期刊文献+
共找到17篇文章
< 1 >
每页显示 20 50 100
Protein tyrosine phosphatase 1B regulates migration of ARPE-19 cells through EGFR/ERK signaling pathway 被引量:3
1
作者 Zhao-Dong Du Li-Ting Hu +4 位作者 Gui-Qiu Zhao Qian Wang Qiang Xu Nan Jiang Jing Lin 《International Journal of Ophthalmology(English edition)》 SCIE CAS 2015年第5期891-897,共7页
AIMTo evaluate whether protein tyrosine phosphatase 1B (PTP1B) contributed to initiate human retinal pigment epithelium cells (A)-19 migration and investigate the signaling pathways involved in this process.METHODSARP... AIMTo evaluate whether protein tyrosine phosphatase 1B (PTP1B) contributed to initiate human retinal pigment epithelium cells (A)-19 migration and investigate the signaling pathways involved in this process.METHODSARPE-19 cells were cultured and treated with the siRNA-PTP1B. Expression of PTP1B was confirmed by quantitative reverse transcriptase-polymerase chain reaction (qRT-PCR). AG1478 [a selective inhibitor of epidermal growth factor receptor (EGFR)] and PD98059 (a specific inhibitor of the activation of mitogen-activated protein kinase) were used to help to determine the PTP1B signaling mechanism. Western blot analysis verified expression of EGFR and extracellular signal-regulated kinase (ERK) in ARPE-19 cells. The effect of siRNA-PTP1B on cell differentiation was confirmed by immunostaining for &#x003b1;-smooth muscle actin (&#x003b1;-SMA) and qRT-PCR. Cell migration ability was analyzed by transwell chamber assay.RESULTSThe mRNA levels of PTP1B were reduced by siRNA-PTP1B as determined by qRT-PCR assay. SiRNA-PTP1B activated EGFR and ERK phosphorylation. &#x003b1;-SMA staining and qRT-PCR assay demonstrated that siRNA-PTP1B induced retinal pigment epithelium (RPE) cells to differentiate toward better contractility and motility. Transwell chamber assay proved that PTP1B inhibition improved migration activity of RPE cells. Treatment with AG1478 and PD98059 abolished siRNA-PTP1B-induced activation of EGFR and ERK, &#x003b1;-SMA expression and cell migration.CONCLUSIONPTP1B inhibition promoted myofibroblast differentiation and migration of ARPE-19 cells, and EGFR/ERK signaling pathway played important role in migration process. 展开更多
关键词 protein tyrosine phosphatase 1B retinal pigment epithelium cell migration epidermal growth factor receptor extracellular signal-regulated kinase
下载PDF
Structural Insight into the Design on Oleanolic Acid Derivatives as Potent Protein Tyrosine Phosphatase 1B Inhibitors 被引量:2
2
作者 施建成 涂文通 +1 位作者 罗敏 黄初升 《Chinese Journal of Structural Chemistry》 SCIE CAS CSCD 2017年第7期1063-1076,共14页
Oleanolic acid derivatives act as newer protein tyrosine phosphatase 1B (PTP-1B) inhibitors for type 2 diabetes mellitus (T2DM). In order to understand the structural requirement of PTP-1B inhibitors, 52 oleanolic... Oleanolic acid derivatives act as newer protein tyrosine phosphatase 1B (PTP-1B) inhibitors for type 2 diabetes mellitus (T2DM). In order to understand the structural requirement of PTP-1B inhibitors, 52 oleanolic acid derivatives were divided into a training set (34 compounds) and a test set (18 compounds). The highly reliable and predictive 3D-QSAR models were constructed by CoMFA, CoMSIA and topomer CoMFA methods, respectively. The results showed that the cross validated coefficient (q2) and non-cross-validated coefficient (R2) were 0.554 and 0.999 