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Acta Pharmacologica Sinica

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https://www.readbyqxmd.com/read/28414207/defining-the-minimum-substrate-and-charge-recognition-model-of-gamma-secretase
#1
Yan Yan, Ting-Hai Xu, Karsten Melcher, H Eric Xu
γ-Secretase is an intramembrane aspartyl protease that cleaves the C99 fragment of amyloid precursor protein to generate extracellular Aβ peptides. These peptides can oligomerize and aggregate to form amyloid plaques, processes that are widely believed to be causal for Alzheimer's disease. In spite of this critical function, it remains unknown how γ-secretase recognizes C99 and its other substrates, including Notch. In this study we determined E22-K55 as the minimal C99 fragment that was sufficient and required for initial cleavage...
April 17, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28414206/wenshen-zhuanggu-formula-effectively-suppresses-breast-cancer-bone-metastases-in-a-mouse-xenograft-model
#2
Jia-Jia Li, Wei-Ling Chen, Jian-Yi Wang, Qian-Wen Hu, Zhen-Ping Sun, Shuai Zhang, Sheng Liu, Xiang-Hui Han
Wenshen Zhuanggu formula (WSZG) is a traditional Chinese medicine used as an adjuvant for the prevention of bone metastases in breast cancer patients. In this study we investigated the efficacy of WSZG in preventing bone metastases and the potential mechanisms in a mouse xenograft model of breast cancer bone metastases. This model was established by injection of human MDA-MB-231BO-Luc breast cancer cells alone or a mixture of the cancer cells with bone marrow-derived mesenchymal stem cells (BMSCs) into left ventricle of the heart in female nude mice...
April 17, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28414205/molecular-tumor-targeting-of-gelonin-by-fusion-with-f3-peptide
#3
Song-Hee Ham, Kyoung Ah Min, Meong Cheol Shin
Therapeutically potent macromolecular drugs have shown great promise for overcoming the limitations of small-molecule anti-cancer drugs. But tumor cell-selective intracellular delivery of the macromolecules remains a major hurdle for their successful clinical application. To overcome this challenge, we engineered a novel genetic fusion protein (F3-Gel) that composed of F3 peptide, a tumor-homing peptide, and gelonin, a plant-derived ribosome-inactivating protein (RIP), and then evaluated its anti-cancer activity in vitro and in vivo...
April 17, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28414204/docking-based-structural-splicing-and-reassembly-strategy-to-develop-novel-deazapurine-derivatives-as-potent-b-raf-v600e-inhibitors
#4
Gui-Min Wang, Xiang Wang, Jian-Ming Zhu, Bin-Bin Guo, Zhuo Yang, Zhi-Jian Xu, Bo Li, He-Yao Wang, Ling-Hua Meng, Wei-Liang Zhu, Jian Ding
The mutation of B-Raf(V600E) is widespread in a variety of human cancers. Its inhibitors vemurafenib and dabrafenib have been launched as drugs for treating unresectable melanoma, demonstrating that B-Raf(V600E) is an ideal drug target. This study focused on developing novel B-Raf(V600E) inhibitors as drug leads against various cancers with B-Raf(V600E) mutation. Using molecular modeling approaches, 200 blockbuster drugs were spliced to generate 283 fragments followed by molecular docking to identify potent fragments...
April 17, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28414203/self-assembled-nanocomplex-between-polymerized-phenylboronic-acid-and-doxorubicin-for-efficient-tumor-targeted-chemotherapy
#5
Junseok Lee, Jinhwan Kim, Yeong Mi Lee, Dongsik Park, Sooseok Im, Eun Ho Song, Hansoo Park, Won Jong Kim
Since the discovery that nano-scaled particulates can easily be incorporated into tumors via the enhanced permeability and retention (EPR) effect, such nanostructures have been exploited as therapeutic small molecule delivery systems. However, the convoluted synthetic process of conventional nanostructures has impeded their feasibility and reproducibility in clinical applications. Herein, we report an easily prepared formulation of self-assembled nanostructures for systemic delivery of the anti-cancer drug doxorubicin (DOX)...
April 17, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28414202/recent-advances-in-peptide-nucleic-acid-for-cancer-bionanotechnology
#6
REVIEW
Jun-Chen Wu, Qing-Chun Meng, Hong-Mei Ren, Hong-Tao Wang, Jie Wu, Qi Wang
Peptide nucleic acid (PNA) is an oligomer, in which the phosphate backbone has been replaced by a pseudopeptide backbone that is meant to mimic DNA. Peptide nucleic acids are of the utmost importance in the biomedical field because of their ability to hybridize with neutral nucleic acids and their special chemical and biological properties. In recent years, PNAs have emerged in nanobiotechnology for cancer diagnosis and therapy due to their high affinity and sequence selectivity toward corresponding DNA and RNA...
