Search Results - "Wold, Eric A."

Allosteric Modulation of Class A GPCRs: Targets, Agents, and Emerging Concepts by Wold, Eric A, Chen, Jianping, Cunningham, Kathryn A, Zhou, Jia

“…G-protein-coupled receptors (GPCRs) have been tractable drug targets for decades with over one-third of currently marketed drugs targeting GPCRs. Of these, the…”
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Discovery and development of natural product oridonin-inspired anticancer agents by Ding, Ye, Ding, Chunyong, Ye, Na, Liu, Zhiqing, Wold, Eric A., Chen, Haiying, Wild, Christopher, Shen, Qiang, Zhou, Jia

“…Natural products have historically been, and continue to be, an invaluable source for the discovery of various therapeutic agents. Oridonin, a natural…”
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Therapeutic Potential of Spirooxindoles as Antiviral Agents by Ye, Na, Chen, Haiying, Wold, Eric A, Shi, Pei-Yong, Zhou, Jia

“…Antiviral therapeutics with profiles of high potency, low resistance, panserotype, and low toxicity remain challenging, and obtaining such agents continues to…”
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GPCR Allosteric Modulators: Mechanistic Advantages and Therapeutic Applications by Wold, Eric A, Zhou, Jia

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Applications of Bioorthogonal Chemistry in Tumor-Targeted Drug Discovery by Liu, Gang, Wold, Eric A, Zhou, Jia

“…Chemical reactions that can proceed in living systems while not interfering with native biochemical processes are collectively referred to as bioorthogonal…”
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Orphan Receptor GPR88 as an Emerging Neurotherapeutic Target by Ye, Na, Li, Bang, Mao, Qi, Wold, Eric A, Tian, Sheng, Allen, John A, Zhou, Jia

“…Although G protein-coupled receptors (GPCRs) are recognized as pivotal drug targets involved in multiple physiological and pathological processes, the majority…”
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Discovery of a Small Molecule Inhibitor of Human Adenovirus Capable of Preventing Escape from the Endosome by Xu, Jimin, Berastegui-Cabrera, Judith, Carretero-Ledesma, Marta, Chen, Haiying, Xue, Yu, Wold, Eric A, Pachón, Jerónimo, Zhou, Jia, Sánchez-Céspedes, Javier

“…Human adenoviruses (HAdVs) display a wide range of tissue tropism and can cause an array of symptoms from mild respiratory illnesses to disseminated and…”
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Drug Discovery Targeting Bromodomain-Containing Protein 4 by Liu, Zhiqing, Wang, Pingyuan, Chen, Haiying, Wold, Eric A, Tian, Bing, Brasier, Allan R, Zhou, Jia

“…BRD4, the most extensively studied member of the BET family, is an epigenetic regulator that localizes to DNA via binding to acetylated histones and controls…”
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Therapeutic Potential of Oridonin and Its Analogs: From Anticancer and Antiinflammation to Neuroprotection by Xu, Jimin, Wold, Eric A, Ding, Ye, Shen, Qiang, Zhou, Jia

“…Oridonin, a diterpenoid natural product commonly used in East Asian herbal medicine, is garnering increased attention in the biomedical community due to its…”
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Small Molecules Selectively Targeting Sigma‑1 Receptor for the Treatment of Neurological Diseases by Ye, Na, Qin, Wangzhi, Tian, Sheng, Xu, Qingfeng, Wold, Eric A, Zhou, Jia, Zhen, Xue-Chu

“…The sigma-1 (σ1) receptor, an enigmatic protein originally classified as an opioid receptor subtype, is now understood to possess unique structural and…”
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Small-Molecule Inhibitors Targeting the Canonical WNT Signaling Pathway for the Treatment of Cancer by Liu, Zhiqing, Wang, Pingyuan, Wold, Eric A, Song, Qiaoling, Zhao, Chenyang, Wang, Changyun, Zhou, Jia

“…Canonical WNT signaling is an important developmental pathway that has attracted increased attention for anticancer drug discovery. From the production and…”
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Discovery of Orally Bioavailable Chromone Derivatives as Potent and Selective BRD4 Inhibitors: Scaffold Hopping, Optimization, and Pharmacological Evaluation by Liu, Zhiqing, Chen, Haiying, Wang, Pingyuan, Li, Yi, Wold, Eric A, Leonard, Paul G, Joseph, Sarah, Brasier, Allan R, Tian, Bing, Zhou, Jia

“…Bromodomain-containing protein 4 (BRD4) represents a promising drug target for anti-inflammatory therapeutics. Herein, we report the design, synthesis, and…”
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BH4 domain of Bcl-2 as a novel target for cancer therapy by Liu, Zhiqing, Wild, Christopher, Ding, Ye, Ye, Na, Chen, Haiying, Wold, Eric A., Zhou, Jia