in the CoMFA model, 0.675 and 0.971 in the CoMSIA model, and 0.628 and 0.939 in the topomer CoMFA model, which suggests that three models are robust and have good exterior predictive capabilities. Furthermore, ten novel inhibitors with much higher inhibitory potency were designed. Our design strategy was that (i) the electronegative substituents (Cl, -CH2OH, OH and -CH2Cl) were introduced into the double bond of ring C, (ii) the hydrogen bond acceptor groups (C≡N and N atom), electronegative groups (C≡N, N atom, -COOH and -COOCH3) and bulky substituents (C6H5N) were connected to the C-3 position, which would result in generating potent and selective PTP-1B inhibitors. We expect that the results in this paper have the potential to facilitate the process of design and to develop new potent PTP-1B inhibitors. 展开更多
关键词 Type 2 diabetes mellitus (T2DM) protein tyrosine phosphatase 1B (PTP-1B) inhibitor 3D-QSAR Molecular design
下载PDF
Synthesis and protein tyrosine phosphatase 1B inhibition activities of two new synthetic bromophenols and their methoxy derivatives 被引量:1
3
作者 崔永超 史大永 胡志强 《Chinese Journal of Oceanology and Limnology》 SCIE CAS CSCD 2011年第6期1237-1242,共6页
3-bromo-4,5-bis(2,3-dibromo-4,5-dihydroxybenzyl)-l,2-benzenediol (1) is a natural bromophenol isolated from the red algae Rhodomela confervoides that exhibits significant inhibition against protein tyrosine phosph... 3-bromo-4,5-bis(2,3-dibromo-4,5-dihydroxybenzyl)-l,2-benzenediol (1) is a natural bromophenol isolated from the red algae Rhodomela confervoides that exhibits significant inhibition against protein tyrosine phosphatase 1B (PTP1B). Based on its activity, we synthesized two new synthetic bromophenols and their methoxy derivatives from vanillin using the structure of natural bromophenol 1 as a scaffold. The structures of these bromophenols were elucidated from H NMR, 13C NMR, and high resolution electron ionization mass spectrometry as 2,3-dibromo-1-(2'-bromo-6'-(3",4"-dimethoxybenzyl)- 3 ',4 '-dimethoxybenzyl)-4,5 -dimethoxybenzene (2), 2,3-dibromo- 1 -(2 '-bromo-6'-(2 "-bromo-4",5 "-dimethoxy- benzyl)-3',4'-dimethoxybenzyl)-4,5-dimethoxybenzene (3), 3,4-dibromo-5-(2'-bromo-6'-(2"-bromo-4",5"- dihydroxybenzyl)-3',4'-dihydroxybenzyl)pyrocatechol (4) and 3,4-dibromo-5-(2'-bromo-6'-(3",4"- dihydroxybenzyl)-3',4'-dihydroxybenzyl)pyrocatechol (5). PTP1B inhibition activities of these compounds were evaluated using a colorimetric assay, and compounds 3 and 4 demonstrated interesting activity against PTP1B. 展开更多
关键词 protein tyrosine phosphatase 1B inhibition bromophenol derivatives SYNTHESIS
下载PDF
POM analysis and computational interactions of 8-hydroxydiospyrin inside active site of protein tyrosine phosphatase 1B
4
作者 SAUD BAWAZER ASGHAR KHAN +9 位作者 ABDUR RAUF TAIBI B EN HADDA YAHYA SAL-AWTHAN OMAR BAHATTAB UMER RASHID INAMULLAH KHAN MUHAMMAD A SIF NAWAZ MD SAHAB UDDIN OLATUNDE AHMED MOHAMMAD A LI SHARIATI 《BIOCELL》 SCIE 2021年第3期751-759,共9页