April 17, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28414201/intrinsic-radiolabeling-of-titanium-45-using-mesoporous-silica-nanoparticles
#7
Feng Chen, Hector F Valdovinos, Reinier Hernandez, Shreya Goel, Todd E Barnhart, Weibo Cai
Titanium-45 ((45)Ti) with a three-hour half-life (t1/2=3.08 h), low maximum positron energy and high positron emission branching ratio, is a suitable positron emission tomography (PET) isotope whose potential has not yet been fully explored. Complicated radiochemistry and rapid hydrolysis continue to be major challenges to the development of (45)Ti compounds based on a traditional chelator-based radiolabeling strategy. In this study we introduced an intrinsic (or chelator-free) radiolabeling technique for the successful labeling of (45)Ti using mesoporous silica nanoparticle (MSN)...
April 17, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28414200/combining-53bp1-with-brca1-as-a-biomarker-to-predict-the-sensitivity-of-poly-adp-ribose-polymerase-parp-inhibitors
#8
Zhong-Min Yang, Xue-Mei Liao, Yi Chen, Yan-Yan Shen, Xin-Ying Yang, Yi Su, Yi-Ming Sun, Ying-Lei Gao, Jian Ding, Ao Zhang, Jin-Xue He, Ze-Hong Miao
Over half of patients with BRCA1-deficient cancers do not respond to treatment with poly(ADP-ribose) polymerase (PARP) inhibitors. In this study, we report that a combination of 53BP1 and BRCA1 may serve as a biomarker of PARP inhibitor sensitivity. Based on the mRNA levels of four homologous recombination repair (HR) genes and PARP inhibitor sensitivity, we selected BRCA1-deficient MDA-MB-436 cells to conduct RNA interference. Reducing expression of 53BP1, but not the other three HR genes, was found to lower simmiparib sensitivity...
April 17, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28414199/structure-of-the-prc2-complex-and-application-to-drug-discovery
#9
REVIEW
Yi Shi, Xiao-Xi Wang, You-Wen Zhuang, Yi Jiang, Karsten Melcher, H Eric Xu
The polycomb repressive complexes 2 (PRC2) complex catalyzes tri-methylation of histone H3 lysine 27 (H3K27), a repressive chromatin marker associated with gene silencing. Overexpression and mutations of PRC2 are found in a wide variety of cancers, making the catalytic activity of PRC2 an important target of cancer therapy. This review highlights recent structural breakthroughs of the human PRC2 complex bound to the H3K27 peptide and a small molecule inhibitor, which provide critically needed insight into PRC2-targeted drug discovery...
April 17, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28414198/ly333531-a-pkc%C3%AE-inhibitor-attenuates-glomerular-endothelial-cell-apoptosis-in-the-early-stage-of-mouse-diabetic-nephropathy-via-down-regulating-swiprosin-1
#10
Zhi-Bin Wang, Su Zhang, Ya Li, Rong-Mei Wang, Ling-Chang Tong, Yue Wang, Wei-Ye Liu, Ding-Feng Su, Ye Tu, Li-Chao Zhang, Ling Li
Glomerular endothelial cell (GEC) injury plays an important role in the early stage of diabetic nephropathy (DN). Previous studies show that a PKCβ inhibitor is effective for treating DN. In the current study we further explored the effects and molecular mechanisms of PKCβ inhibitors on GEC apoptosis in DN in streptozotocin-induced diabetic mice in vivo and high glucose- or PMA-treated human renal glomerular endothelial cells (HRGECs) in vitro. In the diabetic mice, hyperglycemia caused aggravated nephropathy and GEC apoptosis accompanied by significantly increased expression of swiprosin-1, a potentally pro-apoptotic protein...
