Article
Pharmacology & Pharmacy
Shi-Jye Chu, Shih-En Tang, Hsin-Ping Pao, Shu-Yu Wu, Wen- Liao
Summary: This study demonstrates that the PAR-1 antagonist SCH530348 exerts protective effects by blocking PAR-1 expression and modulating the downstream PI3K, NF-kappa B, and MAPK pathways, reducing IR-induced acute lung injury. These findings suggest that PAR-1 antagonist could be a potential therapeutic candidate for lung protection following IR injury.
FRONTIERS IN PHARMACOLOGY
(2021)
Review
Biochemistry & Molecular Biology
Elena Pompili, Valerio De Franchis, Claudia Giampietri, Stefano Leone, Elena De Santis, Francesco Fornai, Lorenzo Fumagalli, Cinzia Fabrizi
Summary: Schwann cells play a crucial role in peripheral nerve regeneration by promptly activating, dedifferentiating, and assisting axon regrowth after nerve injury. PAR1, a thrombin receptor present on Schwann cell plasma membrane, is emerging as a possible regulator of Schwann cells' pro-regenerative capacity. This review summarizes recent literature on the contribution of PAR1 and PAR1-activating proteases in regulating peripheral nerve regeneration.
Article
Hematology
Sujuan Li, Weili Wang, Lisha Lin, Lian Yang, Ying Cai, Xingzhi Yang, Taocui Zhang, Chuang Xiao, Hui Yan, Na Gao, Jinhua Zhao
Summary: An oligosaccharide HS-11, derived from sea cucumber Holothuria fuscopunctata, inhibits thrombin-mediated platelet activation and aggregation by directly binding to thrombin exosite II, demonstrating its antiplatelet and antithrombotic activity.
ARTERIOSCLEROSIS THROMBOSIS AND VASCULAR BIOLOGY
(2023)
Article
Multidisciplinary Sciences
Sukanya Tripathy, Bader O. Almutairi, Sanjay Singh, Atul Rawat, Durgesh Dubey, Monisha Banerjee, Dinesh R. Modi, Anand Prakash
Summary: Thrombin-activated receptor-1 (PAR1) plays a crucial role in tumor angiogenesis, cell proliferation, and invasion. The present study investigated the expression of PAR1 in human glioma cell lines D54 and U87, as well as its downstream signaling pathway. The results showed that PAR1 was highly expressed in D54 cells compared to U87 cells. Activation of PAR1 led to increased ERK1/2 activity and enhanced migration and invasion. The antagonist SCH79797 significantly inhibited the migration and invasion of the glioma cell lines. Moreover, PAR1 activation affected intracellular Ca+2 concentration ([Ca+2]i). Thrombin and TFLLR induced an increase in [Ca+2]i, which was suppressed by the PAR1 inhibitor SCH79797. The study suggests that PAR1 signaling contributes to glioma progression and may serve as a potential therapeutic target for glioma prevention.
JOURNAL OF KING SAUD UNIVERSITY SCIENCE
(2022)
Article
Pharmacology & Pharmacy
Mohd Aslam Saifi, Shivaraju Annaldas, Chandraiah Godugu
Summary: The study revealed the therapeutic effect of a direct thrombin inhibitor on tubulointerstitial fibrosis in chronic kidney disease by improving kidney injury and fibrosis through inhibition of thrombin-activated PAR-1 expression.
EUROPEAN JOURNAL OF PHARMACOLOGY
(2021)
Article
Cell Biology
Julian Friebel, Eileen Moritz, Marco Witkowski, Kai Jakobs, Elisabeth Straessler, Andrea Doerner, Daniel Steffens, Marianna Puccini, Stella Lammel, Rainer Glauben, Franziska Nowak, Nicolle Kraenkel, Arash Haghikia, Verena Moos, Heinz-Peter Schutheiss, Stephan B. Felix, Ulf Landmesser, Bernhard H. Rauch, Ursula Rauch
Summary: The study found that vorapaxar may reduce inflammation in atherosclerosis by inhibiting the PAR1 signaling pathway, potentially helping to lower the risk of thrombo-inflammatory events in patients.
Article
Multidisciplinary Sciences
Nasim Shahidi Hamedani, Felix Lucian Happich, Eva-Maria Klein, Heiko Ruehl, Gunter Mayer, Johannes Oldenburg, Jens Mueller, Bernd Poetzsch
Summary: In this study, a one-step activation and purification method of APC using an APC-specific aptamer was developed. By optimizing the Ca2+-dependent binding and elution conditions, high purity and yield of purified APC can be achieved.
