Frizzled receptors (FZDs) in Wnt signaling: potential therapeutic targets for human cancers
Acta Pharmacol Sin. 2024 Apr 17. doi: 10.1038/s41401-024-01270-3. Online ahead of print.ABSTRACTFrizzled receptors (FZDs) are key contributors intrinsic to the Wnt signaling pathway, activation of FZDs triggering the Wnt signaling cascade is frequently observed in human tumors and intimately associated with an aggressive carcinoma phenotype. It has been shown that the abnormal expression of FZD receptors contributes to the manifestation of malignant characteristics in human tumors such as enhanced cell proliferation, metastasis, chemotherapy resistance as well as the acquisition of cancer stemness. Given the essential role...
Source: Acta Pharmacologica Sinica - April 17, 2024 Category: Drugs & Pharmacology Authors: Hui-Yu Liu Xiao-Jiao Sun Si-Yu Xiu Xiang-Yu Zhang Zhi-Qi Wang Yan-Lun Gu Chu-Xiao Yi Jun-Yan Liu Yu-Song Dai Xia Yuan Hua-Peng Liao Zhen-Ming Liu Xiao-Cong Pang Tian-Cheng Li Source Type: research
Liver receptor homolog-1: structures, related diseases, and drug discovery
Acta Pharmacol Sin. 2024 Apr 17. doi: 10.1038/s41401-024-01276-x. Online ahead of print.ABSTRACTLiver receptor homolog-1 (LRH-1), a member of the nuclear receptor superfamily, is a ligand-regulated transcription factor that plays crucial roles in metabolism, development, and immunity. Despite being classified as an 'orphan' receptor due to the ongoing debate surrounding its endogenous ligands, recent researches have demonstrated that LRH-1 can be modulated by various synthetic ligands. This highlights the potential of LRH-1 as an attractive drug target for the treatment of inflammation, metabolic disorders, and cancer. In ...
Source: Acta Pharmacologica Sinica - April 17, 2024 Category: Drugs & Pharmacology Authors: Tong Wu Zhi-Fang Lu Hao-Nan Yu Xi-Shan Wu Yang Liu Yong Xu Source Type: research
Frizzled receptors (FZDs) in Wnt signaling: potential therapeutic targets for human cancers
Acta Pharmacologica Sinica, Published online: 17 April 2024; doi:10.1038/s41401-024-01270-3Frizzled receptors (FZDs) in Wnt signaling: potential therapeutic targets for human cancers (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - April 17, 2024 Category: Drugs & Pharmacology Authors: Hui-yu Liu Xiao-jiao Sun Si-yu Xiu Xiang-yu Zhang Zhi-qi Wang Yan-lun Gu Chu-xiao Yi Jun-yan Liu Yu-song Dai Xia Yuan Hua-peng Liao Zhen-ming Liu Xiao-cong Pang Tian-cheng Li Source Type: research
Liver receptor homolog-1: structures, related diseases, and drug discovery
Acta Pharmacologica Sinica, Published online: 17 April 2024; doi:10.1038/s41401-024-01276-xLiver receptor homolog-1: structures, related diseases, and drug discovery (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - April 17, 2024 Category: Drugs & Pharmacology Authors: Tong Wu Zhi-fang Lu Hao-nan Yu Xi-shan Wu Yang Liu Yong Xu Source Type: research
Ripretinib inhibits HIV-1 transcription through modulation of PI3K-AKT-mTOR
In this study, we performed high-throughput screening of FDA-approved compound library in the J-Lat A2 cell line to discover more efficacious LPAs. We discovered ripretinib being an LPA candidate, which was validated and observed to hinder proviral activation in cell models harboring latent infections, as well as CD4+ T cells derived from infected patients. We demonstrated that ripretinib effectively impeded proviral activation through inhibition of the PI3K-AKT-mTOR signaling pathway in the HIV-1 latent cells, thereby suppressing the opening states of cellular chromatin. The results of this research offer a promising drug...
