Search Results - "WOOLFORD, J"
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Changes in Body Mass Index Among Children and Adolescents During the COVID-19 Pandemic
Published in JAMA : the journal of the American Medical Association (12-10-2021)“…The COVID-19 pandemic has been associated with weight gain among adults, but little is known about the weight of US children and adolescents. To evaluate…”
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Approaches to the diagnosis and prevention of frailty
Published in Aging clinical and experimental research (01-09-2020)“…An individual who is living with frailty has impairments in homeostasis across several body systems and is more vulnerable to stressors that may ultimately…”
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Monoacidic Inhibitors of the Kelch-like ECH-Associated Protein 1: Nuclear Factor Erythroid 2‑Related Factor 2 (KEAP1:NRF2) Protein–Protein Interaction with High Cell Potency Identified by Fragment-Based Discovery
Published in Journal of medicinal chemistry (28-04-2016)“…KEAP1 is the key regulator of the NRF2-mediated cytoprotective response, and increasingly recognized as a target for diseases involving oxidative stress…”
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4
Systemic inflammation and disease progression in Alzheimer disease
Published in Neurology (08-09-2009)“…Acute and chronic systemic inflammation are characterized by the systemic production of the proinflammatory cytokine tumor necrosis factor alpha (TNF-alpha)…”
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Multi-Morbidity and Polypharmacy in Older People: Challenges and Opportunities for Clinical Practice
Published in Geriatrics (Basel) (28-10-2020)“…Multi-morbidity and polypharmacy are common in older people and pose a challenge for health and social care systems, especially in the context of global…”
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Design and Synthesis of 56 Shape‐Diverse 3D Fragments
Published in Chemistry : a European journal (22-07-2020)“…Fragment‐based drug discovery is now widely adopted for lead generation in the pharmaceutical industry. However, fragment screening collections are often…”
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Conceptualizing Trust and Distrust as Alternative Stable States: Lessons from the Flint Water Crisis
Published in Ecology and society (01-09-2023)“…Despite the universally recognized importance of fostering trust and avoiding distrust in governance relationships, there remains considerable debate on core…”
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Structure–Activity and Structure–Conformation Relationships of Aryl Propionic Acid Inhibitors of the Kelch-like ECH-Associated Protein 1/Nuclear Factor Erythroid 2‑Related Factor 2 (KEAP1/NRF2) Protein–Protein Interaction
Published in Journal of medicinal chemistry (09-05-2019)“…The KEAP1–NRF2-mediated cytoprotective response plays a key role in cellular homoeostasis. Insufficient NRF2 signaling during chronic oxidative stress may be…”
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Fragment-Based Drug Discovery Targeting Inhibitor of Apoptosis Proteins: Discovery of a Non-Alanine Lead Series with Dual Activity Against cIAP1 and XIAP
Published in Journal of medicinal chemistry (27-08-2015)“…Inhibitor of apoptosis proteins (IAPs) are important regulators of apoptosis and pro-survival signaling pathways whose deregulation is often associated with…”
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10
Fragment-Based Drug Discovery Applied to Hsp90. Discovery of Two Lead Series with High Ligand Efficiency
Published in Journal of medicinal chemistry (26-08-2010)“…Inhibitors of the chaperone Hsp90 are potentially useful as chemotherapeutic agents in cancer. This paper describes an application of fragment screening to…”
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Discovery of (2,4-Dihydroxy-5-isopropylphenyl)-[5-(4-methylpiperazin-1-ylmethyl)-1,3-dihydroisoindol-2-yl]methanone (AT13387), a Novel Inhibitor of the Molecular Chaperone Hsp90 by Fragment Based Drug Design
Published in Journal of medicinal chemistry (26-08-2010)“…Inhibitors of the molecular chaperone heat shock protein 90 (Hsp90) are currently generating significant interest in clinical development as potential…”
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12
Fragment-Based Discovery of a Potent, Orally Bioavailable Inhibitor That Modulates the Phosphorylation and Catalytic Activity of ERK1/2
Published in Journal of medicinal chemistry (14-06-2018)“…Aberrant activation of the MAPK pathway drives cell proliferation in multiple cancers. Inhibitors of BRAF and MEK kinases are approved for the treatment of…”
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COVID-19 and associations with frailty and multimorbidity: a prospective analysis of UK Biobank participants
Published in Aging clinical and experimental research (01-09-2020)“…Background Frailty and multimorbidity have been suggested as risk factors for severe COVID-19 disease. Aims We investigated, in the UK Biobank, whether frailty…”
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Fragment-Guided Discovery of Pyrazole Carboxylic Acid Inhibitors of the Kelch-like ECH-Associated Protein 1: Nuclear Factor Erythroid 2 Related Factor 2 (KEAP1:NRF2) Protein−Protein Interaction
Published in Journal of medicinal chemistry (11-11-2021)“…The NRF2-mediated cytoprotective response is central to cellular homoeostasis, and there is increasing interest in developing small-molecule activators of this…”
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15
Sleep Duration Predicts Cardiometabolic Risk in Obese Adolescents
Published in The Journal of pediatrics (01-05-2014)“…Objective To examine the independent contributions of objectively measured sleep duration and fragmentation on cardiometabolic risk accumulation in free-living…”
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Identification of N-(4-Piperidinyl)-4-(2,6-dichlorobenzoylamino)-1H-pyrazole-3-carboxamide (AT7519), a Novel Cyclin Dependent Kinase Inhibitor Using Fragment-Based X-Ray Crystallography and Structure Based Drug Design
Published in Journal of medicinal chemistry (28-08-2008)“…The application of fragment-based screening techniques to cyclin dependent kinase 2 (CDK2) identified multiple (>30) efficient, synthetically tractable small…”
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201 Challenges Encountered and Lessons Learned from Developing and Implementing the Michigan Research Engaging the Academy and Community in Health (M-REACH) Platform
Published in Journal of clinical and translational science (01-04-2024)“…OBJECTIVES/GOALS: Communities of color often report that their concerns are ignored and desire a means to facilitate effective community-academic engagement,…”
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Fragment-Based Discovery of a Novel, Brain Penetrant, Orally Active HDAC2 Inhibitor
Published in ACS medicinal chemistry letters (13-10-2022)“…Fragment-based ligand discovery was successfully applied to histone deacetylase HDAC2. In addition to the anticipated hydroxamic acid- and benzamide-based…”
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Fragment-Based Approach to the Development of an Orally Bioavailable Lactam Inhibitor of Lipoprotein-Associated Phospholipase A2 (Lp-PLA2)
Published in Journal of medicinal chemistry (08-12-2016)“…Lp-PLA2 has been explored as a target for a number of inflammation associated diseases, including cardiovascular disease and dementia. This article describes…”
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Exploitation of a Novel Binding Pocket in Human Lipoprotein-Associated Phospholipase A2 (Lp-PLA2) Discovered through X‑ray Fragment Screening
Published in Journal of medicinal chemistry (09-06-2016)“…Elevated levels of human lipoprotein-associated phospholipase A2 (Lp-PLA2) are associated with cardiovascular disease and dementia. A fragment screen was…”
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