SCIENTIFIC REPORTS
(2022)
Article
Biochemistry & Molecular Biology
Shani Berkowitz, Shany Guly Gofrit, Shay Anat Aharoni, Valery Golderman, Lamis Qassim, Zehavit Goldberg, Amir Dori, Nicola Maggio, Joab Chapman, Efrat Shavit-Stein
Summary: The study found that there is an interaction between neuroinflammation and coagulation, and enoxaparin can protect against inflammation induced by LPS, reducing neuronal damage. The findings may provide a new pharmacological mechanism for intervening in neuroinflammation.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Cell Biology
Jing Yang, Claudio Mapelli, Zhaoqing Wang, Chi Shing Sum, Ji Hua, R. Michael Lawrence, Yan Ni, Dietmar A. Seiffert
Summary: Protease-activated receptor 4 (PAR4) is a promising drug target for improving the efficacy and safety of antiplatelet agents. However, the current PAR4 agonist peptides have limited utility in pharmacodynamic assays due to their high concentrations required to elicit an agonist response. This study developed a more potent PAR4 agonist peptide and a platelet aggregation assay for evaluating PAR4 antagonists, providing a valuable tool for the clinical development of PAR4 antagonists.
Article
Cardiac & Cardiovascular Systems
Laura C. Burzynski, Alejandra Morales-Maldonado, Amanda Rodgers, Lauren A. Kitt, Melanie Humphry, Nichola Figg, Martin R. Bennett, Murray C. H. Clarke
Summary: Atherosclerosis is driven by multiple processes involving the immune and coagulation systems. Thrombin can activate interleukin-1α, which contributes to atherogenesis. Inhibition of thrombin can reduce atherosclerotic plaque formation, but also results in a more unstable plaque phenotype.
CARDIOVASCULAR RESEARCH
(2023)
Review
Biochemistry & Molecular Biology
Aditi Kothari, Matthew J. Flick
Summary: Pancreatic ductal adenocarcinoma (PDAC) is a highly fatal disease with a low 5-year survival rate due to its aggressive nature and late-stage diagnosis. The coagulation system plays a crucial role in PDAC progression and dissemination, promoting tumor growth and spread.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Gastroenterology & Hepatology
Ying Xie, Lindsey Fontenot, Andrea Chupina Estrada, Becca Nelson, Jiani Wang, David Q. Shih, Wendy Ho, S. Anjani Mattai, Florian Rieder, Dane D. Jensen, Nigel W. Bunnett, Hon Wai Koon
Summary: The study demonstrates that Elafin can suppress collagen synthesis in intestinal fibroblasts by inhibiting protease-activated receptor 2, which is dependent on cathelin S, leading to a reduction in intestinal fibrosis.
CELLULAR AND MOLECULAR GASTROENTEROLOGY AND HEPATOLOGY
(2022)
Article
Cardiac & Cardiovascular Systems
Christine Joseph, Eva Maria Berghausen, Arnica Behringer, Bernhard Rauch, Henrik Ten Freyhaus, Leoni Luisa Gnatzy-Feik, Maximilian Krause, Dickson W. L. Wong, Peter Boor, Stephan Baldus, Marius Vantler, Stephan Rosenkranz
Summary: This study characterizes the effects of thrombin and Factor Xa on PASMCs and their involvement in pulmonary vascular remodeling through PAR-1 and PAR-2. Inhibition of PAR-1 and PAR-2 significantly reduces vascular muscularization and improves right ventricular function in PAH. These findings suggest that PARs, rather than their activators, could be potential targets for PAH treatment.
CARDIOVASCULAR RESEARCH
(2022)
Article
Dentistry, Oral Surgery & Medicine
T. Hattori, S. Kawano, S. Tanaka, R. Matsubara, T. Sakamoto, Y. Hashiguchi, N. Kaneko, Y. Mikami, M. Morioka, Y. Maruse, R. Kitamura, E. Hamada, M. Hiwatashi, K. Oobu, T. Kiyoshima, S. Nakamura
Summary: This study found that increased PAR1 expression in both cancer and stromal cells at the invasive front of oral squamous cell carcinoma is associated with higher histological grade tumors, higher incidence of nodal metastasis, and lower survival rate. Delta Np63 is involved in regulating PAR1 expression.
