83405-98-5Relevant articles and documents
One-step modification to identify dual-inhibitors targeting both pancreatic triglyceride lipase and Niemann-Pick C1-like 1
Zhang, Renshuai,Song, Zhengming,Wang, Xueting,Xue, Jiao,Xing, Dongming
supporting information, (2021/03/16)
Pancreatic triglyceride lipase (PTL) and Niemann-Pick C1-like 1 (NPC1L1) have been identified as attractive therapeutic targets for obesity and hypercholesteremia, respectively. Obesity and hypercholesteremia usually co-exist, however no dual-inhibitors against PTL and NPC1L1 were reported for the treatment of obesity patients with hypercholesteremia so far. In this work, molecular hybridization-based one-step modification screening identified a potent dual-inhibitor against PTL and NPC1L1. Compound P1-11 has IC50 values of 2.1 μM against PTL through covalent binding, as well as significantly reduces cholesterol absorption in a non-competitive inhibitory manner. Molecule docking and molecular dynamics studies revealed the reason of its activity to both PTL and NPC1L1. Moreover, the gene and protein expression levels of PTL and NPC1L1 were also determined respectively after the treatment of P1-11. Development of dual-inhibitors against PTL and NPC1L1 could provide novel treatment options for obesity patients with hypercholesteremia. The results of current research would great support the development of dual-inhibitors against PTL and NPC1L1.
Tumor diagnosis and treatment fluorescent probe for targeting tumor Wolburg effect
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, (2020/11/02)
The invention discloses a tumor diagnosis and treatment fluorescent probe for targeting tumor Warburg effect, and the structure of the fluorescent probe is shown as a formula (I). The fluorescent probe can be directly used in a cell line to analyze and detect the expression degree of tumor cell GLUT1 protein, so as to complete the screening of tumor cells. Meanwhile, tumor cell proliferation is inhibited by directly blocking the GLUT1 channel to inhibit intake of sugar nutritional ingredients by tumors. And an effective means and a useful tool are provided for early screening and diagnosis oftumors, development of new anti-tumor drugs and the like.
Composition, thermal conductive sheet, the thermally conductive layer with a device (by machine translation)
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Paragraph 0175, (2020/04/18)
The film thickness of the thermal conductivity sheet having thermal conductivity [to] direction forming a composition. Also, in the film thickness direction of the heat conductive sheet having excellent thermal conductivity, the thermal conductivity sheet
