Search Results - "Huang, Yunyuan"
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N‑Acylamino Saccharin as an Emerging Cysteine-Directed Covalent Warhead and Its Application in the Identification of Novel FBPase Inhibitors toward Glucose Reduction
Published in Journal of medicinal chemistry (14-07-2022)“…With a resurgence of covalent drugs, there is an urgent need for the identification of new moieties capable of cysteine bond formation. Herein, we report on…”
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Structure-Guided Discovery of the Novel Covalent Allosteric Site and Covalent Inhibitors of Fructose-1,6-Bisphosphate Aldolase to Overcome the Azole Resistance of Candidiasis
Published in Journal of medicinal chemistry (10-02-2022)“…Fructose-1,6-bisphosphate aldolase (FBA) represents an attractive new antifungal target. Here, we employed a structure-based optimization strategy to discover…”
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Specific tracking of monoamine oxidase A in heart failure models by a far-red fluorescent probe with an ultra large Stokes shift
Published in Chinese chemical letters (01-03-2022)“…Monoamine oxidase A (MAO-A) is a prominent myocardial source of reactive oxygen species (ROS), and its expression and activity are strongly increased in…”
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Anti-aging effects of chlorpropamide depend on mitochondrial complex-II and the production of mitochondrial reactive oxygen species
Published in Acta pharmaceutica Sinica. B (01-02-2022)“…Sulfonylureas are widely used oral anti-diabetic drugs. However, its long-term usage effects on patients’ lifespan remain controversial, with no reports of…”
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A Senomorphlytic Three-Drug Combination Discovered in Salsola collina for Delaying Aging Phenotypes and Extending Healthspan
Published in Advanced science (01-09-2024)“…The pursuit of pharmacological interventions in aging aims focuses on maximizing safety and efficacy, prompting an exploration of natural products endowed with…”
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Structural repurposing of SGLT2 inhibitor empagliflozin for strengthening anti-heart failure activity with lower glycosuria
Published in Acta pharmaceutica Sinica. B (01-04-2023)“…Sodium-glucose cotransporter 2 (SGLT2) inhibitors have been reapproved for heart failure (HF) therapy in patients with and without diabetes. However, the…”
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Advances in inhibitor development targeting the PWWP domain
Published in Trends in pharmacological sciences (Regular ed.) (01-03-2024)“…The PWWP domain binds to both histone and DNA of a nucleosome in a bivalent way. PWWP domain-containing proteins are involved in different biological…”
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Inhibitors targeting the PWWP domain-containing proteins
Published in European journal of medicinal chemistry (15-12-2024)“…PWWP domain-containing proteins play a pivotal role in chromatin-mediated biological processes, and their aberrant regulation is linked to various human…”
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N/C-degron pathways and inhibitor development for PROTAC applications
Published in Biochimica et biophysica acta. Gene regulatory mechanisms (01-03-2024)“…Ubiquitination is a fascinating post-translational modification that has received continuous attention since its discovery. In this review, we first provide a…”
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Novel Combination Therapy for Heart Failure: Trimebutine–Methoxsalen Identified through Synergistic Network Virtual Screening and Experimental Validation
Published in Journal of chemical information and modeling (23-09-2024)“…Combination therapy is increasingly favored by pharmaceutical companies and researchers as an effective way to quickly discover new drugs with excellent…”
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Cov_FB3D: A De Novo Covalent Drug Design Protocol Integrating the BA-SAMP Strategy and Machine-Learning-Based Synthetic Tractability Evaluation
Published in Journal of chemical information and modeling (28-09-2020)“…De novo drug design actively seeks to use sets of chemical rules for the fast and efficient identification of structurally new chemotypes with the desired set…”
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Discovery of novel dual RAGE/SERT inhibitors for the potential treatment of the comorbidity of Alzheimer's disease and depression
Published in European journal of medicinal chemistry (05-06-2022)“…Depression is identified as one of the most common psychiatric symptoms in Alzheimer's disease (AD). The comorbidity of AD and depression increases the burden…”
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Rapid Repurposing of Novel Combination Drugs for the Treatment of Heart Failure via a Computationally Guided Network Screening Approach
Published in Journal of chemical information and modeling (14-11-2022)“…Combination drugs, characterized by high efficacy and few side effects, have received extensive attention from pharmaceutical companies and researchers for the…”
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14
Discovery of novel allosteric site and covalent inhibitors of FBPase with potent hypoglycemic effects
Published in European journal of medicinal chemistry (15-12-2019)“…Fructose-1,6-bisphosphatase (FBPase) is an essential enzyme of GNG pathway. Significant advances demonstrate the FBPase plays a critical role in treatment of…”
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Identification of the New Covalent Allosteric Binding Site of Fructose-1,6-bisphosphatase with Disulfiram Derivatives toward Glucose Reduction
Published in Journal of medicinal chemistry (11-06-2020)“…Fructose 1,6-bisphosphatase (FBPase) has attracted substantial interest as a target associated with cancer and type 2 diabetes. Herein, we found that…”
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Photoactivatable senolysis with single-cell resolution delays aging
Published in Nature aging (01-03-2023)“…Strategies that can selectively eliminate senescent cells (SnCs), namely senolytics, have been shown to promote healthy lifespan. However, it is challenging to…”
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The novel therapeutic strategy of vilazodone-donepezil chimeras as potent triple-target ligands for the potential treatment of Alzheimer's disease with comorbid depression
Published in European journal of medicinal chemistry (05-02-2022)“…Depression is one of the most frequent comorbid psychiatric symptoms of Alzheimer's disease (AD), and no efficacious drugs have been approved specifically for…”
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Biological evaluation and SAR analysis of novel covalent inhibitors against fructose-1,6-bisphosphatase
Published in Bioorganic & medicinal chemistry (15-09-2020)“…[Display omitted] Fructose-1,6-bisphosphatase (FBPase) is an attractive target for affecting the GNG pathway. In our previous study, the C128 site of FBPase…”
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Nicandra physalodes Extract Exerts Antiaging Effects in Multiple Models and Extends the Lifespan of Caenorhabditis elegans via DAF-16 and HSF-1
Published in Oxidative medicine and cellular longevity (2022)“…The development of safe and effective therapeutic interventions is an important issue for delaying aging and reducing the risk of aging-related diseases…”
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Identification of Guaifenesin–Andrographolide as a Novel Combinatorial Drug Therapy for Epilepsy Using Network Virtual Screening and Experimental Validation
Published in ACS chemical neuroscience (06-04-2022)“…Combinatorial drug therapy has attracted substantial attention as an emerging strategy for the treatment of diseases with complex pathological mechanisms. We…”
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