INTERNATIONAL JOURNAL OF ORAL AND MAXILLOFACIAL SURGERY
(2021)
Article
Biochemistry & Molecular Biology
Xiaobin Fang, Mengmeng Li, Weiyi Zhang, Jingyi Li, Tao Zhu
Summary: Thrombin-induced mast cell activation results in the production of both pro- and anti-inflammatory mediators, involving the expression of PAR1 and PAR4 as well as activation of MAPK signaling pathways. Dual activation of mast cells occurs after thrombin stimulation.
MOLECULAR IMMUNOLOGY
(2022)
Article
Dermatology
Yi-Kai Hong, Yao-Chou Lee, Tsung-Lin Cheng, Chao-Han Lai, Chao-Kai Hsu, Cheng-Hsiang Kuo, Yun-Yan Hsu, Jui-Ting Li, Bi-Ing Chang, Chih-Yuan Ma, Shu-Wha Lin, Kuan-Chieh Wang, Guey-Yueh Shi, Hua-Lin Wu
JOURNAL OF INVESTIGATIVE DERMATOLOGY
(2019)
Article
Cardiac & Cardiovascular Systems
Chao-Han Lai, Ching-Wen Chang, Fang-Tzu Lee, Cheng-Hsiang Kuo, Jong-Hau Hsu, Chung-Pin Liu, Hua-Lin Wu, Jwu-Lai Yeh
Article
Dentistry, Oral Surgery & Medicine
Lan-Yun Chang, Chao-Han Lai, Cheng-Hsiang Kuo, Bi-Ing Chang, Hua-Lin Wu, Tsung-Lin Cheng
Summary: Our study found that rTMD1 attenuates Pg-LPS-enhanced M1 macrophage polarization, osteoclastogenesis and periodontal bone resorption, showing therapeutic promise for periodontitis.
JOURNAL OF PERIODONTOLOGY
(2021)
Article
Hematology
Cheng-Hsiang Kuo, Yi-Hsun Huang, Po-Ku Chen, Gang-Hui Lee, Ming-Jer Tang, Edward M. Conway, Guey-Yueh Shi, Hua-Lin Wu
Summary: The study reveals that the VEGF-ROCK2-ezrin-TM-F-actin axis plays a critical role in promoting the formation of 3DPs in endothelial cells during sprouting angiogenesis. TM expression enhances angiogenic activity in endothelial cells by interacting with ezrin and maintaining the integrity of its lectin-like domain. Mice lacking the lectin-like domain of TM show reduced neovascularization in wound healing and retinal neovascularization, indicating the importance of TM in angiogenesis.
ARTERIOSCLEROSIS THROMBOSIS AND VASCULAR BIOLOGY
(2021)
Article
Biochemistry & Molecular Biology
Yi-Hsun Huang, Cheng-Hsiang Kuo, I-Chen Peng, Yi-Sheng Chang, Sung-Huei Tseng, Edward M. Conway, Hua-Lin Wu
Summary: The study reveals that rTMD1 not only inhibits VEGF-induced angiogenesis in vitro, but also significantly reduces retinal neovascularization in an OIR animal model while sparing normal physiological vessel growth. Furthermore, loss of TMD1 promotes PA in OIR.
CELLULAR AND MOLECULAR LIFE SCIENCES
(2021)
Article
Pharmacology & Pharmacy
Cheng-Hsiang Kuo, Ban-Hua Zhang, Shang-En Huang, Jong-Hau Hsu, Yan-Hsiung Wang, Thi Tuyet Ngan Nguyen, Chao-Han Lai, Jwu-Lai Yeh
Summary: This study demonstrates the therapeutic potential of KMUP-1 in the treatment of periodontitis. KMUP-1 attenuates inflammation and osteoclast differentiation, thus reducing the symptoms of periodontitis.
FRONTIERS IN PHARMACOLOGY
(2022)
Article
Cell Biology
Yu-Chia Hsu, Hao-Chun Chuang, Kun-Ling Tsai, Ting-Yuan Tu, Yan-Jye Shyong, Cheng-Hsiang Kuo, Yuan-Fu Liu, Shu-Shien Shih, Cheng-Li Lin
Summary: The study found that under oxidative stress, levels of p-p38 significantly increased in both hypertrophic and healthy LF cells, while iNOS was elevated only in hypertrophic LF cells. This suggests that oxidative stress negatively impacts both hypertrophic and healthy LF cells, with hypertrophic LF cells showing more active inflammation. After H2O2 treatment, levels of p-p38, p-p65, iNOS, TGF-beta, vimentin, and collagen I all increased significantly, and NAC treatment reversed the effects of oxidative stress.