Proteintyrosine phosphatase 1B(PTP1B)inhibitionis consideredas a potentialtherapeuticfor the treatmentof cancer,type2 diabetes,andobesity.Inour presentwork,weinvestigatedtheanti-diabeticpotentialof8-hydroxydiospyrin(8... Proteintyrosine phosphatase 1B(PTP1B)inhibitionis consideredas a potentialtherapeuticfor the treatmentof cancer,type2 diabetes,andobesity.Inour presentwork,weinvestigatedtheanti-diabeticpotentialof8-hydroxydiospyrin(8-HDN)from D.lotus against the PTP1B enzyme.It showed significant inhibitory activity of PTP1B with an IC 50 value of 18.37±0.02μM.A detailed molecular docking study was carried out to analyze the binding orientation,binding energy,and mechanism of inhibition.A comparative investigation of 8-HDN in the catalytic,as well as the allosteric site of PTP1B,was performed.Binding energy data showed that compound 8-HDN is more selective for the allosteric site and hence avoids the problems associated with catalytic site inhibition.The inhibition mechanism of 8-HDN can be further investigated as an active lead compound against PTP1B by using in vitro and in vivo models. 展开更多
关键词 Diospyros lotus ROOTS 8-Hydroxydiospyrin Molecular docking protein tyrosine phosphatase 1B
下载PDF
Inactivation of Protein Tyrosine Phosphatase 1B (PTP1B) Activity by the Aqueous Partition of Guava Leaf Extract
5
作者 Wan-Jung Wu Wei-Li Yan +11 位作者 Shiou-Cherng Yu Gerry Gunawan Chien-Yih Lin Chih-Yan Huang Chia-Ting Chang Haw-Wen Chen Chong-Kuei Lii Alice L. Yu Ching-Chu Chen Yu-Ting Chung Jeng-Dau Tsai Henry J. Tsai 《Journal of Pharmacy and Pharmacology》 2018年第10期890-906,共17页
Guava leaf tea has been used as a folk medicine for treating hyperglycemic conditions in Asia and Africa. The hypoglycemic efficacy of guava leaf has been documented by many scientists in these regions, but the hypogl... Guava leaf tea has been used as a folk medicine for treating hyperglycemic conditions in Asia and Africa. The hypoglycemic efficacy of guava leaf has been documented by many scientists in these regions, but the hypoglycemic mechanism is poorly understood. Guava leaves were extracted with methanol and the crude extract was partitioned against hexane, ethyl acetate, and butanol in sequence. The leftover in water is defined as the aqueous partition. A second smaller batch was extracted with hot water directly. Oral glucose tolerance test was carried out on healthy mice instead of diabetic mice that lack endogenous insulin. Glucose uptake was examined with 3T3-L1 adipocytes. Oxidative effect on PTP1B (protein tyrosine phosphatase 1b) was carried out with real-time PTP1B enzymatic assay. The aqueous partition of guava leaf extract possesses a potent inhibitory effect on PTP1B enzymatic activity and this PTP1B inhibition is through a slow oxidative but reversible inactivation on the enzyme. The reversible inactivation would suggest guava leaf extract may augment PTP1B inhibition alongside the endogenous H2O2 which itself is induced by insulin. In addition, our study confirmed the hypoglycemic efficacy being associated with guava leaf and found the most effective molecules reside in the aqueous partition which is also less cytotoxic to Chinese hamster ovary cells when compared to other less polar partitions. The guava leaf extract can modulate insulin activity through a redox regulation on PP1B enzymatic activity. It is speculated that a compound similar to gallocatechin in the aqueous partition can reduce an oxygen molecule to hydrogen peroxide which in turn oxidizes the catalytic residue Cys in PTP1B. Therefore, the guava leaf tea can serve as a functional hypoglycemic drink that is suitable for either healthy or diabetic subjects. 展开更多
关键词 Guava leaf extract HYPOGLYCEMIC OXIDATIVE protein tyrosine phosphatase 1b slow inactivation.
