Vol 44, No 1 (January 2023) - Acta Pharmacologica Sinica

Review Article

AlphaFold2 versus experimental structures: evaluation on G protein-coupled receptors Pages (1–7)

Xin-heng He, Chong-zhao You, Hua-liang Jiang, Yi Jiang, H. Eric Xu, Xi Cheng

Protein O-GlcNAcylation in cardiovascular diseases Pages (8–18)

Hui-fang Wang, Yi-xuan Wang, Yu-ping Zhou, Yun-peng Wei, Yi Yan, Ze-jian Zhang, Zhi-cheng Jing

Formyl peptide receptor 2 as a potential therapeutic target for inflammatory bowel disease Pages (19–31)

Wen-sheng Yang, Jing-lin Wang, Wei Wu, Guang-fei Wang, Jun Yan, Qing Liu, Xiao-yan Wu, Qing-tong Zhou, De-hua Yang, Ming-Wei Wang, Zhi-ping Li

Article

Pramipexole inhibits astrocytic NLRP3 inflammasome activation via Drd3-dependent autophagy in a mouse model of Parkinson’s disease Pages (32–43) Open

An-qi Dong, Ya-ping Yang, Shu-min Jiang, Xiao-yu Yao, Di Qi, Cheng-jie Mao, Xiao-yu Cheng, Fen Wang, Li-fang Hu, Chun-feng Liu

Low-dose nifedipine rescues impaired endothelial progenitor cell-mediated angiogenesis in diabetic mice Pages (44–57)

Cheng Peng, Li-jun Yang, Chuan Zhang, Yu Jiang, Liu-wen-xin Shang, Jia-bei He, Zhen-wei Zhou, Xia Tao, Lu Tie, Alex F. Chen, He-hui Xie

Costunolide alleviates atherosclerosis in high-fat diet-fed ApoE^−/− mice through covalently binding to IKKβ and inhibiting NF-κB-mediated inflammation Pages (58–70)

Zhu-qi Huang, Wu Luo, Wei-xin Li, Pan Chen, Zhe Wang, Rui-jie Chen, Yi Wang, Wei-jian Huang, Guang Liang

EPSTI1 promotes monocyte adhesion to endothelial cells in vitro via upregulating VCAM-1 and ICAM-1 expression Pages (71–80)

Yan-rou Bei, Shun-chi Zhang, Yu Song, Mao-lin Tang, Ke-lan Zhang, Min Jiang, Run-chao He, Shao-guo Wu, Xue-hui Liu, Li-mei Wu, Xiao-yan Dai, Yan-wei Hu

CP-25 enhances OAT1-mediated absorption of methotrexate in synoviocytes of collagen-induced arthritis rats Pages (81–91)

Chun Wang, Hao Tang, Yong Wang, Yan Chang, Yi-jin Wu, Bin Wang, Wei Sun, Feng Xiao, Wei Wei

TGFβR-1/ALK5 inhibitor RepSox induces enteric glia-to- neuron transition and influences gastrointestinal mobility in adult mice Pages (92–104) Open

Chang-jie Shi, Jun-jiang Lian, Bo-wen Zhang, Jia-xue Cha, Qiu-hong Hua, Xiao-ping Pi, Yu-jun Hou, Xin Xie, Ru Zhang

Hederacoside C ameliorates colitis via restoring impaired intestinal barrier through moderating S100A9/MAPK and neutrophil recruitment inactivation Pages (105–119)

Zheng-xia Zha, Yu Lin, Ke-xin Wang, Yan-lin Zhang, Dan Li, Guo-qiang Xu, Qiong-ming Xu, Yan-li Liu

Dectin-1 plays a deleterious role in high fat diet-induced NAFLD of mice through enhancing macrophage activation Pages (120–132)

Min-xiu Wang, Wu Luo, Lin Ye, Lei-ming Jin, Bin Yang, Qian-hui Zhang, Jian-chang Qian, Yi Wang, Yi Zhang, Guang Liang

Silybin regulates P450s activity by attenuating endoplasmic reticulum stress in mouse nonalcoholic fatty liver disease Pages (133–144)

Jing Wu, Yun-ge Lou, Xu-le Yang, Rui Wang, Ran Zhang, Ji-ye Aa, Guang-ji Wang, Yuan Xie