Source: Acta Pharmacologica Sinica - April 16, 2024 Category: Drugs & Pharmacology Authors: Jin-Feng Cai Jia-Sheng Zhou Zhuo-Yue Meng Zi-Qi Wu Jia-Cong Zhao Hai-Xiang Peng Xin-Yu Liang Jun-Jian Chen Pei-Pei Wang Kai Deng Source Type: research
Ripretinib inhibits HIV-1 transcription through modulation of PI3K-AKT-mTOR
Acta Pharmacologica Sinica, Published online: 16 April 2024; doi:10.1038/s41401-024-01282-zRipretinib inhibits HIV-1 transcription through modulation of PI3K-AKT-mTOR (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - April 16, 2024 Category: Drugs & Pharmacology Authors: Jin-feng Cai Jia-sheng Zhou Zhuo-yue Meng Zi-qi Wu Jia-cong Zhao Hai-xiang Peng Xin-yu Liang Jun-jian Chen Pei-pei Wang Kai Deng Source Type: research
Transcriptional regulation and post-translational modifications in the glycolytic pathway for targeted cancer therapy
Acta Pharmacol Sin. 2024 Apr 15. doi: 10.1038/s41401-024-01264-1. Online ahead of print.ABSTRACTCancer cells largely rely on aerobic glycolysis or the Warburg effect to generate essential biomolecules and energy for their rapid growth. The key modulators in glycolysis including glucose transporters and enzymes, e.g. hexokinase 2, enolase 1, pyruvate kinase M2, lactate dehydrogenase A, play indispensable roles in glucose uptake, glucose consumption, ATP generation, lactate production, etc. Transcriptional regulation and post-translational modifications (PTMs) of these critical modulators are important for signal transductio...
Source: Acta Pharmacologica Sinica - April 15, 2024 Category: Drugs & Pharmacology Authors: Xuan Ni Cheng-Piao Lu Guo-Qiang Xu Jing-Jing Ma Source Type: research
Transcriptional regulation and post-translational modifications in the glycolytic pathway for targeted cancer therapy
Acta Pharmacol Sin. 2024 Apr 15. doi: 10.1038/s41401-024-01264-1. Online ahead of print.ABSTRACTCancer cells largely rely on aerobic glycolysis or the Warburg effect to generate essential biomolecules and energy for their rapid growth. The key modulators in glycolysis including glucose transporters and enzymes, e.g. hexokinase 2, enolase 1, pyruvate kinase M2, lactate dehydrogenase A, play indispensable roles in glucose uptake, glucose consumption, ATP generation, lactate production, etc. Transcriptional regulation and post-translational modifications (PTMs) of these critical modulators are important for signal transductio...
Source: Acta Pharmacologica Sinica - April 15, 2024 Category: Drugs & Pharmacology Authors: Xuan Ni Cheng-Piao Lu Guo-Qiang Xu Jing-Jing Ma Source Type: research
Transcriptional regulation and post-translational modifications in the glycolytic pathway for targeted cancer therapy
Acta Pharmacologica Sinica, Published online: 15 April 2024; doi:10.1038/s41401-024-01264-1Transcriptional regulation and post-translational modifications in the glycolytic pathway for targeted cancer therapy (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - April 15, 2024 Category: Drugs & Pharmacology Authors: Xuan Ni Cheng-piao Lu Guo-qiang Xu Jing-jing Ma Source Type: research
Tumor-targeted PROTAC prodrug nanoplatform enables precise protein degradation and combination cancer therapy
This study paves the way for utilizing tumor-targeted protein degradation for precise anticancer therapy and the effective combination treatment of complex diseases.PMID:38609561 | DOI:10.1038/s41401-024-01266-z (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - April 12, 2024 Category: Drugs & Pharmacology Authors: Zhi-Feng Zou Lei Yang Hui-Jun Nie Jing Gao Shu-Min Lei Yi Lai Fan Zhang Ernst Wagner Hai-Jun Yu Xiao-Hua Chen Zhi-Ai Xu Source Type: research
Novel STAT3 oligonucleotide compounds suppress tumor growth and overcome the acquired resistance to sorafenib in hepatocellular carcinoma
Acta Pharmacol Sin. 2024 Apr 12. doi: 10.1038/s41401-024-01261-4. Online ahead of print.ABSTRACTSignal transducer and activator of transcription 3 (STAT3) plays an important role in the occurrence and progression of tumors, leading to resistance and poor prognosis. Activation of STAT3 signaling is frequently detected in hepatocellular carcinoma (HCC), but potent and less toxic STAT3 inhibitors have not been discovered. Here, based on antisense technology, we designed a series of stabilized modified antisense oligonucleotides targeting STAT3 mRNA (STAT3 ASOs). Treatment with STAT3 ASOs decreased the STAT3 mRNA and protein l...
