Explanipedia

Hand, Foot, and Mouth Disease Risk Prediction in Southern China: Time Series Study Integrating Web-Based Search and Epidemiological Surveillance Data Open

Yixiong Chen, Xue Zhang, Sheng Zhang, Wenjie Han, Z Wang , et al. · 2025

Background Hand, foot, and mouth disease (HFMD) is a global health concern requiring a risk assessment framework based on systematic factors analysis for prevention and control. Objective This study aims to construct a comprehensive HFMD r…

Pretreated exosomes by electrical stimulation accelerate bone regeneration Open

Jialu Chen, Jian Jeffrey Chen, Jiahao Chen, Renjie Lu, Ziyuan Liu , et al. · 2025

Correction to “Discovery of CMX990: A Potent SARS-CoV-2 3CL Protease Inhibitor Bearing a Novel Warhead” Open

N. G. R. Dayan Elshan, Karen C. Wolff, Laura Riva, Ashley K. Woods, Gennadii A. Grabovyi , et al. · 2024

Discovery of CMX990: A Potent SARS-CoV-2 3CL Protease Inhibitor Bearing a Novel Warhead Open

N. G. R. Dayan Elshan, Karen C. Wolff, Laura Riva, Ashley K. Woods, Gennadii A. Grabovyi , et al. · 2024

There remains a need to develop novel SARS-CoV-2 therapeutic options that improve upon existing therapies by an increased robustness of response, fewer safety liabilities, and global-ready accessibility. Functionally critical viral main pr…

Discovery of CMX990: A Potent SARS-CoV-2 3CL Protease Inhibitor Bearing a Novel Covalent Warhead Open

N. G. R. Dayan Elshan, Karen C. Wolff, Laura Riva, Ashley K. Woods, Gennadii A. Grabovyi , et al. · 2023

There remains a need to develop novel SARS-CoV-2 therapeutic options that improve upon existing therapies by increased robustness of response, fewer safety liabilities, and global-ready accessibility. Functionally critical viral main prote…

Pharmacological YAP activation promotes regenerative repair of cutaneous wounds Open

Edyta M. Grzelak, N. G. R. Dayan Elshan, Sida Shao, Maya L. Bulos, Sean B. Joseph , et al. · 2023

Chronic cutaneous wounds remain a persistent unmet medical need that decreases life expectancy and quality of life. Here, we report that topical application of PY-60, a small-molecule activator of the transcriptional coactivator Yes-associ…

Targeting the Mitotic Kinesin KIF18A in Chromosomally Unstable Cancers: Hit Optimization Toward an In Vivo Chemical Probe Open

Nuria Tamayo, Matthew P. Bourbeau, Jennifer R. Allen, Kate S. Ashton, Jian Jeffrey Chen , et al. · 2022

Chromosomal instability (CIN) is a hallmark of cancer that results from errors in chromosome segregation during mitosis. Targeting of CIN-associated vulnerabilities is an emerging therapeutic strategy in drug development. KIF18A, a mitotic…

Discovery of a Covalent Inhibitor of KRASG12C (AMG 510) for the Treatment of Solid Tumors Open

Brian A. Lanman, Jennifer R. Allen, John G. Allen, Albert Amegadzie, Kate S. Ashton , et al. · 2019

KRASG12C has emerged as a promising target in the treatment of solid tumors. Covalent inhibitors targeting the mutant cysteine-12 residue have been shown to disrupt signaling by this long-“undruggable” target; however clinically viable inh…

Crystal structure of human KRAS G12C covalently bound to a phthalazine inhibitor Open

Brian A. Lanman, J.R. Allen, John G. Allen, Albert Amegadzie, Kate S. Ashton , et al. · 2019

KRAS^G12C has emerged as a promising target in the treatment of solid tumors. Covalent inhibitors targeting the mutant cysteine-12 residue have been shown to disrupt signaling by this long-"undruggable" target; however clinically…

Drug Repurposing: The Anthelmintics Niclosamide and Nitazoxanide Are Potent TMEM16A Antagonists That Fully Bronchodilate Airways Open

Kent Miner, Katja Labitzke, Benxian Liu, Paul Wang, Kathryn Henckels , et al. · 2019

There is an unmet need in severe asthma where approximately 40% of patients exhibit poor β-agonist responsiveness, suffer daily symptoms and show frequent exacerbations. Antagonists of the Ca²⁺-activated Cl^- channel, …

Discovery of TRPM8 Antagonist (S)-6-(((3-Fluoro-4-(trifluoromethoxy)phenyl)(3-fluoropyridin-2-yl)methyl)carbamoyl)nicotinic Acid (AMG 333), a Clinical Candidate for the Treatment of Migraine Open

Daniel B. Horne, Kaustav Biswas, James Brown, Michael D. Bartberger, Jeffrey Clarine , et al. · 2018

Transient-receptor-potential melastatin 8 (TRPM8), the predominant mammalian cold-temperature thermosensor, is a nonselective cation channel expressed in a subpopulation of sensory neurons in the peripheral nervous system, including nerve …

Drug Repurposing: The Anthelmintics Niclosamide and Nitazoxanide are Potent TMEM16A Antagonists that Fully Bronchodilate Airways Open

Kent Miner, Katja Labitzke, Benxian Liu, Paul Wang, Kathryn Henckels , et al. · 2018

There is an unmet need in severe asthma where approximately 40% of patients exhibit poor β-agonist responsiveness, suffer daily symptoms and show frequent exacerbations. Antagonists of the Ca 2+ -activated-Cl − channel, TMEM16A, offers a n…

CCDC 1841307: Experimental Crystal Structure Determination Open

Daniel B. Horne, Kaustav Biswas, James M. Brown, Michael D. Bartberger, Jeffrey Clarine , et al. · 2018

An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …

Oxopyrido[2,3-d]pyrimidines as Covalent L858R/T790M Mutant Selective Epidermal Growth Factor Receptor (EGFR) Inhibitors Open

Ryan P. Wurz, Liping H. Pettus, Kate Ashton, James Brown, Jian Jeffrey Chen , et al. · 2015

In nonsmall cell lung cancer (NSCLC), the threonine(790)-methionine(790) (T790M) point mutation of EGFR kinase is one of the leading causes of acquired resistance to the first generation tyrosine kinase inhibitors (TKIs), such as gefitinib…

Development of 2-aminooxazoline 3-azaxanthenes as orally efficacious β-secretase inhibitors for the potential treatment of Alzheimer’s disease Open

Jian Jeffrey Chen, Qingyian Liu, Chester Yuan, Vijay Gore, Patrícia Luciana da Costa Lopez , et al. · 2015

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