“…•No Bcl-2 inhibitors targeting the BH3 domain approved for clinical use.•BH4 domain of Bcl-2 is identified as a promising novel target for cancer…”
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Discovery, X‑ray Crystallography, and Anti-inflammatory Activity of Bromodomain-containing Protein 4 (BRD4) BD1 Inhibitors Targeting a Distinct New Binding Site by Liu, Zhiqing, Li, Yi, Chen, Haiying, Lai, Hsien-Tsung, Wang, Pingyuan, Wu, Shwu-Yuan, Wold, Eric A, Leonard, Paul G, Joseph, Sarah, Hu, Haitao, Chiang, Cheng-Ming, Brasier, Allan R, Tian, Bing, Zhou, Jia

“…Bromodomain-containing protein 4 (BRD4) is an emerging epigenetic drug target for intractable inflammatory disorders. The lack of highly selective inhibitors…”
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Regio- and Stereospecific Synthesis of Oridonin D‑Ring Aziridinated Analogues for the Treatment of Triple-Negative Breast Cancer via Mediated Irreversible Covalent Warheads by Ding, Ye, Li, Dengfeng, Ding, Chunyong, Wang, Pingyuan, Liu, Zhiqing, Wold, Eric A, Ye, Na, Chen, Haiying, White, Mark A, Shen, Qiang, Zhou, Jia

“…Covalent drug discovery has undergone a resurgence in recent years due to comprehensive optimization of the structure–activity relationship (SAR) and the…”
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Design, Synthesis, and Characterization of 4‑Undecylpiperidine-2-carboxamides as Positive Allosteric Modulators of the Serotonin (5-HT) 5‑HT2C Receptor by Wild, Christopher T, Miszkiel, Joanna M, Wold, Eric A, Soto, Claudia A, Ding, Chunyong, Hartley, Rachel M, White, Mark A, Anastasio, Noelle C, Cunningham, Kathryn A, Zhou, Jia

“…An impaired signaling capacity of the serotonin (5-HT) 5-HT2C receptor (5-HT2CR) has been implicated in the neurobehavioral processes that promote relapse…”
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Discovery of Novel Oleamide Analogues as Brain-Penetrant Positive Allosteric Serotonin 5‑HT2C Receptor and Dual 5‑HT2C/5-HT2A Receptor Modulators by Chen, Jianping, Garcia, Erik J., Merritt, Christina R., Zamora, Joshua C., Bolinger, Andrew A., Pazdrak, Konrad, Stafford, Susan J., Mifflin, Randy C., Wold, Eric A., Wild, Christopher T., Chen, Haiying, Anastasio, Noelle C., Cunningham, Kathryn A., Zhou, Jia

“…The serotonin 5-HT2A receptor (5-HT2AR) and 5-HT2CR localize to the brain and share overlapping signal transduction facets that contribute to their roles in…”
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Discovery of 4‑Phenylpiperidine-2-Carboxamide Analogues as Serotonin 5‑HT2C Receptor-Positive Allosteric Modulators with Enhanced Drug-like Properties by Wold, Eric A, Garcia, Erik J, Wild, Christopher T, Miszkiel, Joanna M, Soto, Claudia A, Chen, Jianping, Pazdrak, Konrad, Fox, Robert G, Anastasio, Noelle C, Cunningham, Kathryn A, Zhou, Jia

“…Targeting the serotonin (5-HT) 5-HT2C receptor (5-HT2CR) allosteric site to potentiate endogenous 5-HT tone may provide novel therapeutics to alleviate the…”
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Design, Synthesis, and Characterization of 4-Undecylpiperidine-2-carboxamides as Positive Allosteric Modulators of the Serotonin (5-HT) 5-HT 2C Receptor by Wild, Christopher T, Miszkiel, Joanna M, Wold, Eric A, Soto, Claudia A, Ding, Chunyong, Hartley, Rachel M, White, Mark A, Anastasio, Noelle C, Cunningham, Kathryn A, Zhou, Jia

“…An impaired signaling capacity of the serotonin (5-HT) 5-HT receptor (5-HT R) has been implicated in the neurobehavioral processes that promote relapse…”
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Structure-activity relationship studies on Bax activator SMBA1 for the treatment of ER-positive and triple-negative breast cancer by Liu, Gang, Yin, Tao, Kim, Hyejin, Ding, Chunyong, Yu, Zhuo, Wang, Hong, Chen, Haiying, Yan, Ruping, Wold, Eric A., Zou, Hao, Liu, Xi, Ding, Ye, Shen, Qiang, Zhou, Jia

“…In an effort to develop novel Bax activators for breast cancer treatment, a series of diverse analogues have been designed and synthesized based on lead…”
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