Synthesis and Pharmacological Evaluation of Tetrahydro-γ-carboline Derivatives as Potent Anti-inflammatory Agents Targeting Cyclic GMP

Synthesis and Pharmacological Evaluation of Tetrahydro-γ-carboline Derivatives as Potent Anti-inflammatory Agents Targeting Cyclic GMP–AMP Synthase

Published:2021-05-28 Issue:11 Volume:64 Page:7667-7690
ISSN:0022-2623
Container-title:Journal of Medicinal Chemistry
language:en
Short-container-title:J. Med. Chem.

Author:

Tan Jing¹²³,Wu Bing¹³,Chen Tingting²,Fan Chen¹³,Zhao Jiannan¹²³⁴,Xiong Chaodong¹²³,Feng Chunlan¹³,Xiao Ruoxuan²,Ding Chunyong²⁵,Tang Wei¹³,Zhang Ao¹²³⁴⁵^ORCID

Affiliation:

1. Shanghai Institute of Materia Medica (SIMM), Chinese Academy of Sciences, Shanghai 201203, China

2. Pharm-X Center, School of Pharmacy, Shanghai Jiao Tong University, Shanghai 200240, China

3. University of Chinese Academy of Sciences, Beijing 100049, China

4. School of Life Science and Technology, ShanghaiTech University, Shanghai 201210, China

5. Shanghai Key Laboratory for Molecular Engineering of Chiral Drugs, School of Pharmacy, Shanghai Jiao Tong University, Shanghai 200240, China

Funder

Shanghai Jiao Tong University

Science and Technology Commission of Shanghai Municipality

National Natural Science Foundation of China

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

Link

https://pubs.acs.org/doi/pdf/10.1021/acs.jmedchem.1c00398

Reference39 articles.

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2. Recognition of Endogenous Nucleic Acids by the Innate Immune System

3. Cyclic GMP-AMP Is an Endogenous Second Messenger in Innate Immune Signaling by Cytosolic DNA

4. The Cytosolic DNA Sensor cGAS Forms an Oligomeric Complex with DNA and Undergoes Switch-like Conformational Changes in the Activation Loop

5. STING is an endoplasmic reticulum adaptor that facilitates innate immune signalling

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