下载PDF
Bioactive chemical constituents from the marine-derived fungus Cladosporium sp.DLT-5
6
作者 Luting DAI Qingyi XIE +6 位作者 Jiaocen GUO Qingyun MA Li YANG Jingzhe YUAN Haofu DAI Zhifang YU Youxing ZHAO 《Journal of Oceanology and Limnology》 SCIE CAS CSCD 2024年第3期905-914,共10页
A new isochromanone,cladosporinisochromanone(1),accompanied by 15 known compounds(2–16)were obtained from secondary metabolites produced by marine-derived fungus Cladosporium sp.DLT-5.NMR and HRESIMS spectra elucidat... A new isochromanone,cladosporinisochromanone(1),accompanied by 15 known compounds(2–16)were obtained from secondary metabolites produced by marine-derived fungus Cladosporium sp.DLT-5.NMR and HRESIMS spectra elucidation determined the planar structure of 1.Subsequent electronic circular dichroism(ECD)experiment assigned the absolute configuration of 1.Compounds 1,2,4–6,and 10 displayed different degrees of neuroprotective activities on human neuroblastoma cells SH-SY5Y.Five compounds(1,3–5,and 13)emerged resistance to protein tyrosine phosphatase 1B(PTP1B),further kinetic analysis and molecular docking study indicated that the most potent compound 13(IC50value of 10.74±0.61μmol/L)was found as a noncompetitive inhibitor for PTP1B.Surface plasmon resonance(SPR)and molecular docking studies also demonstrated the interaction between compound 12 and Niemann-Pick C1 Like 1(NPC1L1),which has been identified as significant therapeutic target for hypercholesteremia.In addition,compounds 3,6,and 14 showed attractive inhibitory activity against the phytopathogenic fungi:Colletotrichum capsici.Therefore,library of Cladosporium metabolites is enriched and new active uses of known compounds are explored. 展开更多
关键词 Cladosporium sp. marine-derived fungus neuroprotective effects protein tyrosine phosphatase 1B(PTP1B) Niemann-Pick C1 Like 1(NPC1L1) antifungal activity
下载PDF
Pachymic acid exerts antitumor activities by modulating the Wnt/β-catenin signaling pathway via targeting PTP1B
7
作者 Hao Zhang Kun Zhu +5 位作者 Xue-Feng Zhang Yi-Hui Ding Bing Zhu Wen Meng Qing-Song Ding Fan Zhang 《Asian Pacific Journal of Tropical Biomedicine》 SCIE CAS 2024年第4期170-180,共11页
Objective:To determine the inhibitory effects of pachymic acid on lung adenocarcinoma(LUAD)cells and elucidate its underlying mechanism.Methods:CCK-8,wound healing,Transwell,Western blot,tube formation,and immunofluor... Objective:To determine the inhibitory effects of pachymic acid on lung adenocarcinoma(LUAD)cells and elucidate its underlying mechanism.Methods:CCK-8,wound healing,Transwell,Western blot,tube formation,and immunofluorescence assays were carried out to measure the effects of various concentrations of pachymic acid on LUAD cell proliferation,metastasis,angiogenesis as well as autophagy.Subsequently,molecular docking technology was used to detect the potential targeted binding association between pachymic acid and protein tyrosine phosphatase 1B(PTP1B).Moreover,PTP1B was overexpressed in A549 cells to detect the specific mechanisms of pachymic acid.Results:Pachymic acid suppressed LUAD cell viability,metastasis as well as angiogenesis while inducing cell autophagy.It also targeted PTP1B and lowered PTP1B expression.However,PTP1B overexpression reversed the effects of pachymic acid on metastasis,angiogenesis,and autophagy as well as the expression of Wnt3a andβ-catenin in LUAD cells.Conclusions:Pachymic acid inhibits metastasis and angiogenesis,and promotes autophagy in LUAD cells by modulating the Wnt/β-catenin signaling pathway via targeting PTP1B. 展开更多
关键词 Pachymic acid Lung adenocarcinoma protein tyrosine phosphatase 1B Wnt/β-catenin signaling pathway METASTASIS ANGIOGENESIS AUTOPHAGY
下载PDF
Inhibition of protein tyrosine phosphatase 1B activity by triterpenes isolated from Aceriphyllum rossii