OXIDATIVE MEDICINE AND CELLULAR LONGEVITY
(2022)
Article
Integrative & Complementary Medicine
Pei-Tzu Yen, Shang-En Huang, Jong-Hau Hsu, Cheng-Hsiang Kuo, Yu-Ying Chao, Lung-Shuo Wang, Jwu-Lai Yeh
Summary: The study found that puerarin, derived from the root of Pueraria lobate, has cardioprotective effects and can reduce the risk of cardiovascular disease in postmenopausal women. Puerarin alleviates cytotoxicity and oxidative stress, restores normal gene expression, and protects the heart from damage.
AMERICAN JOURNAL OF CHINESE MEDICINE
(2023)
Review
Biochemical Research Methods
Thi Kim Ngan Ngo, Cheng-Hsiang Kuo, Ting-Yuan Tu
Summary: Despite improvements in cancer immunotherapy, more study is needed. Microfluidic-based cancer immunotherapy-on-a-chip systems help researchers replicate the tumor microenvironment and immune system. This review summarizes recent advancements in microfluidic devices for cancer treatment and presents future perspectives on immunotherapy research.
Article
Plant Sciences
Yi-Ju Chen, Boon Huat Cheah, Chih-Yu Lin, Yu-Ting Ku, Cheng-Hsiang Kuo, Yuan-Yun Zhang, Bing-Rong Chen, Olga Nean, Cheng-Han Hsieh, Pei-Min Yeh, Freddy Kuok San Yeo, Ya-Ping Lin, Wen-Po Chuang, Cheng-Ruei Lee, Hieng-Ming Ting
Summary: We identified Mungbean genotypes resistant (R1) and susceptible (S1) to the common cutworm through screening. RNA-Seq data suggested the involvement of CaMK, MAPK and JA signaling in the defense response of R1 plants. R1 plants exhibited higher expression levels of defense-related genes and accumulated higher amounts of JA, tryptophan, and tyrosine, leading to the production of glucosylated kaempferols and emission of (E)-beta-ocimene. However, R1 plants showed lower drought tolerance and endogenous proline levels.
ENVIRONMENTAL AND EXPERIMENTAL BOTANY
(2023)
Article
Medicine, Research & Experimental
Jwu-Lai Yeh, Cheng-Hsiang Kuo, Po-Wen Shih, Jong-Hau Hsu, Peng I-Chen, Yi-Hsun Huang
Summary: This study investigated the effects of KMUP-1, a xanthine-based derivative, on retinopathy in vitro and in vivo. KMUP-1 showed anti-angiogenic, anti-inflammatory, and anti-apoptotic effects on hypoxic endothelium, reducing vascular endothelial growth factor (VEGF) expression and inhibiting endothelial migration and tube formation. KMUP-1 also increased the BCL-2/BAX ratio and decreased the expression of pro-inflammatory cytokines in the oxygen-induced retinopathy mouse retina samples.
BIOMEDICINE & PHARMACOTHERAPY
(2023)
Article
Pharmacology & Pharmacy
Chian-Wei Chen, Chun-Ping Chang, Yi-Shuan Wen, Cheng-Hsiang Kuo, Shang-Wen Lin, Jui-Chen Tsai, Yan-Jye Shyong
JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
(2023)
Article
Cell Biology
Cheng-Hsiang Kuo, Ya-Fang Wu, Bi-Ing Chang, Chao-Kai Hsu, Chao-Han Lai, Hua-Lin Wu
Summary: CD248 expression in melanoma cells promotes malignant transformation by increasing the activity of cell adhesion, migration, and vascular mimicry, whereas rCD248 protein functions as a molecular decoy interfering with tumor-promoting effects of CD248 in melanoma cells.
JOURNAL OF BIOMEDICAL SCIENCE
(2022)
Article
Multidisciplinary Sciences
Chao-Han Lai, Ching-Wen Chang, Fang-Tzu Lee, Cheng-Hsiang Kuo, Jong-Hau Hsu, Chung-Pin Liu, Hua-Lin Wu, Jwu-Lai Yeh
Article
Cell Biology
Gang-Hui Lee, Chia-Lin Chang, Wen-Tai Chiu, Tsun-Hsien Hsiao, Po-Yuan Chen, Kuan-Chieh Wang, Cheng-Hsiang Kuo, Bing-Hung Chen, Guey-Yueh Shi, Hua-Lin Wu, Tzu-Fun Fu
JOURNAL OF BIOMEDICAL SCIENCE
(2019)