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Allosteric modulation of G protein-coupled receptors as a novel therapeutic strategy in neuropathic pain

Acta Pharmaceutica Sinica B 2024年第1期14卷 67-86页

作者： Chunhao Zhu Xiaobing Lan Zhiqiang Wei Jianqiang Yu Jian Zhang School of Pharmacy Ningxia Medical UniversityYinchuan 750004China Medicinal Chemistry and Bioinformatics Center Shanghai Jiao Tong University School of MedicineShanghai 200025China School of Basic medical Science Ningxia Medical UniversityYinchuan 750004China Medicinal Chemistry and Bioinformatics Center Ocean University of ChinaQingdao 266100China State Key Laboratory of Pharmaceutical Biotechnology Nanjing UniversityNanjing 210023China

Neuropathic pain is a debilitating pathological condition that presents significant therapeutic challenges in clinical ***,current pharmacological treatments for neuropathic pain lack clinical efficacy and often lead to harmful adverse *** G protein-coupled receptors(GPCRs)are widely distributed throughout the body,including the pain transmission pathway and descending inhibition pathway,the development of novel neuropathic pain treatments based on GPCRs allosteric modulation theory is gaining *** research has shown that allosteric modulators targeting GPCRs on the pain pathway can effectively alleviate symptoms of neuropathic pain while reducing or eliminating adverse *** review aims to provide a comprehensive summary of the progress made in GPCRs allosteric modulators in the treatment of neuropathic pain,and discuss the potential benefits and adverse factors of this *** will also concentrate on the development of biased agonists of GPCRs,and based on important examples of biased agonist development in recent years,we will describe universal strategies for designing structure-based biased *** is foreseeable that,with the continuous improvement of GPCRs allosteric modulation and biased agonist theory,effective GPCRs allosteric drugs will eventually be available for the treatment of neuropathic pain with acceptable safety.

关键词： Neuropathic pain Allosteric modulators G protein-coupled receptors Analgesia

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Enhanced photocatalytic performance of Bi_(2)O_(2)CO_(3)/Bi_(4)O_(5)Br_(2)/reduced graphene oxide Z-schemehe terojunction via a one-pot room-temperature synthesis

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Journal of Environmental Sciences 2024年第4期138卷 418-427页

作者： Xiaoge Wu Lei Yan Rongrong Qin Qikai Zhang Wei Yang Xiaozhi Wang Yongcai Zhang Min Luo Jianhua Hou College of Environmental Science and Engineering Yangzhou UniversityYangzhouJiangsu 225009China Jiangsu Collaborative Innovation Center for Solid Organic Waste Resource Utilization Nanjing 210095China Beijing Xinfeng Aerospace Equipment Co. Ltd.Beijing 100854China Beijing System Design Institute of Electro-Mechanic Engineering Beijing 100005China College of Chemistry and Chemical Engineering Ningxia UniversityYinchuanNingxia 750021China

Bi_(2)O_(2)CO_(3)(BOC)/Bi_(4)O_5Br_(2)(BOB)/reduced graphene oxide(rGO)Z-scheme heterojunction with promising photocatalytic properties was synthesized via a facile one-pot room-temperature ***-thin nanosheets of BOC and BOB were grown in situ on r *** formed 2D/2D direct Z-scheme heterojunction of BOC/BOB with oxygen vacancies(OVs)effectively leads to lower negative electron reduction potential of BOB as well as higher positive hole oxidation potential of BOC,showing improved reduction/oxidation ***,rGO is an acceptor of the electrons from the conduction band of *** dual roles significantly improve the transfer performance of photo-induced charge carriers and accelerate their *** layered nanosheet structure,rich OVs,high specific surface area,and increased utilization efficiency of visible light,the multiple synergistic effects of BOC/BOB/rGO can achieve effective generation and separation of the electron-holes,thereby generating more·O_(2)^(-)and h^(+).The photocatalytic reduction efficiency of CO_(2)to CO(12.91μmol/(g·hr))is three times higher than that of BOC(4.18μmol/(g·hr)).Moreover,it also achieved almost 100%removal of Rhodamine B and cyanobacterial cells within 2 hours.