8
作者 崔龙 李志 +2 位作者 孙亚楠 张南 金永镐 《Journal of Chinese Pharmaceutical Sciences》 CAS 2012年第2期178-182,共5页
An organic layer prepared from the seed of Aceriphyllum rossii was studied to identify the active compounds for protein tyrosine phosphatase 1B(PTP1B) inhibition.Bioassay guided fractionation resulted in the isolati... An organic layer prepared from the seed of Aceriphyllum rossii was studied to identify the active compounds for protein tyrosine phosphatase 1B(PTP1B) inhibition.Bioassay guided fractionation resulted in the isolation of PTP1B inhibitory activity of triterpenes(1-4).These four compounds were identified as aceriphyllic acid C(1),aceriphyllic acid D(2),aceriphyllic acid E(3) and aceriphyllic acid F(4).The isolated 1-4 compounds inhibited PTP1B with IC50 values ranged from(2.1±1.5) μmol/L to(11.2±2.5) μmol/L.Kinetic analysis of PTP1B inhibition by aceriphyllic acid C(1) and aceriphyllic acid D(2) suggested that oleanane-type triterpenes inhibited PTP1B activity in a mixed-type manner. 展开更多
关键词 Aceriphyllum rossii protein tyrosine phosphatase 1B TRITERPENES Bioassay guided
原文传递
Inhibition of protein tyrosine phosphatase 1B by triterpenes isolated from Potentilla discolor Bge 被引量:2
9
作者 脱振东 李娜 +4 位作者 李佳琳 齐世洲 李班班 张乐 崔龙 《Journal of Chinese Pharmaceutical Sciences》 CAS CSCD 2016年第3期224-227,共4页
Seven oleanene triterpenes were isolated from the roots of Potentilla discolor Bge and their structures were identified as 3-oxoolean-12-en-27-oic acid(1), gypsogenic acid(2), 3α-hydroxyolean-12-en-27-oic acid(3... Seven oleanene triterpenes were isolated from the roots of Potentilla discolor Bge and their structures were identified as 3-oxoolean-12-en-27-oic acid(1), gypsogenic acid(2), 3α-hydroxyolean-12-en-27-oic acid(3), 3β-hydroxyolean-12-en-27-oic acid(4), aceriphyllic acid A(5), aceriphyllic acid A methyl ester(6), and oleanolic acid(7). Compounds 1–7 inhibited protein tyrosine phosphatase 1B(PTP1B) activity, with IC50 values ranging from(7.5±0.5) to(22.7±0.5) μmol/L. Among the isolates, compounds 1, 2, 3 and 7 from the Potentilla discolor Bge were found to exhibit selective PTP1 B inhibitory activity. 展开更多
关键词 Potentilla discolor Bge protein tyrosine phosphatase 1B TRITERPENES
原文传递
Novel and emerging diabetes mellitus drug therapies for the type 2 diabetes patient 被引量:3
10
作者 Charmaine D Rochester Oluwaranti Akiyode 《World Journal of Diabetes》 SCIE CAS 2014年第3期305-315,共11页
Type 2 diabetes mellitus is a metabolic disorder of deranged fat, protein and carbohydrate metabolism resulting in hyperglycemia as a result of insulin resistance and inadequate insulin secretion. Although a wide vari... Type 2 diabetes mellitus is a metabolic disorder of deranged fat, protein and carbohydrate metabolism resulting in hyperglycemia as a result of insulin resistance and inadequate insulin secretion. Although a wide variety of diabetes therapies is available, yet limited efficacy, adverse effects, cost, contraindications, renal dosage adjustments, inflexible dosing schedules and weight gain significantly limit their use. In addition, many patients in the United States fail to meet the therapeutic HbA1c goal of 【 7% set by the American Diabetes Association. As such new and emerging diabetes therapies with different mechanisms of action hope to address some of these drawbacks to improve the patient with type 2 diabetes. This article reviews new and emerging classes, including the sodium-glucosecotransporter-2 inhibitors, 11β-Hydroxysteroid dehydrogenase type 1 inhibitors, glycogen phosphorylase inhibitors; protein tyrosine phosphatase 1B inhibitors, G Protein-Coupled receptor agonists and glucokinase activators. These emerging diabetes agents hold the promise of providing benefit of glucose lowering, weight reduction, low hypoglycemia risk, improve insulin sensitivity, pancreatic β cell preservation, and oral formulation availability. However, further studies are needed to evaluate their safety profile, cardiovascular effects, and efficacy durability in order to determine their role in type 2 diabetes management. 展开更多
