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Jinlei Bian
China Pharmaceutical University
Organic chemistryChemistryCancer researchBiochemistryStereochemistry
44Publications
12H-index
313Citations
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Publications 42
Newest
#1Jie Han (CAS: Chinese Academy of Sciences)H-Index: 4
#2Yucheng Tian (CPU: China Pharmaceutical University)H-Index: 1
Last. LUOCheng (CAS: Chinese Academy of Sciences)
view all 15 authors...
Abstract USP8, one member of deubiquitinating enzymes (DUBs) families, maintains the ubiquitination level of EGFR and regulates the downstream signaling pathways. The deregulation of USP8 has been implicated in many human diseases, especially in cancer. Therefore, USP8 has been identified as a promising target for drug design. Herein, via high throughput screening based on Ubiquitin-rhodamine-110 (Ubiquitin-Rho-110) fluorometric activity assay, we discovered a novel inhibitor DC-U43. By structur...
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#1Pengfei Xu (CPU: China Pharmaceutical University)H-Index: 3
Last. Raoling GeH-Index: 5
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A scalable and practical route to the P2Y2 receptor agonist diquafosol tetrasodium has been described. Diquafosol tetrasodium was obtained via a four-step process starting from commercially availab...
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#1Hongyu Luan (CPU: China Pharmaceutical University)H-Index: 2
#2Pengfei Xu (CPU: China Pharmaceutical University)H-Index: 3
Last. Jinlei Bian (CPU: China Pharmaceutical University)H-Index: 12
view all 5 authors...
Abstract Prostate cancer is the most common carcinoma of the male urinary system in developed countries. Androgen deprivation therapy has been commonly used in the treatment of Prostate cancer for decades, but most patients will inevitably develop into more aggressive castration-resistant prostate cancer. Therefore, novel strategies are urgent to address this resistance mechanism. In this review, we discussed some new strategies for targeting androgen receptors through degradation pathways as po...
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#1Pengfei Xu (CPU: China Pharmaceutical University)H-Index: 3
#2Pei Shen (CPU: China Pharmaceutical University)H-Index: 1
Last. Jubo Wang (CPU: China Pharmaceutical University)H-Index: 6
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Abstract The Janus kinases or JAKs are a family of intracellular tyrosine kinases that play an essential role in the signaling of numerous cytokines that have been implicated in the pathogenesis of autoimmune diseases and myeloproliferative disorders. JAKs are activated upon ligand induced receptor homo- or heterodimerization, which results in the immediate phosphorylation of tyrosine residues and the phosphotyrosines then serve as docking sites for cytoplasmic signal transducer and activator of...
1 CitationsSource
#1Xi Xu (CPU: China Pharmaceutical University)H-Index: 5
#2Qianming Du (Nanjing Medical University)H-Index: 1
Last. Siqi Xue (Nanjing Medical University)
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Abstract Prostate cancer (PC) is the most diagnosed type of malignancy in men and the major frequently cause of cancer-related death worldwide. The androgen receptor (AR) has become a promising drug target for the treatment of PC. Here, we reported the design, optimization and evaluation of pyridine tetrahydroisoquinoline thiohydantoin derivatives with improved activity and safety as potent AR antagonists. The most promising compound 42f exhibited potent inhibitory activity on AR and strongly bl...
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#1Yucheng Tian (CPU: China Pharmaceutical University)H-Index: 1
#2Jubo Wang (CPU: China Pharmaceutical University)H-Index: 6
Last. Jinlei Bian (CPU: China Pharmaceutical University)H-Index: 12
view all 9 authors...
A microwave-assisted, efficient and rapid Sonogashira reaction was developed for the synthesis of polysubstituted aromatic alkynes. The reaction was environmentally friendly and easy to handle by replacing traditional amine solvents with water. The optimized reaction conditions could obtain the products with high yields, while reducing the dependence on anaerobic reaction conditions with no inert gas protection. The reaction can also achieve milligram level, overcoming the problem of TMSA volati...
1 CitationsSource
#1Xi Feng (CPU: China Pharmaceutical University)H-Index: 2
#2Dongyu Liu (CPU: China Pharmaceutical University)H-Index: 1
Last. Jinlei Bian (CPU: China Pharmaceutical University)H-Index: 12
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The cyclic GMP-AMP synthase (cGAS)-stimulator of interferon genes (STING)-pathway triggers innate immune responses by recognizing cytosolic DNA. Recent studies revealed that STING adaptor associates with various diseases, and several modulators targeting STING have been identified including three agonists that have entered clinical trials for treating cancer over the past 2 years. In particular, the efficacy of STING agonists and/or antagonists suggests adaptor STING as a potential therapeutic t...
1 CitationsSource
#1Xi Xu (CAS: Chinese Academy of Sciences)
#2Zijian Kuang (CPU: China Pharmaceutical University)H-Index: 1
Last. Jinlei Bian (CPU: China Pharmaceutical University)H-Index: 12
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Glutaminase (GLS1) is a cancer energy metabolism protein which plays a predominant role in cell growth and proliferation. Because of its major involvement in malignant tumor, small-molecule GLS1 inhibitors are urgently needed to assess its therapeutic potential and for probing their underlying biology function. Recent studies showed that targeting the allosteric binding site represented a promising strategy for identifying potent and selective GLS1 inhibitors. Herein, we present the synthesis of...
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#1Ying Meng (CPU: China Pharmaceutical University)H-Index: 2
#2Xi Xu (CPU: China Pharmaceutical University)H-Index: 5
Last. Jinlei Bian (CPU: China Pharmaceutical University)H-Index: 12
view all 7 authors...
A major difference between glucose metabolism in cancer cells and normal cells is that glucose in cancer cells is preferably converted to lactate in aerobic conditions rather than oxidized in mitoc...
2 CitationsSource
#1Yi Zhong (CPU: China Pharmaceutical University)H-Index: 1
#2Ying Meng (CPU: China Pharmaceutical University)H-Index: 2
Last. Jinlei Bian (CPU: China Pharmaceutical University)H-Index: 12
view all 7 authors...
Abstract Two new series of compounds were designed and synthesized as potent PARP-1 inhibitors. These compounds were evaluated for PARP-1 enzyme and cellular inhibitory activities. All efforts lead to the identification of 9k (named as LG-12) with efficient potency both for PARP-1 and BRCA1 deficient MDA-MB-436 cells. Additionally, the novel PARP-1 inhibitor LG-12 is an efficient chemosensitizer, which could potentiate the anti-cancer effect of TMZ. Our data presented herein provide a comprehens...
1 CitationsSource
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