Caffeic acid phenethyl ester suppresses intestinal FXR signaling and ameliorates nonalcoholic fatty liver disease by inhibiting bacterial bile salt hydrolase activity Pages (145–156)

Xian-chun Zhong, Ya-meng Liu, Xiao-xia Gao, Kristopher W. Krausz, Bing Niu, Frank J. Gonzalez, Cen Xie

Hepatocyte-derived MANF mitigates ethanol-induced liver steatosis in mice via enhancing ASS1 activity and activating AMPK pathway Pages (157–168)

Han-yang Xu, Yan-hong Jiao, Shi-yu Li, Xu Zhu, Sheng Wang, Yu-yang Zhang, Yi-jun Wei, Yu-jun Shen, Wei Wang, Yu-xian Shen, Jun-tang Shao

Long-term treatment with the mPXR agonist PCN promotes hepatomegaly and lipid accumulation without hepatocyte proliferation in mice Pages (169–177)

Yi-fei Zhang, Yue Gao, Jie Yang, Yi-ming Jiang, Min Huang, Shi-cheng Fan, Hui-chang Bi

Calcipotriol abrogates cancer-associated fibroblast-derived IL-8-mediated oxaliplatin resistance in gastric cancer cells via blocking PI3K/Akt signaling Pages (178–188)

Zhen-xiong Zhao, Yan-qiu Zhang, Hui Sun, Zi-qi Chen, Jin-jia Chang, Xin Wang, Xu Wang, Cong Tan, Shu-juan Ni, Wei-wei Weng, Meng Zhang, Lei Wang, Dan Huang, Yun Feng, Wei-qi Sheng, Mi-die Xu

Aiphanol, a multi-targeting stilbenolignan, potently suppresses mouse lymphangiogenesis and lymphatic metastasis Pages (189–200)

Shan-mei Chen, Chuan-ke Zhao, Li-cheng Yao, Li-xin Wang, Yu-nan Ma, Lin Meng, Shao-qing Cai, Cai-yun Liu, Li-ke Qu, Yan-xing Jia, Cheng-chao Shou

The hybrid oncolytic peptide NTP-385 potently inhibits adherent cancer cells by targeting the nucleus Pages (201–210)

Hao Yin, Xi-tong Chen, Qiao-na Chi, Yan-nan Ma, Xing-yan Fu, Shan-shan Du, Yun-kun Qi, Ke-wei Wang

Aspirin modulates succinylation of PGAM1K99 to restrict the glycolysis through NF-κB/HAT1/PGAM1 signaling in liver cancer Pages (211–220)

Yu-fei Wang, Li-na Zhao, Yu Geng, Hong-feng Yuan, Chun-yu Hou, Hui-hui Zhang, Guang Yang, Xiao-dong Zhang

Pharmacokinetics, mass balance, and metabolism of [¹⁴C] TPN171, a novel PDE5 inhibitor, in humans for the treatment of pulmonary arterial hypertension Pages (221–233)

Yi-fei He, Yin Liu, Jing-hua Yu, Huan Cheng, Abdullajon Odilov, Fei-pu Yang, Guang-hui Tian, Xiu-mei Yao, Hua-qing Duan, Cheng-yin Yu, Chen Yu, Yan-mei Liu, Gang-yi Liu, Jing-shan Shen, Zhen Wang, Xing-xing Diao

Discovery of toxoflavin, a potent IRE1α inhibitor acting through structure-dependent oxidative inhibition Pages (234–243)

Kai-long Jiang, Chang-mei Liu, Li-tong Nie, Hai-ni Jiang, Lei Xu, Kun-zhi Zhang, Li-xia Fan, An-hui Gao, Lu-ling Lin, Xiang-yu Wang, Ming-jia Tan, Qi-qing Zhang, Yu-bo Zhou, Jia Li

Dual-responsive nanoparticles loading bevacizumab and gefitinib for molecular targeted therapy against non-small cell lung cancer Pages (244–254)

Zi-tong Zhao, Jue Wang, Lei Fang, Xin-di Qian, Ying Cai, Hai-qiang Cao, Guan-ru Wang, Mei-lin He, Yan-yan Jiang, Dang-ge Wang, Ya-ping Li