April 17, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28414197/engineering-of-a-self-adjuvanted-itep-delivered-ctl-vaccine
#11
Shuyun Dong, Tiefeng Xu, Peng Wang, Peng Zhao, Mingnan Chen
Cytotoxic T lymphocyte (CTL) epitope peptide-based vaccines are widely used in cancer and infectious disease therapy. We previously generated an immune-tolerant elastin-like polypeptides (iTEPs)-based carrier to deliver a peptide CTL vaccine and enhance the efficiency of the vaccine. To further optimize the vaccine carrier, we intended to potentiate its function by designing an iTEP-based carrier that was able to deliver adjuvant and a vaccine epitope as one molecule. Thus, we fused a 9-mer H100, a peptide derived from the high-mobility group box 1 protein (HMGB1) that could induce activation of dendritic cells (DCs), with an iTEP polymer to generate a new iTEP polymer named H100-iTEP...
April 17, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28392570/human-t-cell-lymphotropic-virus-type-1-and-its-oncogenesis
#12
REVIEW
Lan-Lan Zhang, Jing-Yun Wei, Long Wang, Shi-le Huang, Ji-Long Chen
Human T-cell lymphotropic virus type 1 (HTLV-1) is the etiologic agent of adult T-cell leukemia/lymphoma (ATL), a rapidly progressing clonal malignancy of CD4+ T lymphocytes. Exploring the host-HTLV-1 interactions and the molecular mechanisms underlying HTLV-1-mediated tumorigenesis is critical for developing efficient therapies against the viral infection and associated leukemia/lymphoma. It has been demonstrated to date that several HTLV-1 proteins play key roles in the cellular transformation and immortalization of infected T lymphocytes...
April 10, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28392569/multichannel-polymer-scaffold-seeded-with-activated-schwann-cells-and-bone-mesenchymal-stem-cells-improves-axonal-regeneration-and-functional-recovery-after-rat-spinal-cord-injury
#13
Er-Zhu Yang, Guo-Wang Zhang, Jian-Guang Xu, Shuai Chen, Hua Wang, Liang-Liang Cao, Bo Liang, Xiao-Feng Lian
The adult mammalian CNS has a limited capacity to regenerate after traumatic injury. In this study, a combinatorial strategy to promote axonal regeneration and functional recovery after spinal cord injury (SCI) was evaluated in adult rats. The rats were subjected to a complete transection in the thoracic spinal cord, and multichannel scaffolds seeded with activated Schwann cells (ASCs) and/or rat bone marrow-derived mesenchymal stem cells (MSCs) were acutely grafted into the 3-mm-wide transection gap. At 4 weeks post-transplantation and thereafter, the rats receiving scaffolds seeded with ASCs and MSCs exhibited significant recovery of nerve function as shown by the Basso, Beattie and Bresnahan (BBB) score and electrophysiological test results...
April 10, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28392568/therapeutic-gene-editing-delivery-and-regulatory-perspectives
#14
REVIEW
Gayong Shim, Dongyoon Kim, Gyu Thae Park, Hyerim Jin, Soo-Kyung Suh, Yu-Kyoung Oh
Gene-editing technology is an emerging therapeutic modality for manipulating the eukaryotic genome by using target-sequence-specific engineered nucleases. Because of the exceptional advantages that gene-editing technology offers in facilitating the accurate correction of sequences in a genome, gene editing-based therapy is being aggressively developed as a next-generation therapeutic approach to treat a wide range of diseases. However, strategies for precise engineering and delivery of gene-editing nucleases, including zinc finger nucleases, transcription activator-like effector nuclease, and CRISPR/Cas9 (clustered regularly interspaced short palindromic repeats-associated nuclease Cas9), present major obstacles to the development of gene-editing therapies, as with other gene-targeting therapeutics...
April 10, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28392567/engineering-exosomes-as-refined-biological-nanoplatforms-for-drug-delivery
#15
REVIEW
Xin Luan, Kanokwan Sansanaphongpricha, Ila Myers, Hongwei Chen, Hebao Yuan, Duxin Sun
Exosomes, a subgroup of extracellular vesicles (EVs), have been recognized as important mediators of long distance intercellular communication and are involved in a diverse range of biological processes. Because of their ideal native structure and characteristics, exosomes are promising nanocarriers for clinical use. Exosomes are engineered at the cellular level under natural conditions, but successful exosome modification requires further exploration. The focus of this paper is to summarize passive and active loading approaches, as well as specific exosome modifications and examples of the delivery of therapeutic and imaging molecules...
