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Expert Opinion on Drug Discovery

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https://www.readbyqxmd.com/read/28541811/future-drug-discovery-in-renin-angiotensin-aldosterone-system-intervention
#1
Maria Tamargo, Juan Tamargo
Renin-angiotensin- aldosterone system inhibitors (RAASIs), including angiotensin-converting enzyme inhibitors, angiotensin AT1 receptor blockers and mineralocorticoid receptor antagonists (MRAs), are the cornerstone for the treatment of cardiovascular and renal diseases. Areas covered: The authors searched MEDLINE, PubMed and ClinicalTrials.gov to identify eligible full-text English language papers. Herein, the authors discuss AT2-receptor agonists and ACE2/angiotensin-(1- 7)/Mas-receptor axis modulators, direct renin inhibitors, brain aminopeptidase A inhibitors, biased AT1R blockers, chymase inhibitors, multitargeted drugs, vaccines and aldosterone receptor antagonists as well as aldosterone synthase inhibitors...
May 25, 2017: Expert Opinion on Drug Discovery
https://www.readbyqxmd.com/read/28521526/the-impact-of-genetics-on-future-drug-discovery-in-schizophrenia
#2
Mitsuyuki Matsumoto, Noah M Walton, Hiroshi Yamada, Yuji Kondo, Gerard J Marek, Katsunori Tajinda
Failures of investigational new drugs (INDs) for schizophrenia have left huge unmet medical needs for patients. Given the recent lackluster results, it is imperative that new drug discovery approaches (and resultant drug candidates) target pathophysiological alterations that are shared in specific, stratified patient populations that are selected based on pre-identified biological signatures. One path to implementing this paradigm is achievable by leveraging recent advances in genetic information and technologies...
May 18, 2017: Expert Opinion on Drug Discovery
https://www.readbyqxmd.com/read/28513220/corrigendum
#3
(no author information available yet)
No abstract text is available yet for this article.
May 17, 2017: Expert Opinion on Drug Discovery
https://www.readbyqxmd.com/read/28511597/understanding-sleep-wake-mechanisms-and-drug-discovery
#4
Ana Clementina Equihua-Benítez, Khalil Guzmán-Vásquez, René Drucker-Colín
Although not discernible at first glance, sleep is a highly active and regulated brain state. Although we spend practically one third of our lifetimes in this stage, its importance is often taken for granted. Sleep loss can lead to disease, error and economic loss. Our understanding of how sleep is achieved has greatly advanced in recent years, and with that, the management of sleep disorders has improved. Nevertheless, there is still room for improvement and recently many new compounds have reached clinical trials with a few being approved for commercial use...
May 17, 2017: Expert Opinion on Drug Discovery
https://www.readbyqxmd.com/read/28506090/rational-design-strategies-for-fimh-antagonists-new-drugs-on-the-horizon-for-urinary-tract-infection-and-crohn-s-disease
#5
Laurel K Mydock-McGrane, Thomas J Hannan, James W Janetka
The bacterial adhesin FimH is a virulence factor and an attractive therapeutic target for urinary tract infection (UTI) and Crohn's Disease (CD). Located on type 1 pili of uropathogenic E. coli (UPEC), the FimH adhesin plays an integral role in the pathogenesis of UPEC. Recent efforts have culminated in the development of small-molecule mannoside FimH antagonists that target the mannose-binding lectin domain of FimH, inhibiting its function and preventing UPEC from binding mannosylated host cells in the bladder, thereby circumventing infection...
May 16, 2017: Expert Opinion on Drug Discovery
https://www.readbyqxmd.com/read/28504025/the-preclinical-discovery-of-vosaroxin-for-the-treatment-of-acute-myeloid-leukemia
#6
Etienne Paubelle, Florence Zylbersztejn, Xavier Thomas
Acute myeloid leukemia (AML) represents a disease with a very poor outcome and remains an area of significant unmet need necessitating novel therapeutic strategies. Among novel therapeutic agents, vosaroxin is a first-in-class anticancer quinolone derivative that targets topoisomerase II and induces site-selective double-strand breaks in DNA, leading to tumor cell apoptosis. Area covered: Herein, the authors provide a comprehensive review of the preclinical development of vosaroxin. This includes coverage of vosaroxin's mechanism of action in addition to its pharmacology and of the main studies reported over the past few years with vosaroxin when used to treat adult AML...
