journal
MENU ▼
Read by QxMD icon Read
search

Expert Opinion on Drug Discovery

journal
https://www.readbyqxmd.com/read/28306363/genome-database-mining-for-the-discovery-of-novel-lantibiotics
#1
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 17, 2017: Expert Opinion on Drug Discovery
https://www.readbyqxmd.com/read/28306350/the-utility-of-target-based-discovery
#2
Glenn E Croston
No abstract text is available yet for this article.
March 17, 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
#3
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/28286965/harnessing-the-power-of-proteomics-for-identification-of-oncogenic-druggable-signalling-pathways-in-cancer
#4
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 13, 2017: Expert Opinion on Drug Discovery
https://www.readbyqxmd.com/read/28277840/signaling-bias-in-drug-discovery
#5
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/28271909/challenges-in-searching-for-therapeutics-against-botulinum-neurotoxins
#6
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 8, 2017: Expert Opinion on Drug Discovery
https://www.readbyqxmd.com/read/28277836/approaches-for-targeting-self-renewal-pathways-in-cancer-stem-cells-implications-for-haematological-treatments
#7
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 6, 2017: Expert Opinion on Drug Discovery
https://www.readbyqxmd.com/read/28277835/selective-targeting-of-epigenetic-reader-domains
#8
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 approved drugs or which are being evaluated in clinical trials, the targeting of epigenetic readers has lagged. 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 6, 2017: Expert Opinion on Drug Discovery
https://www.readbyqxmd.com/read/28277838/using-natural-products-for-drug-discovery-the-impact-of-the-genomics-era
#9
Mingzi M Zhang, Qiao Yuan, 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 4, 2017: Expert Opinion on Drug Discovery
https://www.readbyqxmd.com/read/28277837/an-overview-of-ca-2-mobilization-assays-in-gpcr-drug-discovery
#10
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 4, 2017: Expert Opinion on Drug Discovery
https://www.readbyqxmd.com/read/28277839/zebrafish-xenograft-models-of-cancer-and-metastasis-for-drug-discovery
#11
Hannah K Brown, Kristina Schiavone, Simon Tazzyman, Dominique Heymann, Timothy Ja Chico
Patients with metastatic cancer suffer the highest rate of cancer-related death, but existing animal models of metastasis have disadvantages that limit our ability to understand this process. The zebrafish is increasingly used for cancer modelling, particularly xenografting of human cancer cell lines, and drug discovery, and may provide novel scientific and therapeutic insights. However, this model system remains underexploited. Areas covered: The authors discuss the advantages and disadvantages of the zebrafish xenograft model for the study of cancer, metastasis and drug discovery...
March 1, 2017: Expert Opinion on Drug Discovery
https://www.readbyqxmd.com/read/28276704/cell-impedance-based-label-free-technology-for-the-identification-of-new-drugs
#12
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
#13
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
https://www.readbyqxmd.com/read/28276705/exploring-the-epigenetic-drug-discovery-landscape
#14
Veda Prachayasittikul, Philip Prathipati, Reny Pratiwi, Chuleeporn Phanus-Umporn, Aijaz Ahmad Malik, Nalini Schaduangrat, Kanokwan Seenprachawong, Prapimpun Wongchitrat, Aungkura Supokawej, Virapong Prachayasittikul, Jarl E S Wikberg, Chanin Nantasenamat
Epigenetic modification has been implicated in a wide range of diseases and the ability to modulate such systems is a lucrative therapeutic strategy in drug discovery. Areas covered: This article focuses on the concepts and drug discovery aspects of epigenomics. This is achieved by providing a survey of the following concepts: (i) factors influencing epigenetics, (ii) diseases arising from epigenetics, (iii) epigenetic enzymes as druggable targets along with coverage of existing FDA-approved drugs and pharmacological agents, and (iv) drug repurposing/repositioning as a means for rapid discovery of pharmacological agents targeting epigenetics...