Correspondence

Structure basis for inhibition of SARS-CoV-2 by the feline drug GC376 Pages (255–257)

Xiao-dong Luan, Bin-xian Chen, Wei-juan Shang, Wan-chao Yin, Ye Jin, Lei-ke Zhang, H. Eric Xu, Shu-yang Zhang

Correction

Author Correction: Structure basis for inhibition of SARS-CoV-2 by the feline drug GC376 Pages (258)

Xiao-dong Luan, Bin-xian Chen, Wei-juan Shang, Wan-chao Yin, Ye Jin, Lei-ke Zhang, H. Eric Xu, Shu-yang Zhang

Vol 44, No 1 (January 2023): Acta Pharmacologica Sinica

Review Article

AlphaFold2 versus experimental structures: evaluation on G protein-coupled receptors Pages (1–7)

Protein O-GlcNAcylation in cardiovascular diseases Pages (8–18)

Formyl peptide receptor 2 as a potential therapeutic target for inflammatory bowel disease Pages (19–31)

Article

Pramipexole inhibits astrocytic NLRP3 inflammasome activation via Drd3-dependent autophagy in a mouse model of Parkinson’s disease Pages (32–43) Open

Low-dose nifedipine rescues impaired endothelial progenitor cell-mediated angiogenesis in diabetic mice Pages (44–57)

Costunolide alleviates atherosclerosis in high-fat diet-fed ApoE^−/− mice through covalently binding to IKKβ and inhibiting NF-κB-mediated inflammation Pages (58–70)

EPSTI1 promotes monocyte adhesion to endothelial cells in vitro via upregulating VCAM-1 and ICAM-1 expression Pages (71–80)

CP-25 enhances OAT1-mediated absorption of methotrexate in synoviocytes of collagen-induced arthritis rats Pages (81–91)

TGFβR-1/ALK5 inhibitor RepSox induces enteric glia-to- neuron transition and influences gastrointestinal mobility in adult mice Pages (92–104) Open

Hederacoside C ameliorates colitis via restoring impaired intestinal barrier through moderating S100A9/MAPK and neutrophil recruitment inactivation Pages (105–119)

Dectin-1 plays a deleterious role in high fat diet-induced NAFLD of mice through enhancing macrophage activation Pages (120–132)

Silybin regulates P450s activity by attenuating endoplasmic reticulum stress in mouse nonalcoholic fatty liver disease Pages (133–144)

Caffeic acid phenethyl ester suppresses intestinal FXR signaling and ameliorates nonalcoholic fatty liver disease by inhibiting bacterial bile salt hydrolase activity Pages (145–156)

Hepatocyte-derived MANF mitigates ethanol-induced liver steatosis in mice via enhancing ASS1 activity and activating AMPK pathway Pages (157–168)

Long-term treatment with the mPXR agonist PCN promotes hepatomegaly and lipid accumulation without hepatocyte proliferation in mice Pages (169–177)

Calcipotriol abrogates cancer-associated fibroblast-derived IL-8-mediated oxaliplatin resistance in gastric cancer cells via blocking PI3K/Akt signaling Pages (178–188)

Aiphanol, a multi-targeting stilbenolignan, potently suppresses mouse lymphangiogenesis and lymphatic metastasis Pages (189–200)

The hybrid oncolytic peptide NTP-385 potently inhibits adherent cancer cells by targeting the nucleus Pages (201–210)

Aspirin modulates succinylation of PGAM1K99 to restrict the glycolysis through NF-κB/HAT1/PGAM1 signaling in liver cancer Pages (211–220)

Pharmacokinetics, mass balance, and metabolism of [¹⁴C] TPN171, a novel PDE5 inhibitor, in humans for the treatment of pulmonary arterial hypertension Pages (221–233)

Discovery of toxoflavin, a potent IRE1α inhibitor acting through structure-dependent oxidative inhibition Pages (234–243)

Dual-responsive nanoparticles loading bevacizumab and gefitinib for molecular targeted therapy against non-small cell lung cancer Pages (244–254)

Correspondence

Structure basis for inhibition of SARS-CoV-2 by the feline drug GC376 Pages (255–257)

