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Expert Opinion on Drug Discovery

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https://www.readbyqxmd.com/read/28441902/nonhuman-primates-as-models-for-the-discovery-and-development-of-radiation-countermeasures
#1
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...
April 25, 2017: Expert Opinion on Drug Discovery
https://www.readbyqxmd.com/read/28440681/discovery-and-preclinical-development-of-dasabuvir-for-the-treatment-of-hepatitis-c-infection
#2
Mohamed El Kassas, Tamer Elbaz, Enas Hafez, Mohamed Naguib Wifi, Gamal Esmat
Hepatitis C virus (HCV) is a leading cause of liver-related morbidity and mortality. Positively, the introduction of new directly-acting antivirals (DAAs) have led to dramatic improvements in response rates to antiviral therapy. Furthermore, newer generations of DAAs have demonstrated better safety profiles as well as efficacy than older generations. Current treatment recommendations are based on different combinations of DAAs. Current combination therapies rely on agents that target the different steps of viral replication by using different molecules from various DAAs families...
April 25, 2017: Expert Opinion on Drug Discovery
https://www.readbyqxmd.com/read/28388235/applications-of-crispr-genome-editing-technology-in-drug-target-identification-and-validation
#3
Quinn Lu, George P Livi, Sundip Modha, Kosuke Yusa, Ricardo Macarrón, David J Dow
The analysis of pharmaceutical industry data indicates that the major reason for drug candidates failing in late stage clinical development is lack of efficacy, with a high proportion of these due to erroneous hypotheses about target to disease linkage. More than ever, there is a requirement to better understand potential new drug targets and their role in disease biology in order to reduce attrition in drug development. Genome editing technology enables precise modification of individual protein coding genes, as well as noncoding regulatory sequences, enabling the elucidation of functional effects in human disease relevant cellular systems...
April 23, 2017: Expert Opinion on Drug Discovery
https://www.readbyqxmd.com/read/28425306/therapeutic-targeting-and-patient-selection-for-cancers-with-homologous-recombination-defects
#4
Francien Talens, Mathilde Jalving, Jourik A Gietema, Marcel A T M van Vugt
DNA double-strand breaks (DSBs) are toxic DNA lesions that can be repaired by non-homologous end-joining (NHEJ) or homologous recombination (HR). Mutations in HR genes elicit a predisposition to cancer; yet, they also result in increased sensitivity to certain DNA damaging agents and poly (ADP-ribose) polymerase (PARP) inhibitors. To optimally implement PARP inhibitor treatment, it is important that patients with HR-deficient tumors are adequately selected. Areas covered: Herein, the authors describe the HR pathway mechanistically and review the treatment of HR-deficient cancers, with a specific focus on PARP inhibition for BRCA1/2-mutated breast and ovarian cancer...
April 20, 2017: Expert Opinion on Drug Discovery
https://www.readbyqxmd.com/read/28399679/an-overview-of-quinoline-as-a-privileged-scaffold-in-cancer-drug-discovery
#5
Robert Musiol
The concept of privileged structures is well known and is often used in the process of drug design and development. Although its assumptions are not clear, its overall usefulness remains high. Various substructures have been identified as privileged and quinoline is a prime example of such a structure. Areas covered: Quinoline drugs that are currently approved or under clinical investigation were reviewed based on a literature search. Their modes of action and outcomes during clinical research are discussed...
April 20, 2017: Expert Opinion on Drug Discovery
https://www.readbyqxmd.com/read/28398099/enhancing-the-therapeutic-potential-of-peptide-toxins
#6
Raymond S Norton
Peptide toxins are potent and often exquisitely selective probes of the structure and function of ion channels and receptors, and as such are of significant interest to the pharmaceutical and biotech industries as both therapeutic leads and pharmacological tools. Their progression as clinical candidates, however, faces many of the challenges that are common to peptide drugs generally. Areas covered: The attributes of peptide toxins as therapeutic leads are outlined, as well as some of the limiting factors that have hampered the clinical development of many promising candidates...
April 20, 2017: Expert Opinion on Drug Discovery
https://www.readbyqxmd.com/read/28402221/an-update-on-the-use-of-c-elegans-for-preclinical-drug-discovery-screening-and-identifying-anti-infective-drugs
#7
Wooseong Kim, Gabriel Lambert Hendricks, Kiho Lee, Eleftherios Mylonakis
The emergence of antibiotic-resistant and -tolerant bacteria is a major threat to human health. Although efforts for drug discovery are ongoing, conventional bacteria-centered screening strategies have thus far failed to yield new classes of effective antibiotics. Therefore, new paradigms for discovering novel antibiotics are of critical importance. Caenorhabditis elegans, a model organism used for in vivo, offers a promising solution for identification of anti-infective compounds. Areas covered:This review examines the advantages of C...
April 12, 2017: Expert Opinion on Drug Discovery
https://www.readbyqxmd.com/read/28394189/academia-pharma-partnerships-for-novel-drug-discovery-essential-or-nice-to-have
#8
Michelle Palmer, Rathnam Chaguturu
No abstract text is available yet for this article.
April 10, 2017: Expert Opinion on Drug Discovery
https://www.readbyqxmd.com/read/28306350/the-utility-of-target-based-discovery
#9
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
#10
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
#11
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
#12
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
#13
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
#14
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
#15
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
#16
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
#17
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
#18
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
#19
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
https://www.readbyqxmd.com/read/28276703/a-look-at-ligand-binding-thermodynamics-in-drug-discovery
#20
Rafael Claveria-Gimeno, Sonia Vega, Olga Abian, Adrian Velazquez-Campoy
Drug discovery is a challenging endeavor requiring the interplay of many different research areas. Gathering information on ligand binding thermodynamics may help considerably in reducing the risk within a high uncertainty scenario, allowing early rejection of flawed compounds and pushing forward optimal candidates. In particular, the free energy, the enthalpy, and the entropy of binding provide fundamental information on the intermolecular forces driving such interaction. Areas covered: The authors review the current status and recent developments in the application of ligand binding thermodynamics in drug discovery...
March 1, 2017: Expert Opinion on Drug Discovery
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