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Phosphoprotein phosphatase 1-interacting proteins as therapeutic targets in prostate cancer
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作者 Juliana Felgueiras Margarida Fardilha 《World Journal of Pharmacology》 2014年第4期120-139,共20页
Prostate cancer is a major public health concern world-wide, being one of the most prevalent cancers in men. Great improvements have been made both in terms of early diagnosis and therapeutics. However, there is still... Prostate cancer is a major public health concern world-wide, being one of the most prevalent cancers in men. Great improvements have been made both in terms of early diagnosis and therapeutics. However, there is still an urgent need for reliable biomarkers that could overcome the lack of cancer-specifcity of prostate-specifc antigen, as well as alternative therapeutic targets for advanced metastatic cases. Reversible phosphorylation of proteins is a post-translational modifcation critical to the regulation of numerous cellular processes. Phosphoprotein phosphatase 1 (PPP1) is a major serine/threonine phos-phatase, whose specifcity is determined by its interacting proteins. These interactors can be PPP1 substrates, regulators, or even both. Deregulation of this protein-protein interaction network alters cell dynamics and underlies the development of several cancer hallmarks. Therefore, the identification of PPP1 interactome in specific cellular context is of crucial importance. The knowledge on PPP1 complexes in prostate cancer remains scarce, with only 4 holoenzymes characterized in human prostate cancer models. However, an increasing number of PPP1 interactors have been identifed as expressed in human prostate tissue, including the tumor suppressors TP53 and RB1. Efforts should be made in order to identify the role of such proteins in prostate carcinogenesis, since only 26 have yet well-recognized roles. Here, we revise literature and human protein databases to provide an in-depth knowledge on the biological significance of PPP1 complexes in human prostate carcinogenesis and their potential use as therapeutic targets for the development of new therapies for prostate cancer. 展开更多
关键词 Prostate cancer Reversible phosphorylation Phosphoprotein phosphatase 1 Phosphoprotein phosphatase 1-interacting proteins protein complexes Therapeutic targets
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Mitogen-activated protein kinase phosphatase 1 protects PC12 cells from amyloid beta-induced neurotoxicity 被引量:7
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作者 Yue Gu Lian-Jun Ma +4 位作者 Xiao-Xue Bai Jing Jie Xiu-Fang Zhang Dong Chen Xiao-Ping Li 《Neural Regeneration Research》 SCIE CAS CSCD 2018年第10期1842-1850,共9页
The mitogen-activated protein kinase(MAPK) signaling pathway plays an important role in the regulation of cell growth, proliferation, differentiation, transformation and death. Mitogen-activated protein kinase phosp... The mitogen-activated protein kinase(MAPK) signaling pathway plays an important role in the regulation of cell growth, proliferation, differentiation, transformation and death. Mitogen-activated protein kinase phosphatase 1(MKP1) has an inhibitory effect on the p38 MAPK and JNK pathways, but it is unknown whether it plays a role in Aβ-induced oxidative stress and neuronal inflammation. In this study, PC12 cells were infected with MKP1 sh RNA, MKP1 lentivirus or control lentivirus for 12 hours, and then treated with 0.1, 1, 10 or 100 μM amyloid beta 42(Aβ42). The cell survival rate was measured using the cell counting kit-8 assay. MKP1, tumor necrosis factor-alpha(TNF-α) and interleukin-1β(IL-1β) m RNA expression levels were analyzed using quantitative real time-polymerase chain reaction. MKP1 and phospho-c-Jun N-terminal kinase(JNK) expression levels were assessed using western blot assay. Reactive oxygen species(ROS) levels were detected using 2′,7′-dichlorofluorescein diacetate. Mitochondrial membrane potential was measured using flow cytometry. Superoxide dismutase activity and malondialdehyde levels were evaluated using the colorimetric method. Lactate dehydrogenase activity was measured using a microplate reader. Caspase-3 expression levels were assessed by enzyme-linked immunosorbent assay. Apoptosis was evaluated using the terminal deoxynucleotidyl transferase d UTP nick end labeling method. MKP1 overexpression inhibited Aβ-induced JNK phosphorylation and the increase in ROS levels. It also suppressed the Aβ-induced increase in TNF-α and IL-1β levels as well as apoptosis in PC12 cells. In contrast, MKP1 knockdown by RNA interference aggravated Aβ-induced oxidative stress, inflammation and cell damage in PC12 cells. Furthermore, the JNK-specific inhibitor SP600125 abolished this effect of MKP1 knockdown on Aβ-induced neurotoxicity. Collectively, these results show that MKP1 mitigates Aβ-induced apoptosis, oxidative stress and neuroinflammation by inhibiting the JNK signaling pathway, thereby playing a neuroprotective role. 展开更多
关键词 nerve regeneration mitogen-activated protein kinase phosphatase 1 c-Jun N-terminal kinase signaling pathway Alzheimer's disease neurons DEMENTIA apoptosis RNA interference lentivirus inflammation oxidative stress neural regeneration
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Protein tyrosine phosphatase 1B regulates migration of ARPE-19 cells through EGFR/ERK signaling pathway 被引量:3