May 13, 2017: Expert Opinion on Drug Discovery
https://www.readbyqxmd.com/read/28494631/learning-from-the-failures-of-drug-discovery-in-b-cell-non-hodgkin-lymphomas-and-perspectives-for-the-future-chronic-lymphocytic-leukemia-and-diffuse-large-b-cell-lymphoma-as-two-ends-of-a-spectrum-in-drug-development
#7
Boris Kubuschok, Martin Trepel
Despite substantial recent advances, there is still an unmet need for better therapies in B-cell non Hodgkin lymphomas (B-NHL), especially in relapsed or refractory disease. Many novel targeted drugs have been developed based on a better molecular understanding of B-NHL. Areas covered: This article focuses on chronic lymphocytic leukemia (CLL) as a representative for indolent lymphomas and paradigmatic for the tremendous progress in treating B-NHL on the one hand and diffuse large B-cell lymphoma (DLBCL) as a representative for aggressive lymphomas and paradigmatic for many unsolved problems in lymphoma treatment on the other hand...
May 12, 2017: Expert Opinion on Drug Discovery
https://www.readbyqxmd.com/read/28494630/harnessing-public-domain-data-to-discover-and-validate-therapeutic-targets
#8
William C Reisdorf, Neha Chhugani, Philippe Sanseau, Pankaj Agarwal
Discovering, developing and validating new disease treatments is a challenging and time-consuming endeavor. Successful drug discovery hinges on selecting the best drug targets with relevance to human disease and evidence that modulating them will be beneficial for patients. Open data initiatives are increasingly placing such knowledge into the public domain. Areas covered: In this review, the authors discuss emerging resources such as Open Targets which integrate key information to prioritize target-disease connections...
May 11, 2017: Expert Opinion on Drug Discovery
https://www.readbyqxmd.com/read/28441902/nonhuman-primates-as-models-for-the-discovery-and-development-of-radiation-countermeasures
#9
Vijay K Singh, Ayodele O Olabisi
Despite significant scientific advances over the past six decades toward the development of safe and effective radiation countermeasures for humans using animal models, only two pharmaceutical agents have been approved by United States Food and Drug Administration (US FDA) for hematopoietic acute radiation syndrome (H-ARS). Additional research efforts are needed to further develop large animal models for improving the prediction of clinical safety and effectiveness of radiation countermeasures for ARS and delayed effects of acute radiation exposure (DEARE) in humans...
May 5, 2017: Expert Opinion on Drug Discovery
https://www.readbyqxmd.com/read/28306350/the-utility-of-target-based-discovery
#10
Glenn E Croston
No abstract text is available yet for this article.
March 23, 2017: Expert Opinion on Drug Discovery
https://www.readbyqxmd.com/read/28306363/genome-database-mining-for-the-discovery-of-novel-lantibiotics
#11
Stephanie K Sandiford
The effectiveness of lantibiotics against MDR pathogens and the progression of agents MU1140, NAI-107, NVB302 and duramycin into pre-clinical and clinical trials have highlighted their potential in the fight against bacterial resistance. The number of known lantibiotics and knowledge of their biosynthetic pathways has increased in recent years due to higher quality genomic data being delivered by next generation sequencing technologies combined with the development of specific genome mining tools, enabling the prediction of lantibiotic clusters...
March 22, 2017: Expert Opinion on Drug Discovery
https://www.readbyqxmd.com/read/28286965/harnessing-the-power-of-proteomics-for-identification-of-oncogenic-druggable-signalling-pathways-in-cancer
#12
Heather C Murray, Matthew D Dun, Nicole M Verrills
Genomic and transcriptomic profiling of tumours has revolutionised our understanding of cancer. However, the majority of tumours possess multiple mutations, and determining which oncogene, or even which pathway, to target is difficult. Proteomics is emerging as a powerful approach to identify the functionally important pathways driving these cancers, and how they can be targeted therapeutically. Areas covered: The authors provide a technical overview of mass spectrometry based approaches for proteomic profiling, and review the current and emerging strategies available for the identification of dysregulated networks, pathways, and drug targets in cancer cells, with a key focus on the ability to profile cancer kinomes...
March 17, 2017: Expert Opinion on Drug Discovery
https://www.readbyqxmd.com/read/28277837/an-overview-of-ca-2-mobilization-assays-in-gpcr-drug-discovery
#13
Qiang Ma, Lingyan Ye, Hongxia Liu, Ying Shi, Naiming Zhou
Calcium ions (Ca(2+)) serve as a second messenger or universal signal transducer implicated in the regulation of a wide range of physiological processes. A change in the concentration of intracellular Ca(2+) is an important step in intracellular signal transduction. G protein-coupled receptors (GPCRs), the largest and most versatile group of cell surface receptors, transduce extracellular signals into intracellular responses via their coupling to heterotrimeric G proteins. Since Ca(2+) plays a crucial role in GPCR-induced signaling, measurement of intracellular Ca(2+) has attracted more and more attention in GPCR-targeted drug discovery...
