly applicable technology that completely revolutionized both basic and applied biomedical research. Implementation of CRISPR makes genome modification easier, faster and significantly cheaper compare to any other currently available technology...
2017: Klinická Onkologie: Casopis Ceské a Slovenské Onkologické Spolecnosti
https://www.readbyqxmd.com/read/28903454/precision-medicine-for-hepatocellular-carcinoma-driver-mutations-and-targeted-therapy
#17
REVIEW
Xiao-Xiao Ding, Qing-Ge Zhu, Shi-Ming Zhang, Lei Guan, Ting Li, Lei Zhang, Shi-Yang Wang, Wan-Li Ren, Xue-Mei Chen, Jing Zhao, Song Lin, Zhi-Zhen Liu, Yan-Xia Bai, Bing He, Hu-Qin Zhang
Hepatocellular carcinoma (HCC) is the third most frequent cause of tumor-related mortality and there are an estimated approximately 850,000 new cases annually. Most HCC patients are diagnosed at middle or advanced stage, losing the opportunity of surgery. The development of HCC is promoted by accumulated diverse genetic mutations, which confer selective growth advantages to tumor cells and are called "driver mutations". The discovery of driver mutations provides a novel precision medicine strategy for late stage HCC, called targeted therapy...
August 15, 2017: Oncotarget
https://www.readbyqxmd.com/read/28902434/biologically-active-quinoline-and-quinazoline-alkaloids-part-i
#18
REVIEW
Xiao-Fei Shang, Susan L Morris-Natschke, Ying-Qian Liu, Xiao Guo, Xiao-Shan Xu, Masuo Goto, Jun-Cai Li, Guan-Zhou Yang, Kuo-Hsiung Lee
Quinoline and quinazoline alkaloids, two important classes of N-based heterocyclic compounds, have attracted tremendous attention from researchers worldwide since the 19th century. Over the past 200 years, many compounds from these two classes were isolated from natural sources, and most of them and their modified analogs possess significant bioactivities. Quinine and camptothecin are two of the most famous and important quinoline alkaloids, and their discoveries opened new areas in antimalarial and anticancer drug development, respectively...
September 13, 2017: Medicinal Research Reviews
https://www.readbyqxmd.com/read/28901955/hepg2-and-human-healthy-hepatocyte-in-vitro-culture-and-co-culture-in-pcl-electrospun-platforms
#19
Ines Fasolino, Vincenzo Guarino, Marica Marrese, Valentina Cirillo, Marianna Vallifuoco, Maria Luisa Tamma, Valentina Vassallo, Adele Bracco, Fulvio Calise, Luigi Ambrosio
The discovery of new drugs to treat pathological cells in the case of aggressive liver primary cancer is imposing the identification of high-throughput screening systems to predict the in vivo response of new therapeutic molecules, in order to reduce current use of animals and drug testing costs. Recently, micro/nanostructured scaffolds have been adopted to reproduce the hepatic microenvironment due to their higher similarity to the biological niche with respect to the traditional two-dimensional culture plate, so providing novel in vitro models for reliably understanding molecular mechanisms related to cancer cells activity...
September 13, 2017: Biomedical Materials
https://www.readbyqxmd.com/read/28901856/recent-patents-and-emerging-therapeutics-on-ocular-inflammation-and-allergy
#20
Vibhuti Francisco Agrahari, Zach Aulgur, Siddhant Thukral, Nikhil Dhall, Ryan Conely, Ashim K Mitra
BACKGROUND: Ocular inflammation and allergic eye diseases range from mild to severe may disturbs visual function and affects quality of life. Since these diseases require intensive therapies, the pathophysiology and treatments of these conditions are highlighted. OBJECTIVE: The ocular diseases caused by inflammation and allergy are extensively studied in this review to provide an overview of the newer compounds, novel delivery approaches, preclinical and clinical trials for treatment of the allergic conjunctivitis, dry eye syndrome, and uveitis...
September 11, 2017: Recent Patents on Inflammation & Allergy Drug Discovery
keyword
keyword
56108
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"