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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
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Overexpression of mitogen-activated protein kinase phosphatase-1 in endothelial cells reduces blood-brain barrier injury in a mouse model of ischemic stroke 被引量:2
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作者 Xiu-De Qin Tai-Qin Yang +6 位作者 Jing-Hui Zeng Hao-Bin Cai Shao-Hua Qi Jian-Jun Jiang Ying Cheng Long-Sheng Xu Fan Bu 《Neural Regeneration Research》 SCIE CAS CSCD 2023年第8期1743-1749,共7页
Ischemic stroke can cause blood-brain barrier(BBB)injury,which worsens brain damage induced by stroke.Abnormal expression of tight junction proteins in endothelial cells(ECs)can increase intracellular space and BBB le... Ischemic stroke can cause blood-brain barrier(BBB)injury,which worsens brain damage induced by stroke.Abnormal expression of tight junction proteins in endothelial cells(ECs)can increase intracellular space and BBB leakage.Selective inhibition of mitogen-activated protein kinase,the negative regulatory substrate of mitogen-activated protein kinase phosphatase(MKP)-1,improves tight junction protein function in ECs,and genetic deletion of MKP-1 aggravates ischemic brain injury.However,whether the latter affects BBB integrity,and the cell type-specific mechanism underlying this process,remain unclear.In this study,we established an adult male mouse model of ischemic stroke by occluding the middle cerebral artery for 60 minutes and overexpressed MKP-1 in ECs on the injured side via lentiviral transfection before stroke.We found that overexpression of MKP-1 in ECs reduced infarct volume,reduced the level of inflammatory factors interleukin-1β,interleukin-6,and chemokine C-C motif ligand-2,inhibited vascular injury,and promoted the recovery of sensorimotor and memory/cognitive function.Overexpression of MKP-1 in ECs also inhibited the activation of cerebral ischemia-induced extracellular signal-regulated kinase(ERK)1/2 and the downregulation of occludin expression.Finally,to investigate the mechanism by which MKP-1 exerted these functions in ECs,we established an ischemic stroke model in vitro by depriving the primary endothelial cell of oxygen and glucose,and pharmacologically inhibited the activity of MKP-1 and ERK1/2.Our findings suggest that MKP-1 inhibition aggravates oxygen and glucose deprivation-induced cell death,cell monolayer leakage,and downregulation of occludin expression,and that inhibiting ERK1/2 can reverse these effects.In addition,co-inhibition of MKP-1 and ERK1/2 exhibited similar effects to inhibition of ERK1/2.These findings suggest that overexpression of MKP-1 in ECs can prevent ischemia-induced occludin downregulation and cell death via deactivating ERK1/2,thereby protecting the integrity of BBB,alleviating brain injury,and improving post-stroke prognosis. 展开更多
关键词 blood-brain barrier brain injury cerebral ischemia endothelial cells extracellular signal-regulated kinase 1/2 functional recovery mitogenactivated protein kinase phosphatase 1 OCCLUDIN oxygen and glucose deprivation transient middle cerebral artery occlusion
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Structural Insight into the Design on Oleanolic Acid Derivatives as Potent Protein Tyrosine Phosphatase 1B Inhibitors 被引量:2
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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
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Synthesis and protein tyrosine phosphatase 1B inhibition activities of two new synthetic bromophenols and their methoxy derivatives 被引量:1
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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
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POM analysis and computational interactions of 8-hydroxydiospyrin inside active site of protein tyrosine phosphatase 1B
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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
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A role for mitogen-activated protein kinase phosphatase 1(MKP1) in neural cell development and survival
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作者 André Toulouse Yvonne M.Nolan 《Neural Regeneration Research》 SCIE CAS CSCD 2015年第11期1748-1749,共2页
The mitogen-activated protein kinase(MAPK)pathways are a group of conserved intracellular signalling pathways present in most cells including neurons and glia.These pathways respond to a variety of stimuli including... The mitogen-activated protein kinase(MAPK)pathways are a group of conserved intracellular signalling pathways present in most cells including neurons and glia.These pathways respond to a variety of stimuli including growth factors,cytokines and oxidative stress to generate appropriate cellular responses such as modulation of gene expression,cell proliferation,differentiation and survival as well as the stress response(Korhonen and Moilanen,2014). 展开更多
关键词 MKP1 A role for mitogen-activated protein kinase phosphatase 1 in neural cell development and survival CELL
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Inactivation of Protein Tyrosine Phosphatase 1B (PTP1B) Activity by the Aqueous Partition of Guava Leaf Extract
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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.