February 28, 2017: Expert Opinion on Drug Discovery
https://www.readbyqxmd.com/read/28164720/applications-of-computer-aided-approaches-in-the-development-of-hepatitis-c-antiviral-agents
#15
Aravindhan Ganesan, Khaled Barakat
Hepatitis C virus (HCV) is a global health problem that causes several chronic life-threatening liver diseases. The numbers of people affected by HCV are rising annually. Since 2011, the FDA has approved several anti-HCV drugs; while many other promising HCV drugs are currently in late clinical trials. Areas covered: This review discusses the applications of different computational approaches in HCV drug design. Expert opinion: Molecular docking and virtual screening approaches have emerged as a low-cost tool to screen large databases and identify potential small-molecule hits against HCV targets...
February 20, 2017: Expert Opinion on Drug Discovery
https://www.readbyqxmd.com/read/28276706/future-strategies-for-the-discovery-of-therapeutic-aptamers
#16
Sorah Yoon, John J Rossi
No abstract text is available yet for this article.
February 15, 2017: Expert Opinion on Drug Discovery
https://www.readbyqxmd.com/read/28165829/an-overview-of-nanofiber-based-antibacterial-drug-design
#17
Semih Calamak, Reza Shahbazi, Ipek Eroglu, Merve Gultekinoglu, Kezban Ulubayram
Conventional administration of antibacterial drugs to the human body can cause vital problems such as dose dependent systemic toxicity and bacterial resistance which prevent the healing process. In this regard, recent studies have been devoted to producing nanofiber based antibacterial drug delivery approaches which surpass bacterial resistance and toxicological issues. Areas covered: This review summarizes latest developments in the production of antibacterial nanofibers, nanofiber based antibacterial action mechanisms and release profiles of nanofibers...
February 15, 2017: Expert Opinion on Drug Discovery
https://www.readbyqxmd.com/read/28095715/an-overview-of-aldehyde-oxidase-an-enzyme-of-emerging-importance-in-novel-drug-discovery
#18
Mohammad-Reza Rashidi, Somaieh Soltani
Given the rising trend in medicinal chemistry strategy to reduce cytochrome P450-dependent metabolism, aldehyde oxidase (AOX) has recently gained increased attention in drug discovery programs and the number of drug candidates that are metabolized by AOX is steadily growing. Areas covered: Despite the emerging importance of AOX in drug discovery, there are certain major recognized problems associated with AOX-mediated metabolism of drugs. Intra- and inter-species variations in AOX activity, the lack of reliable and predictive animal models using the common experimental animals, and failure in the predictions of in vivo metabolic activity of AOX using traditional in vitro methods are among these issues that are covered in this article...
February 6, 2017: Expert Opinion on Drug Discovery
https://www.readbyqxmd.com/read/28118747/in-silico-strategies-on-prion-pathogenic-conversion-and-inhibition-from-prp-c-prp-sc
#19
Nataraj S Pagadala, Khajamohiddin Syed, Rakesh Bhat
To date, various therapeutic strategies identified numerous anti-prion compounds and antibodies that stabilize PrP(C), block the conversion of PrP(C)-PrP(Sc) and increased effect on PrP(Sc) clearance. However, no suitable drug has been identified clinically so far due to the poor oral absorption, low blood-brain-barrier [BBB] penetration, and high toxicity. Although some of the drugs were proven to be effective in prion-infected cell culture and whole animal models, none of them increased the rate of survival compared to placebo...
February 2, 2017: Expert Opinion on Drug Discovery
https://www.readbyqxmd.com/read/28067072/drug-target-identification-at-the-crossroad-of-neuronal-apoptosis-and-survival
#20
Barbara Maino, Simona Paparone, Cinzia Severini, Maria Teresa Ciotti, Velia D'agata, Pietro Calissano, Sebastiano Cavallaro
Inappropriate activation of apoptosis may contribute to neurodegeneration, a multifaceted process that results in various chronic disorders, including Alzheimer's and Parkinson's diseases. Several in vitro and in vivo studies demonstrated that neuronal apoptosis is a multi-pathway cell-death program that requires RNA synthesis. Thus, transcriptionally activated genes whose products induce cell death can be triggered by different stimuli and antagonized by neurotrophic factors. Systems biology is now unveiling the series of intracellular signaling pathways and key drug targets at the intersection of neuronal apoptosis and survival...
January 23, 2017: Expert Opinion on Drug Discovery
journal
journal
41534
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"