关键词： Bi_(2)O_(2)CO_(3) Bi_(4)O_(5)Br_(2) Reduced graphene oxide Z-scheme heterojunction Photocatalysis CO_(2)reduction

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Synthesis and Enhanced Acetone-sensing Properties of Ordered Large-pore Mesoporous Nickel Oxides with Ultrathin Crystalline Frameworks

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Chemical Research in Chinese universities 2024年第3期40卷 521-528页

作者： SHAO Chen GUO Ru LI Hui WANG Xiaozhong YANG Qingfeng LAI Xiaoyong State Key Laboratory of High-efficiency Utilization of Coal and Green Chemical Engineering School of Chemistry and Chemical EngineeringNingxia UniversityYinchuan 750021P.R.China

Acetone is a tracer for monitoring air quality and a potential breath maker for diabetes. It remains a great challenge for current portable sensors to sensitively and selectively detect acetone at low-ppb (part per billion) level. Herein, we present an ordered mesoporous nickel oxide (NiO) with both large mesopores and ultrathin crystalline frameworks for the detection of low-ppb acetone. The ordered mesoporous NiO replicas with predominant large mesopores of 11 nm, high specific surface areas of 121–128 m2/g and ultrathin crystalline frameworks of 5 nm were synthesized by the nanocasting method and the crystalline properties of NiO frameworks were adjusted by changing the annealing temperature from 300℃ to 750℃, which resulted in different contents of oxygen deficient on the surface of ultrathin frameworks. The gas-sensing properties for all the NiO samples were investigated and the ordered large-pore mesoporous NiO (NiO-600) with maximum oxygen deficient obtained at 600℃ exhibited the highest response (R_(gas)/R_(air)−1=2.9) toward acetone (1 ppm, ppm: part per million), which is 3.4 and 30 times larger than those for common mesoporous NiO obtained at 300℃ and bulk NiO. Notably, a low detection limit (2 ppb), good selectivity and cycling stability were also observed in NiO-600.

关键词： Mesoporous semiconductor NiO Gas sensing Acetone

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G protein-coupled receptors(GPCRs):advances in structures,mechanisms,and drug discovery

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Signal Transduction and Targeted Therapy 2024年第5期9卷 1938-1980页

作者： Mingyang Zhang Ting Chen Xun Lu Xiaobing Lan Ziqiang Chen Shaoyong Lu Key Laboratory of Protection Development and Utilization of Medicinal Resources in Liupanshan AreaMinistry of EducationPeptide&Protein Drug Research CenterSchool of PharmacyNingxia Medical UniversityYinchuan 750004China Medicinal Chemistry and Bioinformatics Center Shanghai Jiao Tong University School of MedicineShanghai 200025China Department of Cardiology Changzheng HospitalAffiliated to Naval Medical UniversityShanghai 200003China Department of Orthopedics Changhai HospitalAffiliated to Naval Medical UniversityShanghai 200433China

G protein-coupled receptors(GPCRs),the largest family of human membrane proteins and an important class of drug targets,play a role in maintaining numerous physiological *** or antagonist,orthosteric effects or allosteric effects,and biased signaling or balanced signaling,characterize the complexity of GPCR dynamic *** this study,we first review the structural advancements,activation mechanisms,and functional diversity of *** then focus on GPCR drug discovery by revealing the detailed drug-target interactions and the underlying mechanisms of orthosteric drugs approved by the US Food and Drug Administration in the past five ***,an up-to-date analysis is performed on available GPCR structures complexed with synthetic small-molecule allosteric modulators to elucidate key receptor-ligand interactions and allosteric ***,we highlight how the widespread GPCR-druggable allosteric sites can guide structure-or mechanism-based drug design and propose prospects of designing bitopic ligands for the future therapeutic potential of targeting this receptor family.

关键词： steric designing mechanisms

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Intraperitoneal injection but not oral administration of ellagic acid: A novel immunomodulator via targeting casein kinase 2 signaling pathway

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Food Science and Human Wellness 2024年

作者： Wen-Hui Qi Bing Han Ting-Ting Cui Pei-Xin Shen Zhuo-Hua Zhao Ya-Ping Yan Li-Bin Wang Xin-Yu Lu Yuan Zhang Xing Li Key Laboratory of Medicinal Resources and Natural Pharmaceutical Chemistry (Shaanxi Normal University)， The Ministry of Education College of Life Sciences， Shaanxi Normal University Department of Pharmacology， School of Pharmacy， Fourth Military medical University The Nervous System Disease Diagnosis and Treatment Engineering Technology Research Center of ningxia School of medical Technology， Xi'an medical University