关键词 Type 2 diabetes mellitus Sodium dependent glucose co-transporter 2 inhibitors 11β -Hydroxysteroid dehydrogenase type 1 inhibitors Glycogen phosphorylase inhibitors protein tyrosine phosphatase 1B inhibitors G protein-coupled receptor agonists Glucokinase activators
下载PDF
Extraction and PTP1B inhibitory activity of bromophenols from the marine red alga Symphyocladia latiuscula 被引量:2
11
作者 刘旭 李晓明 +4 位作者 高立信 崔传明 李春顺 李佳 王斌贵 《Chinese Journal of Oceanology and Limnology》 SCIE CAS CSCD 2011年第3期686-690,共5页
Previously, we had characterized several structurally interesting brominated phenols from the marine red alga Symphyocladia latiuscula collected from various sites. However, Phytochemical investigations on this specie... Previously, we had characterized several structurally interesting brominated phenols from the marine red alga Symphyocladia latiuscula collected from various sites. However, Phytochemical investigations on this species collected from the Weihai coastline of Shandong Province remains blank. Therefore, we characterized the chemical constituents of individuals of this species collected from the region. Eight bromophenols were isolated and identified. Using detailed spectroscopic techniques and comparisons with published data, these compounds were identified as 2,3-dibromo-4,5-dihydroxybenzyl methyl ether (1), 3,5-dibromo-4-hydroxybenzoic acid (2), 2,3,6-tribromo-4,5-dihydroxymethylbenzene (3), 2,3,6-tribromo-4,5-dihydroxybenzaldehyde (4), 2,3,6-tribromo-4,5-dihydroxybenzyl methyl ether (5), bis(2,3,6-tribromo-4,5-dihydroxyphenyl)methane (6), 1,2-bis(2,3,6-tribromo-4,5-dihydroxyphenyl)-ethane (7), and 1-(2,3,6-tribromo-4,5-dihydroxybenzyl)-pyrrolidin-2-one (8). Among these compounds, 1 and 2 were isolated for the first time from S. latiuscula. Each compound was evaluated on the ability to inhibit protein tyrosine phosphatase 1B (PTP1B), which is a potential therapeutic target in the treatment of type 2 diabetes. Bromophenols 5, 6, and 7 showed strong activities with IC50 values of 3.9, 4.3, and 3.5 μmol/L, respectively. This study provides further evidence that bromophenols are predominant among the chemical constituents of Symphyocladia, and that some of these compounds may be candidates for the development of anti-diabetes drugs. 展开更多
关键词 marine alga RHODOMELACEAE Symphyocladia latiuscula bromophenol protein tyrosine phosphatase 1B (PTP1B)
下载PDF
Synthesis of mangiferin derivates and study their potent PTP1B inhibitory activity 被引量:2
12
作者 Hong Gang Hu Ming Juan Wang +3 位作者 Qing Jie Zhao Shi Chong Yu Chao Mei Liu Qiu Ye Wu 《Chinese Chemical Letters》 SCIE CAS CSCD 2007年第11期1323-1326,共4页
Protein tyrosine phosphatase 1 B (PTP1 B) has received considerable attention from the drug industry as a potential treatment for diabetes mellitus. Mangiferin has been reported to possess significant antidiabetic a... Protein tyrosine phosphatase 1 B (PTP1 B) has received considerable attention from the drug industry as a potential treatment for diabetes mellitus. Mangiferin has been reported to possess significant antidiabetic activity. Based on the previous study, eight new mangiferin derivates were synthesized and evaluated for their PTP1B inhibitory activity. Some of them displayed good inhibitory activity on PTP1B. 展开更多
关键词 MANGIFERIN protein tyrosine phosphatase 1B Dedvates INHIBITION
下载PDF
Protein tyrosine phosphatase 1B expression contributes to the development of breast cancer 被引量:2