Correction

Author Correction: Structure basis for inhibition of SARS-CoV-2 by the feline drug GC376 Pages (258)

Table of Contents

Cover Image

Vol 44, No 1 (January 2023): Acta Pharmacologica Sinica

Review Article

AlphaFold2 versus experimental structures: evaluation on G protein-coupled receptors Pages (1–7)

Protein O-GlcNAcylation in cardiovascular diseases Pages (8–18)

Formyl peptide receptor 2 as a potential therapeutic target for inflammatory bowel disease Pages (19–31)

Article

Pramipexole inhibits astrocytic NLRP3 inflammasome activation via Drd3-dependent autophagy in a mouse model of Parkinson’s disease Pages (32–43) Open

Low-dose nifedipine rescues impaired endothelial progenitor cell-mediated angiogenesis in diabetic mice Pages (44–57)

Costunolide alleviates atherosclerosis in high-fat diet-fed ApoE−/− mice through covalently binding to IKKβ and inhibiting NF-κB-mediated inflammation Pages (58–70)

EPSTI1 promotes monocyte adhesion to endothelial cells in vitro via upregulating VCAM-1 and ICAM-1 expression Pages (71–80)

CP-25 enhances OAT1-mediated absorption of methotrexate in synoviocytes of collagen-induced arthritis rats Pages (81–91)

TGFβR-1/ALK5 inhibitor RepSox induces enteric glia-to- neuron transition and influences gastrointestinal mobility in adult mice Pages (92–104) Open

Hederacoside C ameliorates colitis via restoring impaired intestinal barrier through moderating S100A9/MAPK and neutrophil recruitment inactivation Pages (105–119)

Dectin-1 plays a deleterious role in high fat diet-induced NAFLD of mice through enhancing macrophage activation Pages (120–132)

Silybin regulates P450s activity by attenuating endoplasmic reticulum stress in mouse nonalcoholic fatty liver disease Pages (133–144)

Caffeic acid phenethyl ester suppresses intestinal FXR signaling and ameliorates nonalcoholic fatty liver disease by inhibiting bacterial bile salt hydrolase activity Pages (145–156)

Hepatocyte-derived MANF mitigates ethanol-induced liver steatosis in mice via enhancing ASS1 activity and activating AMPK pathway Pages (157–168)

Long-term treatment with the mPXR agonist PCN promotes hepatomegaly and lipid accumulation without hepatocyte proliferation in mice Pages (169–177)

Calcipotriol abrogates cancer-associated fibroblast-derived IL-8-mediated oxaliplatin resistance in gastric cancer cells via blocking PI3K/Akt signaling Pages (178–188)

Aiphanol, a multi-targeting stilbenolignan, potently suppresses mouse lymphangiogenesis and lymphatic metastasis Pages (189–200)

The hybrid oncolytic peptide NTP-385 potently inhibits adherent cancer cells by targeting the nucleus Pages (201–210)

Aspirin modulates succinylation of PGAM1K99 to restrict the glycolysis through NF-κB/HAT1/PGAM1 signaling in liver cancer Pages (211–220)

Pharmacokinetics, mass balance, and metabolism of [14C] TPN171, a novel PDE5 inhibitor, in humans for the treatment of pulmonary arterial hypertension Pages (221–233)

Discovery of toxoflavin, a potent IRE1α inhibitor acting through structure-dependent oxidative inhibition Pages (234–243)

Dual-responsive nanoparticles loading bevacizumab and gefitinib for molecular targeted therapy against non-small cell lung cancer Pages (244–254)

Correspondence

Structure basis for inhibition of SARS-CoV-2 by the feline drug GC376 Pages (255–257)

Correction

Author Correction: Structure basis for inhibition of SARS-CoV-2 by the feline drug GC376 Pages (258)

Table of Contents

Cover Image

Costunolide alleviates atherosclerosis in high-fat diet-fed ApoE^−/− mice through covalently binding to IKKβ and inhibiting NF-κB-mediated inflammation Pages (58–70)

Pharmacokinetics, mass balance, and metabolism of [¹⁴C] TPN171, a novel PDE5 inhibitor, in humans for the treatment of pulmonary arterial hypertension Pages (221–233)