Immunosuppressants currently approved for the treatment of autoimmune diseases and organ transplant rejection present diverse adverse effects that impair the life quality of patients. Therefore， the development of novel immunomodulators with high efficiency and low toxicity is essential. Ellagic acid (EA)， a natural polyphenol compound widely distributed in berries， is metabolically transformed by gut microbiome to exert systemic health benefits. Here， we identified that intraperitoneal administration of EA with no cytotoxicity， beyond its well-known oral metabolic fate， effectively decreased clinical severity and CNS inflammation/demyelination in experimental autoimmune encephalomyelitis (EAE)， a mouse model of an autoimmune disease multiple sclerosis (MS). Interestingly， intraperitoneal EA administration at incredibly low doses (0.1 mg/kg/d) is dose-sparing with fingolimod (FTY720)， the first FDA-approved oral drug for MS. In addition， intraperitoneal EA also ameliorated the brain damage in a neuromyelitis optica (NMO) model， and significantly prevented the immune rejection of allograft skin graft. Evidence from pharmacological studies combined with RNA-seq indicate that prototype EA functions by a mechanism that involves direct inhibition of casein kinase II (CKII) to suppress the expression of IL-17 and promote the expression of Cpt1a to regulate Th17 differentiation. In conclusion， our study demonstrates that the prototype EA entering the blood circulation acts as a novel therapeutic immunomodulator for the treatment of autoimmune diseases and transplant rejection through the CKⅡ-mediated JAK/STAT/Cpt1a signaling pathway.

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Correlation between the charge radii difference in mirror partner nuclei and thesymmetry energy slope

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Chinese Physics C 2024年第8期48卷 177-184页

作者： Xiao-Rong Ma Shuai Sun Rong An Li-Gang Cao School of Physics Ningxia UniversityYinchuan 750021China Key Laboratory of Beam Technology of Ministry of Education College of Nuclear Science and TechnologyBeijing Normal UniversityBeijing 100875China Key Laboratory of Beam Technology of Ministry of Education Institute of Radiation TechnologyBeijing Academy of Science and TechnologyBeijing 100875China

A correlation between the charge radii difference of mirror partner nucleiΔR_(ch) and the slope parameter L of symmetry energy has been built to ascertain the equation of state of isospin asymmetric nuclear *** this work,the influences of pairing correlations and isoscalar compression modulus on theΔRch are systematically investigated based on the Skyrme energy density functional *** calculated results suggest that the linear correlation betweenΔR_(ch) and L is decreased by the surface pairing *** slope parameter deduced from the difference of charge radii of mirror-pair nuclei ^(32)Ar-^(32)Si,^(36)Ca-^(36)S,^(38)Ca-^(38)Ar,and ^(54)Ni-^(54)Fe falls into the range of L=42.57−50.64 MeV,that is,the rather soft equation of state of asymmetric nuclear ***,the range of the slope parameter can also be influenced by the effective forces classified by various isoscalar incompressibility coefficients.

关键词： symmetry energy charge radius mirror-pair nuclei slope parameter

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High-density triple-phase contact points for enhanced photocatalytic CO_(2) reduction to methanol

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Chinese Chemical Letters 2024年第2期35卷 252-256页

作者： Hanwen Jian Kaiming Deng Tongyu Wang Chengxi Huang Fang Wu Hailing Huo Bo Ouyang Xuan Liu Jingjing Ma Erjun Kan Ang Li MIIT Key Laboratory of Semiconductor Microstructure and Quantum Sensing School of ScienceNanjing University of Science and TechnologyNanjing 210094China College of Information Science and Technology Nanjing Forestry UniversityNanjing 210037China State Key Laboratory of High-efficiency Utilization of Coal and Green Chemical Engineering Ningxia UniversityYinchuan 750021China

