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Expert Opinion on Drug Discovery

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https://www.readbyqxmd.com/read/28816544/animal-inflammation-based-models-of-depression-and-their-application-to-drug-discovery
#1
Li Ma, Konstantin A Demin, Tatyana O Kolesnikova, Sergey L Kharsko, Xiaokang Zhu, Xiaodong Yuan, Cai Song, Darya A Meshalkina, Brian E Leonard, Li Tian, Allan V Kalueff
Depression, anxiety and other affective disorders are globally widespread and severely debilitating human brain diseases. Despite their high prevalence and mental health impact, affective pathogenesis is poorly understood, and often remains recurrent and resistant to treatment. The lack of efficient antidepressants and presently limited conceptual innovation necessitate novel approaches and new drug targets in the field of antidepressant therapy. Areas covered: Herein, the authors discuss the emerging role of neuro-immune interactions in affective pathogenesis, which can become useful targets for CNS drug discovery, including modulating neuroinflammatory pathways to alleviate affective pathogenesis...
August 17, 2017: Expert Opinion on Drug Discovery
https://www.readbyqxmd.com/read/28814111/ligand-efficiency-metrics-in-drug-discovery-the-pros-and-cons-from-a-practical-perspective
#2
Maria Maddalena Cavalluzzi, Giuseppe Felice Mangiatordi, Orazio Nicolotti, Giovanni Lentini
Ligand efficiency metrics are almost universally accepted as a valuable indicator of compound quality and an aid to reduce attrition. Areas covered: In this review, the authors describe ligand efficiency metrics giving a balanced overview on their merits and points of weakness in order to enable the readers to gain an informed opinion. Relevant theoretical breakthroughs and drug-like properties are also illustrated. Several recent exemplary case studies are discussed in order to illustrate the main fields of application of ligand efficiency metrics...
August 17, 2017: Expert Opinion on Drug Discovery
https://www.readbyqxmd.com/read/28777014/perspectives-on-optical-biosensor-utility-in-small-molecule-screening
#3
Tim Kaminski, Stefan Geschwindner
No abstract text is available yet for this article.
August 10, 2017: Expert Opinion on Drug Discovery
https://www.readbyqxmd.com/read/28776453/new-drug-discovery-approaches-targeting-recurrent-mutations-in-chronic-lymphocytic-leukemia
#4
Rupal Tripathi, Eriong Lee-Verges, Morihiro Higashi, Neus Gimenez, Laia Rosich, Monica Lopez-Guerra, Dolors Colomer
Next generation sequencing has provided a comprehensive understanding of the mutational landscape in chronic lymphocytic leukemia (CLL), and new drivers have been identified. Some of these drivers could be pharmacologically targeted to choose the most effective personalized therapy in each CLL patient. Areas covered: In this article, the authors uncover the potential role of new targeted therapies against the most recurrent mutations in CLL as well as the recently approved therapies. The authors also provide their expert opinion and give their perspectives for the future...
August 4, 2017: Expert Opinion on Drug Discovery
https://www.readbyqxmd.com/read/28770632/an-overview-of-hydrogen-deuterium-exchange-mass-spectrometry-hdx-ms-in-drug-discovery
#5
Glenn R Masson, Meredith L Jenkins, John E Burke
Introduction- Hydrogen deuterium exchange mass spectrometry (HDX-MS) is a powerful methodology to study protein dynamics, protein folding, protein-protein interactions, and protein small molecule interactions. The development of novel methodologies and technical advancements in mass spectrometers has greatly expanded the accessibility and acceptance of this technique within both academia and industry. Areas covered- This review examines the theoretical basis of how amide exchange occurs, how different mass spectrometer approaches can be used for HDX-MS experiments, as well as the use of HDX-MS in drug development, specifically focusing on how HDX-MS is used to characterize bio-therapeutics, and its use in examining protein-protein and protein small molecule interactions...
August 3, 2017: Expert Opinion on Drug Discovery
https://www.readbyqxmd.com/read/28756685/computer-aided-drug-design-time-to-play-with-novel-chemical-matter
#6
Xavier Barril
No abstract text is available yet for this article.
July 31, 2017: Expert Opinion on Drug Discovery
https://www.readbyqxmd.com/read/28758515/approaches-for-discovering-novel-bioactive-small-molecules-targeting-autophagy
#7
Hui-Yun Hwang, Sung Min Cho, Ho Jeong Kwon
In recent years, development of novel bioactive small molecules targeting autophagy has been implicated for autophagy-related disease treatment. Screening new small molecules regulating autophagy allows for the discovery of novel autophagy machinery and therapeutic agents. Areas covered: Two major screening methods for novel autophagy modulators are introduced in this review, namely target based screening and phenotype based screening. With increasing attention focused on chemical compound libraries, coupled with the development of new assay systems, this review attempts to provide an efficient strategy to explore autophagy biology and discover small molecules for the treatment of autophagy-related diseases...