March 17, 2017: Expert Opinion on Drug Discovery
https://www.readbyqxmd.com/read/28271909/challenges-in-searching-for-therapeutics-against-botulinum-neurotoxins
#14
Marco Pirazzini, Ornella Rossetto
Botulinum neurotoxins (BoNTs) are the most potent toxins known. BoNTs are responsible for botulism, a deadly neuroparalytic syndrome caused by the inactivation of neurotransmitter release at peripheral nerve terminals. Thanks to their specificity and potency, BoNTs are both considered potential bio-weapons and therapeutics of choice for a variety of medical syndromes. Several variants of BoNTs have been identified with individual biological properties and little antigenic relation. This expands greatly the potential of BoNTs as therapeutics but poses a major safety problem, increasing the need for finding appropriate antidotes...
March 17, 2017: Expert Opinion on Drug Discovery
https://www.readbyqxmd.com/read/28277838/using-natural-products-for-drug-discovery-the-impact-of-the-genomics-era
#15
Mingzi M Zhang, Yuan Qiao, Ee Lui Ang, Huimin Zhao
Evolutionarily selected over billions of years for their interactions with biomolecules, natural products have been and continue to be a major source of pharmaceuticals. In the 1990s, pharmaceutical companies scaled down their natural product discovery programs in favor of synthetic chemical libraries due to major challenges such as high rediscovery rates, challenging isolation, and low production titers. Propelled by advances in DNA sequencing and synthetic biology technologies, insights into microbial secondary metabolism provided have inspired a number of strategies to address these challenges...
March 14, 2017: Expert Opinion on Drug Discovery
https://www.readbyqxmd.com/read/28277836/approaches-for-targeting-self-renewal-pathways-in-cancer-stem-cells-implications-for-hematological-treatments
#16
Gillian A Horne, Mhairi Copland
Self-renewal is considered a defining property of stem cells. Self-renewal is essential in embryogenesis and normal tissue repair and homeostasis. However, in cancer, self-renewal pathways, e.g. WNT, NOTCH, Hedgehog and BMP, frequently become de-regulated in stem cells, or more mature progenitor cells acquire self-renewal properties, resulting in abnormal tissue growth and tumorigenesis. Areas covered: This review considers the conserved embryonic self-renewal pathways, including WNT, NOTCH, Hedgehog and BMP...
March 14, 2017: Expert Opinion on Drug Discovery
https://www.readbyqxmd.com/read/28277835/selective-targeting-of-epigenetic-reader-domains
#17
Holger Greschik, Roland Schüle, Thomas Günther
Epigenetic regulators including writers, erasers, and readers of chromatin marks have been implicated in numerous diseases and are therefore subject of intense academic and pharmaceutical research. While several small-molecule inhibitors targeting writers or erasers are either approved drugs or are currently being evaluated in clinical trials, the targeting of epigenetic readers has lagged behind. Proof-of-principle that epigenetic readers are also relevant drug targets was provided by landmark discoveries of selective inhibitors targeting the BET family of acetyl-lysine readers...
March 14, 2017: Expert Opinion on Drug Discovery
https://www.readbyqxmd.com/read/28271741/the-preclinical-discovery-and-development-of-quetiapine-for-the-treatment-of-mania-and-depression
#18
Aline Silva de Miranda, Fabrício A Moreira, Antônio Lúcio Teixeira
Bipolar disorder is a chronic disabling condition characterized by alternating manic and depressive episodes. Bipolar disorder has been associated with functional impairment, poor quality of life, morbidity and mortality. Despite its significant clinical, social and economic burden, treatment options for bipolar disorder are still limited. Several clinical trials have shown efficacy of the atypical antipsychotic quetiapine (QTP) in the treatment of this condition. However, the mechanisms underlying the antidepressant and anti-manic effects of QTP remain poorly understood...
March 14, 2017: Expert Opinion on Drug Discovery
https://www.readbyqxmd.com/read/28277840/signaling-bias-in-drug-discovery
#19
Terry Kenakin
The availability of different functional pharmacological assays has revealed that agonists for receptors that are pleiotropically coupled to multiple signaling pathways in the cell can emphasize signals to some pathways over others, i.e. can be biased toward certain signals. This, in turn, opens the possibility that molecules can be made to emphasize favorable signals, de-emphasize harmful signals or selectively block the ability of the natural agonist to produce unfavorable signals. Areas covered: This paper discusses the mechanism of biased signaling, the possible therapeutic implications of this effect, methods to quantify and measure bias and the current literature describing the translation of biased measure in vitro to in vivo systems...
March 9, 2017: Expert Opinion on Drug Discovery
https://www.readbyqxmd.com/read/28276704/cell-impedance-based-label-free-technology-for-the-identification-of-new-drugs
#20
Kenneth Lundstrom
Drug discovery has progressed from relatively simple binding or activity screening assays to high-throughput screening of sophisticated compound libraries with emphasis on miniaturization and automation. The development of functional assays has enhanced the success rate in discovering novel drug molecules. Many technologies, originally based on radioactive labeling, have sequentially been replaced by methods based on fluorescence labeling. Recently, the focus has switched to label-free technologies in cell-based screening assays...
March 1, 2017: Expert Opinion on Drug Discovery
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