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Functional repertoire of protein kinases and phosphatases in synaptic plasticity and associated neurological disorders
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作者 Raheel Khan Don Kulasiri Sandhya Samarasinghe 《Neural Regeneration Research》 SCIE CAS CSCD 2021年第6期1150-1157,共8页
Protein phosphorylation and dephosphorylation are two essential and vital cellular mechanisms that regulate many receptors and enzymes through kinases and phosphatases.Ca^2+- dependent kinases and phosphatases are res... Protein phosphorylation and dephosphorylation are two essential and vital cellular mechanisms that regulate many receptors and enzymes through kinases and phosphatases.Ca^2+- dependent kinases and phosphatases are responsible for controlling neuronal processing;balance is achieved through opposition.During molecular mechanisms of learning and memory,kinases generally modulate positively while phosphatases modulate negatively.This review outlines some of the critical physiological and structural aspects of kinases and phosphatases involved in maintaining postsynaptic structural plasticity.It also explores the link between neuronal disorders and the deregulation of phosphatases and kinases. 展开更多
关键词 Alzheimer’s disease autism spectrum disorder CAMKII CALCINEURIN longterm depression long-term potentiation protein kinase A protein phosphatase 1 protein dephosphorylation protein phosphorylation
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Pachymic acid exerts antitumor activities by modulating the Wnt/β-catenin signaling pathway via targeting PTP1B
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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
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Extraction and PTP1B inhibitory activity of bromophenols from the marine red alga Symphyocladia latiuscula 被引量:2
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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)
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Synthesis of mangiferin derivates and study their potent PTP1B inhibitory activity 被引量:2
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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
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Isoprenylated Flavonoids with PTP1B Inhibition from Macaranga denticulata 被引量:1
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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
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Structural Analysis of an Oligosaccharide and Glycopeptide Mixture from Panax Ginseng Root with Inhibition SHP-1 Function
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作者 WANG Ying GAO Qi-pin +4 位作者 LI Gui-rong CHEN Ying-hong LUO Hao-ming GAO Yang JIANG Rui-zhi 《Chemical Research in Chinese Universities》 SCIE CAS CSCD 2011年第1期104-107,共4页
A mixture of oligosaccharide and glycopeptide was isolated from the aqueous extract of Panax ginseng roots. The mixture inhibits protein tyrosinc phosphatase(SHP-1) function, implying it enhances immune activity. Th... A mixture of oligosaccharide and glycopeptide was isolated from the aqueous extract of Panax ginseng roots. The mixture inhibits protein tyrosinc phosphatase(SHP-1) function, implying it enhances immune activity. The peak molecular mass of the oligosaccharide portion is 1800 calculated via GPC software after separation by HPLC. And the structure of the oligosaccharide portion is the backbone of (1→3)- and (1→4)-linked arabinopyranoside, and (1→4)- and (1→6)-linked glucopyranoside, with non-reducing terminals of arabinopyranoside and glucopyranoside. The peak molecular mass of glycopeptide portion is 1900 calculated via GPC software after separation by HPLC. The structure of glycopeptide portion is the backbone of (1→3)- and (1→4)-linked arabinopyranoside, and (1→3,6)-linked glucopyranoside, with non-reducing terminals of galactopyranose and glucopyranoside. The peptide composition is Glu. Asp, Hyp, Set, Arg, Gly , Thr, Pro, Ala, Val, lie, Leu and Lys. The oligosaccharide-peptide linkage is formed by Ara and Hyp. 展开更多
关键词 Panax ginseng OLIGOSACCHARIDE GLYCOPEPTIDE protein tyrosine phosphatase(SHP-1 Methylation analysis
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Inhibition of protein tyrosine phosphatase 1B activity by triterpenes isolated from Aceriphyllum rossii
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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
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Inhibition of protein tyrosine phosphatase 1B by triterpenes isolated from Potentilla discolor Bge 被引量:2
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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
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Bioactive chemical constituents from the marine-derived fungus Cladosporium sp.DLT-5
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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
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Protein tyrosine phosphatase 1B expression contributes to the development of breast cancer 被引量:2
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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
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Protein Tyrosine Phosphatase 1B Inhibitors from Plantago asiatica
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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
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