April 10, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28344324/diallyl-trisulfide-suppresses-tumor-growth-through-the-attenuation-of-nrf2-akt-and-activation-of-p38-jnk-and-potentiates-cisplatin-efficacy-in-gastric-cancer-treatment
#16
Xiao-Yan Jiang, Xiao-Song Zhu, Hong-Ya Xu, Zhong-Xi Zhao, Si-Ying Li, Shan-Zhong Li, Jian-Hua Cai, Ji-Min Cao
Diallyl trisulfide (DATS), a garlic organosulfide, has shown excellent chemopreventive potential. Cisplatin (DDP) is widely used to treat solid malignant tumors, but causing serious side effects. In the current study, we attempted to elucidate the chemopreventive mechanisms of DATS in human gastric cancer BGC-823 cells in vitro, and to investigate whether DATS could enhance the anti-tumor efficacy of DDP and improve quality of life in BGC-823 xenograft mice in vivo. Treatment with DATS (25-400 μmol/L) dose-dependently inhibited the viability of BGC-823 cells in vitro with an IC50 of 115...
March 27, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28344323/new-knowledge-of-the-mechanisms-of-sorafenib-resistance-in-liver-cancer
#17
REVIEW
Yan-Jing Zhu, Bo Zheng, Hong-Yang Wang, Lei Chen
Sorafenib is an oral multikinase inhibitor that suppresses tumor cell proliferation and angiogenesis and promotes tumor cell apoptosis. It was approved by the FDA for the treatment of advanced renal cell carcinoma in 2006, and as a unique target drug for advanced hepatocellular carcinoma (HCC) in 2007. Sorafenib can significantly extend the median survival time of patients but only by 3-5 months. Moreover, it is associated with serious adverse side effects, and drug resistance often develops. Therefore, it is of great importance to explore the mechanisms underlying sorafenib resistance and to develop individualized therapeutic strategies for coping with these problems...
March 27, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28344322/astragaloside-iv-attenuates-free-fatty-acid-induced-er-stress-and-lipid-accumulation-in-hepatocytes-via-ampk-activation
#18
Bing Zhou, Dan-Li Zhou, Xiao-Hong Wei, Rong-Yu Zhong, Jie Xu, Liao Sun
Although the pathogenesis of non-alcoholic fatty liver disease (NAFLD) is not completely understood, the increased influx of free fatty acids (FFAs) into the liver and the FFA-induced hepatic endoplasmic reticulum (ER) stress are two crucial pathogenic processes in the initiation and development of NAFLD. In this study we investigated the effects of astragaloside IV (AS-IV), a bioactive compound purified from Astragali Radix, on FFA-induced lipid accumulation in hepatocytes and elucidated the underlying mechanisms...
March 27, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28317873/a-new-method-to-evaluate-the-dose-effect-relationship-of-a-tcm-formula-gegen-qinlian-decoction-focus-mode-of-integrated-biomarkers
#19
Zhi-Qiang Huang, Xue-Mei Fan, Yi-Ming Wang, Qiong-Lin Liang, Xiao-Lin Tong, Yu Bai, Ying-Meng Li, Guo-An Luo, Chao Chen
It is difficult to accurately evaluate the efficacy of traditional Chinese medicine (TCM), which leads to the uncertainty and complexity of dose-effect analysis. In this study we established the "Focus" mode of biomarkers to characterize the dose-effect relationship of Gegen Qinlian Decoction (GQD), a TCM formula for treating type 2 diabetes mellitus (2-DM). A rat model of 2-DM was established through high fat diet feeding combined with low-dose STZ injection. Rats with 2-DM were administered high, middle or low doses (6...
March 20, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28317872/preclinical-evaluation-of-the-efficacy-pharmacokinetics-and-immunogenicity-of-js-001-a-programmed-cell-death-protein-1-pd-1-monoclonal-antibody
#20
Jie Fu, Fang Wang, Li-Hou Dong, Jing Zhang, Cheng-Lian Deng, Xue-Li Wang, Xin-Yao Xie, Jing Zhang, Ruo-Xian Deng, Li-Bo Zhang, Hai Wu, Hui Feng, Bo Chen, Hai-Feng Song
JS-001 is the first monoclonal antibody (mAb) against programmed cell death protein-1 (PD-1) approved by the China Food and Drug Administration (CFDA) into the clinical trails. To date, however, no pre-clinical pharmacological and pharmacokinetic (PK) data are available. In this study, we investigated the efficacy of JS-001 and conducted a preclinical PK study, including the monitoring of anti-drug antibodies (ADAs). We found that JS-001 specifically bound to PD-1 antigen with an EC50 of 21 nmol/L, and competently blocked the binding of PD-1 antigen to PD-L1 and PD-L2 with IC50 of 3...
March 20, 2017: Acta Pharmacologica Sinica
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