Search Results - "BROWN, Dean G"
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Analysis of Past and Present Synthetic Methodologies on Medicinal Chemistry: Where Have All the New Reactions Gone?
Published in Journal of medicinal chemistry (26-05-2016)“…An analysis of chemical reactions used in current medicinal chemistry (2014), three decades ago (1984), and in natural product total synthesis has been…”
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Expanding the medicinal chemistry synthetic toolbox
Published in Nature reviews. Drug discovery (01-10-2018)“…Analysis of the role of synthetic organic chemistry in the identification of chemical starting points for drug discovery and subsequent optimization into…”
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ESKAPEing the labyrinth of antibacterial discovery
Published in Nature reviews. Drug discovery (01-08-2015)“…Incentives are increasingly available for the development of new drugs to tackle antibiotic resistance, but major scientific challenges remain, such as…”
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Trends and Exceptions of Physical Properties on Antibacterial Activity for Gram-Positive and Gram-Negative Pathogens
Published in Journal of medicinal chemistry (11-12-2014)“…To better understand the difficulties surrounding the identification of novel antibacterial compounds from corporate screening collections, physical properties…”
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Impact of a five-dimensional framework on R&D productivity at AstraZeneca
Published in Nature reviews. Drug discovery (01-03-2018)“…In 2011, AstraZeneca set out to improve its research and development (R&D) productivity by focusing decision-making using a framework with five technical…”
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Prolonged tau clearance and stress vulnerability rescue by pharmacological activation of autophagy in tauopathy neurons
Published in Nature communications (26-06-2020)“…Tauopathies are neurodegenerative diseases associated with accumulation of abnormal tau protein in the brain. Patient iPSC-derived neuronal cell models…”
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New natural products as new leads for antibacterial drug discovery
Published in Bioorganic & medicinal chemistry letters (15-01-2014)“…Natural products have been a rich source of antibacterial drugs for many decades, but investments in this area have declined over the past two decades. The…”
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Clinical development times for innovative drugs
Published in Nature reviews. Drug discovery (01-11-2022)Get full text
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Novel Antibacterial Targets and Compounds Revealed by a High-Throughput Cell Wall Reporter Assay
Published in Journal of bacteriology (01-05-2015)“…A high-throughput phenotypic screen based on a Citrobacter freundii AmpC reporter expressed in Escherichia coli was executed to discover novel inhibitors of…”
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An Analysis of Successful Hit-to-Clinical Candidate Pairs
Published in Journal of medicinal chemistry (08-06-2023)“…An analysis of 156 published clinical candidates from the Journal of Medicinal Chemistry between 2018 and 2021 was conducted to identify lead generation…”
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A Decade of FDA-Approved Drugs (2010–2019): Trends and Future Directions
Published in Journal of medicinal chemistry (11-03-2021)“…A total of 378 novel drugs and 27 biosimilars approved by the U.S. Food and Drug Administration (FDA) between 2010 and 2019 were evaluated according to…”
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A Drug Discovery Perspective on FDA Expedited Development and Incentive Programs
Published in Journal of medicinal chemistry (08-02-2024)“…Expedited development and approval pathways at the Food and Drug Administration (FDA) such as Priority review, Fast Track Designation, Breakthrough…”
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Adapting to the Changing Landscape of Biotech-Driven Drug Discovery
Published in Journal of medicinal chemistry (14-12-2023)Get full text
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Correction to “An Analysis of Successful Hit-to-Clinical Candidate Pairs”
Published in Journal of medicinal chemistry (13-07-2023)Get full text
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Where Do Recent Small Molecule Clinical Development Candidates Come From?
Published in Journal of medicinal chemistry (08-11-2018)“…An analysis of 66 published clinical candidates from Journal of Medicinal Chemistry has been conducted to shed light on which lead generation strategies are…”
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Tool inhibitors and assays to interrogate the biology of the TRAF2 and NCK interacting kinase
Published in Bioorganic & medicinal chemistry letters (01-08-2019)“…[Display omitted] The TRAF2 and NCK interacting kinase (TNIK) has been proposed to play a role in cytoskeletal organization and synaptic plasticity and has…”
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Axl receptor tyrosine kinase is a regulator of apolipoprotein E
Published in Molecular brain (04-05-2020)“…Alzheimer's disease (AD), the leading cause of dementia, is a chronic neurodegenerative disease. Apolipoprotein E (apoE), which carries lipids in the brain in…”
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In Vitro Metabolism Studies of Nomifensine Monooxygenation Pathways: Metabolite Identification, Reaction Phenotyping, and Bioactivation Mechanism
Published in Drug metabolism and disposition (01-10-2010)“…Multiple GSH adducts of the oxidative products of nomifensine (M1-M9) in human hepatocytes and liver microsomes have been identified recently. The current…”
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Protease-activated receptor-2 ligands reveal orthosteric and allosteric mechanisms of receptor inhibition
Published in Communications biology (17-12-2020)“…Protease-activated receptor-2 (PAR2) has been implicated in multiple pathophysiologies but drug discovery is challenging due to low small molecule tractability…”
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Drug discovery strategies to outer membrane targets in Gram-negative pathogens
Published in Bioorganic & medicinal chemistry (15-12-2016)“…This review article summarizes important chemical and structural advances in Gram-negative outer membrane targets within the key pathways of…”
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