13
作者 Shi-chong LIAO Jin-xin LI +1 位作者 Li YU Sheng-rong SUN 《Journal of Zhejiang University-Science B(Biomedicine & Biotechnology)》 SCIE CAS CSCD 2017年第4期334-342,共9页
The protein tyrosine phosphatase 1B(PTP1B)is an important regulator of metabolism.The relationship between PTP1B and tumors is quite complex.The purpose of this study is to explore the expression pattern and role of... The protein tyrosine phosphatase 1B(PTP1B)is an important regulator of metabolism.The relationship between PTP1B and tumors is quite complex.The purpose of this study is to explore the expression pattern and role of PTP1B in breast cancer.The expression of PTP1B was detected in 67 samples of breast cancer tissue by Western blot.Cell growth assay,Transwell migration assay,and Scratch motility assay were used to examine the proliferation and migration of MCF-7 with and without PTP1B.The total levels and phosphorylated levels of signal transduction and activator of transcription 3(STAT3)and the expression of C-C motif chemokine ligand 5(CCL5)were also examined by Western blot.PTP1B was overexpressed in over 70%of breast cancer tissues,correlating with patients with estrogen receptor(ER)-negative,progesterone receptor(PR)-negative,and human epidermal growth factor receptor 2(HER2)-positive tumors.The data also showed that both tumor size and lymph node metastasis were significantly higher in patients with a higher level of PTP1B.The proliferation and migration of MCF-7 cells were found to be inhibited after knocking down the gene of PTP1B.Our data also showed that PTP1B could up-regulate the dephosphorylated level of STAT3,which could increase the expression of CCL5.These phenomena indicated that PTP1B may play a crucial role in the development of breast cancer. 展开更多
关键词 protein tyrosine phosphatase 1B (PTP1B) Signal transduction and activator of transcription 3 (STAT3) Breast cancer TUMORIGENESIS
原文传递
Isoprenylated Flavonoids with PTP1B Inhibition from Macaranga denticulata 被引量:1
14
作者 Lai-Bin Zhang Chun Lei +3 位作者 Li-Xin Gao Jing-Ya Li Jia Li Ai-Jun Hou 《Natural Products and Bioprospecting》 CAS 2016年第1期25-30,共6页
Three new C-methylated and isoprenylated chalcone derivatives,dentichalcones A–C(1–3),together with six known compounds(4–9),were isolated from the twigs and leaves of Macaranga denticulata.Their structures were el... Three new C-methylated and isoprenylated chalcone derivatives,dentichalcones A–C(1–3),together with six known compounds(4–9),were isolated from the twigs and leaves of Macaranga denticulata.Their structures were elucidated by spectroscopic analysis,including 1D,2D NMR,and MS data.The known compounds,(2E)-1-(5,7-dihydroxy-2,2,6-trimethyl-2H-benzopyran-8-yl)-3-(4-methoxyphenyl)-2-propen-1-one(4),(2E)-1-(5,7-dihydroxy-2,2-dimethyl-2H-benzopyran-8-yl)-3-phenyl-2-propen-1-one(5),laxichalcone(6),macarangin(7),bonanniol A(8),and bonannione A(9),showed inhibitory activities against protein tyrosine phosphatase 1B(PTP1B)in vitro.Graphical Abstract Three new C-methylated and isoprenylated chalcone derivatives,dentichalcones A–C(1–3),together with six known compounds,were isolated from the twigs and leaves of Macaranga denticulata.Some compounds showed inhibitory activities against PTP1B in vitro. 展开更多
关键词 Macaranga denticulata EUPHORBIACEAE Isoprenylated flavonoids Dentichalcones A-C protein tyrosine phosphatase 1B
下载PDF
Protein Tyrosine Phosphatase 1B Inhibitors from Plantago asiatica
15
作者 LEE Hyun-sun AHN Jong-seog 《Chinese Herbal Medicines》 CAS 2011年第2期136-139,共4页
