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ACS Pharmacology and Translational Science

Subject Areas: Pharmacology (medical)
Publisher: American Chemical Society - American Chemical Society
ISSN: 2575-9108
SJR: 20

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Journal Article

Drug-Repurposing Screening Identifies a Gallic Acid Binding Site on SARS-CoV‑2 Non-structural Protein 7

Gu, Yushu; Liu, Miaomiao; Staker, Bart L.; Buchko, Garry W.; Quinn, Ronald J.

2023 ACS Pharmacology & Translational Science

doi:10.1021/acsptsci.2c00225

SARS-CoV-2 is the agent responsible for acute respiratory disease COVID-19 and the global pandemic initiated in early 2020. While the record-breaking development of vaccines has assisted the control of COVID-19, there is still a pressing global demand for antiviral drugs to halt the destructive...
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Journal Article

Role of Turmeric and Curcumin in Prevention and Treatment of Chronic Diseases: Lessons Learned from Clinical Trials

Kunnumakkara, Ajaikumar B.; Hegde, Mangala; Parama, Dey; Girisa, Sosmitha; Kumar, Aviral; Daimary, Uzini Devi; Garodia, Prachi; Yenisetti, Sarat Chandra; Oommen, Oommen V.; Aggarwal, Bharat B.

2023 ACS Pharmacology & Translational Science

doi:10.1021/acsptsci.2c00012

Turmeric (Curcuma longa) has been used for thousands of years for the prevention and treatment of various chronic diseases. Curcumin is just one of >200 ingredients in turmeric. Almost 7000 scientific papers on turmeric and almost 20,000 on curcumin have been published in PubMed. Scientific...
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Journal Article

Novel, Brain-Permeable, Cross-Species Benzothiazole Inhibitors of Microsomal Prostaglandin E Synthase‑1 (mPGES-1) Dampen Neuroinflammation In Vitro and In Vivo

Sluter, Madison N.; Bhuniya, Rajib; Yuan, Xinrui; Ramaraju, Andhavaram; Chen, Yu; Yu, Ying; Parmar, Keyur R.; Temrikar, Zaid H.; Srivastava, Ashish; Meibohm, Bernd; Jiang, Jianxiong; Yang, Chao-Yie

2023 ACS Pharmacology & Translational Science

doi:10.1021/acsptsci.2c00241

Microsomal prostaglandin E synthase-1 (mPGES-1) is an inducible enzyme of the cyclooxygenase (COX) cascade that generates prostaglandin E2 (PGE2) during inflammatory conditions. PGE2 is known to be a potent immune signaling molecule that mediates both peripheral and central inflammations....
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Journal Article

Discovery of a High-Affinity Fluoromethyl Analog of [11C]5-Cyano-N-(4-(4-methylpiperazin-1-yl)-2-(piperidin-1-yl)phenyl)furan-2-carboxamide ([11C]CPPC) and Their Comparison in Mouse and Monkey as Colony-Stimulating Factor 1 Receptor Positron Emission Tomography Radioligands

Altomonte, Stefano; Yan, Xuefeng; Morse, Cheryl L.; Liow, Jeih-San; Jenkins, Madeline D.; Montero Santamaria, Jose A.; Zoghbi, Sami S.; Innis, Robert B.; Pike, Victor W.

2023 ACS Pharmacology & Translational Science

doi:10.1021/acsptsci.3c00003

[11C]CPPC has been advocated as a radioligand for colony-stimulating factor 1 receptor (CSF1R) with the potential for imaging neuroinflammation in human subjects with positron emission tomography (PET). This study sought to prepare fluoro analogs of CPPC with higher affinity to provide the...
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Journal Article

Receptor Binding Profiles for Tryptamine Psychedelics and Effects of 4‑Propionoxy-N,N-dimethyltryptamine in Mice

Glatfelter, Grant C.; Naeem, Marilyn; Pham, Duyen N. K.; Golen, James A.; Chadeayne, Andrew R.; Manke, David R.; Baumann, Michael H.

2023 ACS Pharmacology & Translational Science

doi:10.1021/acsptsci.2c00222

Analogues of 4-phosphoryloxy-N,N-dimethyltryptamine (psilocybin) are being sold on recreational drug markets and developed as potential medications for psychedelic-assisted therapies. Many of these tryptamine-based psilocybin analogues produce psychedelic-like effects in rodents and humans...
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Journal Article

Design, Synthesis, and Biological Evaluation of Pyrimidine Dihydroquinoxalinone Derivatives as Tubulin Colchicine Site-Binding Agents That Displayed Potent Anticancer Activity Both In Vitro and In Vivo

Pochampally, Satyanarayana; Hartman, Kelli L.; Wang, Rui; Wang, Jiaxing; Yun, Mi-Kyung; Parmar, Keyur; Park, Hyunseo; Meibohm, Bernd; White, Stephen W.; Li, Wei; Miller, Duane D.

2023 ACS Pharmacology & Translational Science

doi:10.1021/acsptsci.2c00108

Polymerization of tubulin dimers to form microtubules is one of the key events in cell proliferation. The inhibition of this event has long been recognized as a potential treatment option for various types of cancer. Compound 1e was previously developed by our team as a potent inhibitor of...
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Journal Article

Effects of Gabapentinoids on Heroin-Induced Ventilatory Depression and Reversal by Naloxone

Flynn, Shawn M.; France, Charles P.

2023 ACS Pharmacology & Translational Science

doi:10.1021/acsptsci.2c00230

Despite an increasing prevalence of gabapentinoids (gabapentin and pregabalin) in opioid overdose deaths, little research has evaluated potentially harmful interactions between gabapentinoids and opioids. This study sought to determine the effects of gabapentinoids on the ventilatory depressive...
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Journal Article

Biochemical Discovery, Intracellular Evaluation, and Crystallographic Characterization of Synthetic and Natural Product Adenosine 3′,5′-Cyclic Monophosphate-Dependent Protein Kinase A (PKA) Inhibitors

Wilson, Brice A. P.; Li, Ning; Martinez Fiesco, Juliana A.; Dalilian, Masoumeh; Wang, Dongdong; Smith, Emily A.; Wamiru, Antony; Shah, Rohan; Goncharova, Ekaterina I.; Beutler, John A.; Grkovic, Tanja; Zhang, Ping; O’Keefe, Barry R.

2023 ACS Pharmacology & Translational Science

doi:10.1021/acsptsci.3c00010

The recent demonstration that adenosine 3′,5′-cyclic monophosphate (cAMP)-dependent protein kinase A (PKA) plays an oncogenic role in a number of important cancers has led to a renaissance in drug development interest targeting this kinase. We therefore have established a suite of biochemical,...

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