July 30, 2017: Expert Opinion on Drug Discovery
https://www.readbyqxmd.com/read/28748730/therapeutic-targeting-of-leukemic-stem-cells-in-acute-myeloid-leukemia-the-biological-background-for-possible-strategies
#8
Øystein Bruserud, Elise Aasebø, Maria Hernandez-Valladares, Galina Tsykunova, Håkon Reikvam
Acute myeloid leukemia (AML) is an aggressive malignancy, caused by the accumulation of immature leukemic blasts in blood and bone marrow. There is a relatively high risk of chemoresistant relapse even for the younger patients who can receive the most intensive antileukemic treatment. Treatment directed against the remaining leukemic and preleukemic stem cells will most likely reduce the risk of later relapse. Areas covered: Relevant publications were identified through literature searches. The authors searched for original articles and recent reviews describing (i) the characteristics of leukemic/preleukemic stem cells; (ii) the importance of the bone marrow stem cell niches in leukemogenesis; and (iii) possible therapeutic strategies to target the preleukemic/leukemic stem cells...
July 27, 2017: Expert Opinion on Drug Discovery
https://www.readbyqxmd.com/read/28718334/the-preclinical-discovery-and-development-of-brexpiprazole-for-the-treatment-of-major-depressive-disorder
#9
Awais Aftab, Keming Gao
Brexpiprazole is the most recently approved second-generation antipsychotic, which is used as adjunctive therapy to antidepressants for treating major depressive disorder (MDD) with inadequate response. Brexpiprazole shares pharmacological similarities with other second-generation antipsychotics, especially aripiprazole. Area covered: This review provides a detailed overview of the pre-clinical studies of brexpiprazole, followed by a summary of its clinical studies, and a comparison with other antipsychotics in MDD...
July 18, 2017: Expert Opinion on Drug Discovery
https://www.readbyqxmd.com/read/28712329/organotypic-cultures-of-cerebellar-slices-as-a-model-to-investigate-demyelinating-disorders
#10
Frédéric Doussau, Jean-Luc Dupont, Dorine Neel, Aline Schneider, Bernard Poulain, Jean Louis Bossu
Demyelinating disorders, characterized by a chronic or episodic destruction of the myelin sheath, are a leading cause of neurological disability in young adults in western countries. Studying the complex mechanisms involved in axon myelination, demyelination and remyelination requires an experimental model preserving the neuronal networks and neuro-glial interactions. Organotypic cerebellar slice cultures appear to be the best alternative to in vivo experiments and the most commonly used model for investigating etiology or novel therapeutic strategies in multiple sclerosis...
July 17, 2017: Expert Opinion on Drug Discovery
https://www.readbyqxmd.com/read/28712306/targeting-intrinsic-apoptosis-and-other-forms-of-cell-death-by-bh3-mimetics-in-glioblastoma
#11
Georg Karpel-Massler, Chiaki Tsuge Ishida, Yiru Zhang, Marc-Eric Halatsch, M-Andrew Westhoff, Markus D Siegelin
Novel approaches to treat malignant brain tumors are necessary since these neoplasms still display an unfavorable prognosis. Areas covered: In this review, the authors summarize and analyze recent preclinical data that suggest that targeting intrinsic apoptosis may be a suitable strategy for the treatment of malignant gliomas. They focus on the anti-apoptotic Bcl-2 family members of proteins and the recent drug developments in that field with a special focus on BH3-mimetics. With the discovery of BH3-mimetics that interfere with anti-apoptotic Bcl-2 family members in the low nanomolar range significant excitement has been generated towards these class of inhibitors, such as ABT-737, ABT-263 and the most recent successor, ABT-199 which is most advanced with respect to clinical application...
July 17, 2017: Expert Opinion on Drug Discovery
https://www.readbyqxmd.com/read/28699792/novel-approaches-to-the-design-of-bioavailable-melanotropins
#12
Yang Zhou, Minying Cai
The melanocortin system is a primordial and critical system for survival, involved in a wide variety of physiological functions. It includes melanocortin receptors (MCRs) and melanotropin ligands (MCLs). MCRs are important drug targets that can regulate several key physiological processes. Extensive efforts have been made to develop peptide and peptidomimetics targeting melanocortin receptors including MC1R, MC3R, MC4R and MC5R. Most research is focused on developing potent and selective melanotropins. However, developing bioavailable melanotropins remains challenging...