Source: Acta Pharmacologica Sinica - April 12, 2024 Category: Drugs & Pharmacology Authors: Qi-Yi Zhang Wen Ding Jian-Shan Mo Shu-Min Ou-Yang Zi-You Lin Ke-Ren Peng Guo-Pin Liu Jin-Jian Lu Pei-Bin Yue Jin-Ping Lei Yan-Dong Wang Xiao-Lei Zhang Source Type: research
Tumor-targeted PROTAC prodrug nanoplatform enables precise protein degradation and combination cancer therapy
This study paves the way for utilizing tumor-targeted protein degradation for precise anticancer therapy and the effective combination treatment of complex diseases.PMID:38609561 | DOI:10.1038/s41401-024-01266-z (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - April 12, 2024 Category: Drugs & Pharmacology Authors: Zhi-Feng Zou Lei Yang Hui-Jun Nie Jing Gao Shu-Min Lei Yi Lai Fan Zhang Ernst Wagner Hai-Jun Yu Xiao-Hua Chen Zhi-Ai Xu Source Type: research
Novel STAT3 oligonucleotide compounds suppress tumor growth and overcome the acquired resistance to sorafenib in hepatocellular carcinoma
Acta Pharmacol Sin. 2024 Apr 12. doi: 10.1038/s41401-024-01261-4. Online ahead of print.ABSTRACTSignal transducer and activator of transcription 3 (STAT3) plays an important role in the occurrence and progression of tumors, leading to resistance and poor prognosis. Activation of STAT3 signaling is frequently detected in hepatocellular carcinoma (HCC), but potent and less toxic STAT3 inhibitors have not been discovered. Here, based on antisense technology, we designed a series of stabilized modified antisense oligonucleotides targeting STAT3 mRNA (STAT3 ASOs). Treatment with STAT3 ASOs decreased the STAT3 mRNA and protein l...
Source: Acta Pharmacologica Sinica - April 12, 2024 Category: Drugs & Pharmacology Authors: Qi-Yi Zhang Wen Ding Jian-Shan Mo Shu-Min Ou-Yang Zi-You Lin Ke-Ren Peng Guo-Pin Liu Jin-Jian Lu Pei-Bin Yue Jin-Ping Lei Yan-Dong Wang Xiao-Lei Zhang Source Type: research
Tumor-targeted PROTAC prodrug nanoplatform enables precise protein degradation and combination cancer therapy
Acta Pharmacologica Sinica, Published online: 12 April 2024; doi:10.1038/s41401-024-01266-zTumor-targeted PROTAC prodrug nanoplatform enables precise protein degradation and combination cancer therapy (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - April 12, 2024 Category: Drugs & Pharmacology Authors: Zhi-feng Zou Lei Yang Hui-jun Nie Jing Gao Shu-min Lei Yi Lai Fan Zhang Ernst Wagner Hai-jun Yu Xiao-hua Chen Zhi-ai Xu Source Type: research
Novel STAT3 oligonucleotide compounds suppress tumor growth and overcome the acquired resistance to sorafenib in hepatocellular carcinoma
Acta Pharmacologica Sinica, Published online: 12 April 2024; doi:10.1038/s41401-024-01261-4Novel STAT3 oligonucleotide compounds suppress tumor growth and overcome the acquired resistance to sorafenib in hepatocellular carcinoma (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - April 12, 2024 Category: Drugs & Pharmacology Authors: Qi-yi Zhang Wen Ding Jian-shan Mo Shu-min Ou-yang Zi-you Lin Ke-ren Peng Guo-pin Liu Jin-jian Lu Pei-bin Yue Jin-ping Lei Yan-dong Wang Xiao-lei Zhang Source Type: research