Objective To identify the active compounds for protein tyrosine phosphatase 1B(PTP1B) from the seeds of Plantago asiatica.Methods Bioassay-guided fractionation resulted in the isolation of iridoid glucosides(1-5) with... Objective To identify the active compounds for protein tyrosine phosphatase 1B(PTP1B) from the seeds of Plantago asiatica.Methods Bioassay-guided fractionation resulted in the isolation of iridoid glucosides(1-5) with PTP1B inhibitory activity.Results Five compounds were identified as desacetylhookerioside(1),melittoside(2),geniposidic acid(3),10-O-acetyl-geniposidic acid(4),and alpinoside(5).Conclusion Isolated compounds 35 inhibit PTP1B with IC50 values ranged from(16.3 ± 1.1) to(19.8 ± 1.2) μmol/L. 展开更多
关键词 alpinoside geniposidic acid iridoid glucosides Plantago asiatica protein tyrosine phosphatase 1B
原文传递
A key role for PTP1B in dendritic cell maturation, migration, and T cell activation 被引量:1
16
作者 Cristina Martin-Granados Alan R.Prescott +7 位作者 Samantha Le Sommer Izabela P.Klaska Tian Yu Elizabeth Muckersie Claudiu V.Giuraniuc Louise Grant Mirela Delibegovic John V.Forrester 《Journal of Molecular Cell Biology》 SCIE CAS CSCD 2015年第6期517-528,共12页
Dendritic cells(DC)are the major antigen-presenting cells bridging innate and adaptive immunity,a function they perform by converting quiescent DC to active,mature DC with the capacity to activate naı¨ve T cells.... Dendritic cells(DC)are the major antigen-presenting cells bridging innate and adaptive immunity,a function they perform by converting quiescent DC to active,mature DC with the capacity to activate naı¨ve T cells.They do this by migrating from the tissues to the T cell area of the secondary lymphoid tissues.Here,wedemonstrate thatmyeloid cell-specific genetic deletion of PTP1B(LysM PTP1B)leads to defects in lipopolysaccharide-driven bone marrow-derivedDC(BMDC)activation associated with increased levels of phosphorylated Stat3.We showthatmyeloid cell-specific PTP1Bdeletion also causes decreased migratory capacity of epidermal DC,aswell as reduced CCR7 expression and chemotaxis to CCL19 by BMDC.PTP1B deficiency in BMDC also impairs their migration in vivo.Further,immature LysM PTP1B BMDC display fewer podosomes,increased levels of phosphorylated Src at tyrosine 527,and loss of Src localization to podosome puncta.In co-culture with T cells,LysM PTP1B BMDC establish fewer and shorter contacts than control BMDC.Finally,LysMPTP1BBMDCfail to present antigen to T cells as efficiently as controlBMDC.These data provide first evidence for a key regulatory role for PTP1B in mediating a central DC function of initiating adaptive immune responses in response to innate immune cell activation. 展开更多
关键词 dendritic cell maturation PODOSOMES T cell activation adaptive immune response protein tyrosine phosphatase 1B
原文传递
Enantiomeric pairs of meroterpenoids from Rhododendron fastigiatum
17
作者 HUANG Guang-Hui LEI Chun +3 位作者 ZHU Ke-Xin LI Jing-Ya LI Jia HOU Ai-Jun 《Chinese Journal of Natural Medicines》 SCIE CAS CSCD 2019年第12期963-969,共7页
Five pairs of optically pure meroterpenoid enantiomers(1 a/1 b-5 a/5 b)and two known compounds(6 and 7)were isolated from Rhododendron fastigiatum.Compounds 1 a/1 b-5 a/5 b were resolved from naturally scalemic mixtur... Five pairs of optically pure meroterpenoid enantiomers(1 a/1 b-5 a/5 b)and two known compounds(6 and 7)were isolated from Rhododendron fastigiatum.Compounds 1 a/1 b-5 a/5 b were resolved from naturally scalemic mixtures by chiral HPLC.Their structures were elucidated by spectroscopic methods,X-ray crystallographic experiments,and ECD analyses.Compounds 1 a/1 b,2 a/2 b,3 b,4 a/4 b,and 5 a/5 b were new meroterpenoids with different polycyclic systems.Two enantiomeric pairs(2 a/2 b and 3 a/3 b),6,and 7 exhibited inhibitory effects on protein tyrosine phosphatase 1 B(PTP1 B)in vitro. 展开更多
关键词 Rhododendron fastigiatum Meroterpenoid enantiomers protein tyrosine phosphatase 1B
原文传递
上一页 1 下一页 到第
使用帮助 返回顶部