July 12, 2017: Expert Opinion on Drug Discovery
https://www.readbyqxmd.com/read/28685615/representation-and-identification-of-activity-cliffs
#13
Jürgen Bajorath
No abstract text is available yet for this article.
July 12, 2017: Expert Opinion on Drug Discovery
https://www.readbyqxmd.com/read/28695752/stabilization-of-protein-protein-interactions-in-drug-discovery
#14
Sebastian A Andrei, Eline Sijbesma, Michael Hann, Jeremy Davis, Gavin O'Mahony, Matthew W D Perry, Anna Karawajczyk, Jan Eickhoff, Luc Brunsveld, Richard G Doveston, Lech-Gustav Milroy, Christian Ottmann
PPIs are involved in every disease and specific modulation of these PPIs with small molecules would significantly improve our prospects of developing therapeutic agents. Both industry and academia have engaged in the identification and use of PPI inhibitors. However in comparison, the opposite strategy of employing small-molecule stabilizers of PPIs is underrepresented in drug discovery. Areas covered: PPI stabilization has not been exploited in a systematic manner. Rather, this concept validated by a number of therapeutically used natural products like rapamycin and paclitaxel has been shown retrospectively to be the basis of the activity of synthetic molecules originating from drug discovery projects among them lenalidomide and tafamidis...
July 11, 2017: Expert Opinion on Drug Discovery
https://www.readbyqxmd.com/read/28682135/using-zebrafish-as-a-model-to-study-the-role-of-epigenetics-in-hearing-loss
#15
Yingzi He, Beier Bao, Huawei Li
The rapid progress of bioinformatics and high-throughput screening techniques in recent years has led to the identification of many candidate genes and small-molecule drugs that have the potential to make significant contributions to our understanding of the developmental and pathological processes of hearing, but it remains unclear how these genes and regulatory factors are coordinated. Increasing evidence suggests that epigenetic mechanisms are essential for establishing gene expression profiles and likely play an important role in the development of inner ear and in the pathology of hearing-associated diseases...
July 6, 2017: Expert Opinion on Drug Discovery
https://www.readbyqxmd.com/read/28658992/biophysics-for-hts-hit-validation-chemical-lead-optimization-and-beyond
#16
Christine C Genick, S Kirk Wright
There are many challenges to the drug discovery process, including the complexity of the target, its interactions, and how these factors play a role in causing the disease. Traditionally, biophysics has been used for hit validation and chemical lead optimization. With its increased throughput and sensitivity, biophysics is now being applied earlier in this process to empower target characterization and hit finding. Areas covered: In this article, the authors provide an overview of how biophysics can be utilized to assess the quality of the reagents used in screening assays, to validate potential tool compounds, to test the integrity of screening assays, and to create follow-up strategies for compound characterization...
July 6, 2017: Expert Opinion on Drug Discovery
https://www.readbyqxmd.com/read/28664751/the-latest-advances-in-the-discovery-of-nitric-oxide-hybrid-drug-compounds
#17
Ricardo A M Serafim, Filipe G Pernichelle, Elizabeth I Ferreira
There is a great interest in Nitric oxide (NO) within medicinal chemistry since it's involved in human signaling pathways. Prodrugs or hybrid compounds containing NO-donor scaffolds linked to an active compound are valuable, due to their potential for modulating many pathological conditions due to NO's biological properties when released in addition to the native drug. Compounds that selectively inhibit nitric oxide synthase isoforms (NOS) can also increase therapeutic capacity, particularly in the treatment of chronic diseases...
June 30, 2017: Expert Opinion on Drug Discovery
https://www.readbyqxmd.com/read/28644732/lipophilicity-and-biomimetic-properties-to-support-drug-discovery
#18
Fotios Tsopelas, Constantinos Giaginis, Anna Tsantili-Kakoulidou
Lipophilicity, expressed as the octanol-water partition coefficient, constitutes the most important property in drug action, influencing both pharmacokinetic and pharmacodynamics processes as well as drug toxicity. On the other hand, biomimetic properties defined as the retention outcome on HPLC columns containing a biological relevant agent, provide a considerable advance for rapid experimental - based estimation of ADME properties in early drug discovery stages. Areas covered: This review highlights the paramount importance of lipophilicity in almost all aspects of drug action and safety...
June 28, 2017: Expert Opinion on Drug Discovery
https://www.readbyqxmd.com/read/28650716/erratum
#19
(no author information available yet)
No abstract text is available yet for this article.
June 26, 2017: Expert Opinion on Drug Discovery
https://www.readbyqxmd.com/read/28650697/erratum
#20
(no author information available yet)
No abstract text is available yet for this article.
June 26, 2017: Expert Opinion on Drug Discovery
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