The efficiency of photocatalytic CO_(2) reduction reaction(PCRR)is restricted by the low solubility and mobility of CO_(2) in water,poor CO_(2) adsorption capacity of catalyst,and competition with hydrogen evolution reaction(HER).Recently,hydrophobic modification of the catalyst surface has been proposed as a potential solution to induce the formation of triple-phase contact points(TPCPs)of CO_(2)(gas phase),H_(2) O(liquid phase),and catalysts(solid phase)near the surface of the catalyst,enabling direct delivery of highly concentrated CO_(2) molecules to the active reaction sites,resulting in higher CO_(2) and lower H+surface *** TPCPs thus act as the ideal reaction points with enhanced PCRR and suppressed ***,the initial synthesis of triple-phase photocatalysts tends to possess a lower bulk density of TPCPs due to the simple structure leading to limited active points and CO_(2) adsorption ***,based on constructing a hydrophobic hierarchical porous TiO_(2)(o-HPT)with interconnected macropores and mesopores structure,we have significantly increased the density of TPCPs in a unit volume of the *** with hydrophobic macroporous TiO_(2)(o-MacPT)or mesoporous TiO_(2)(o-MesPT),the o-HPT with increased TPCP density leads to enhanced photoactivity,enabling a high methanol production rate with 1111.5μmol g^(−1) h^(−1) from *** results emphasize the significance of high-density TPCPs design and propose a potential path for developing efficient PCRR systems.

关键词： Photocatalysis CO_(2)reduction reaction Photocatalyst Triple-phase contact points Methanol

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All-dielectric terahertz metasurface governed by bound states in the continuum with high-Q factor

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The Journal of China universities of Posts and Telecommunications 2024年第2期31卷 44-54页

作者： Li Kun Zhao Xu Wang Meng Jia Xingning Zhao Ruiqi Lu Guizhen School of Integrated Circuit Science and Engineering Tianjin University of TechnologyTianjin 300384China School of Electronic and Electrical Engineering Ningxia UniversityYinchuan 750021China QILU Aerospace Information Research Institute Chinese Academy of Sciences(CAS)Jinan 250101China State Key Laboratory of Media Convergence and Communication Communication University of ChinaBeijing 100024China

The method of terahertz(THz)resonance with a high-quality(high-Q)factor offers a vital physical mechanism for metasurface sensors and other high-Q factor ***,it is challenging to excite the resonance with a high-Q factor in metasurfaces with proper sensitivity as well as figure of merit(FOM)***,an all-dielectric metasurface composed of two asymmetrical rectangular blocks is *** and silicon are the materials applied for the substrate and cuboids *** distinct resonance governed by bound states in the continuum(BIC)is excited by forming an asymmetric cluster by a novel hybrid method of cutting and moving the *** investigation focuses on analyzing the transmission spectra of the metasurface under different variations in structural parameters and the loss of silicon refractive *** the proposed defective metasurface serves as a transmittance sensor,it shows a Q factor of 1.08×10^(4)and achieves an FOM up to 4.8×10^(6),which is obtained under the asymmetric parameter equalling 1μ***,the proposed defective metasurface is sensitive to small changes in refractive *** the thickness of the analyte is 180μm,the sensitivity reaches a maximum value of 578 GHz/***,the proposed defective metasurface exhibits an extensive number of possible applications in the filters,biomedical diagnosis,security screening,and so on.

关键词： terahertz(THz)metasurface high-quality(high-Q)factor bound states in the continuum figure of merit(FOM)

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Discovery of a potent and highly selective inhibitor of SIRT6 against pancreatic cancer metastasis in vivo

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Acta Pharmaceutica Sinica B 2024年第3期14卷 1302-1316页

作者： Xinyuan Xu Qian Zhang Xufeng Wang Jing Jin Chengwei Wu Li Feng Xiuyan Yang Mingzhu Zhao Yingyi Chen Shaoyong Lu Zhen Zheng Xiaobing Lan Yi Wang Yan Zheng Xuefeng Lu Qiufen Zhang Jian Zhang State Key Laboratory of medical Genomics National Research Center for Translational Medicine at ShanghaiRuijin HospitalShanghai Jiao Tong University School of MedicineShanghai 200025China Medicinal Chemistry and BioinformaticsCenter Shanghai Jiao Tong University School of MedicineShanghai 200025China Department of General Surgery Huashan HospitalCancer Metastasis InstituteFudan UniversityShanghai 200040China Institute of Immunology and the CAS Key Laboratory of Innate Immunity and Chronic Disease School of Basic Medicine and Medical CenterUniversity of Science and Technology of ChinaHefei 230026China Department of Assisted Reproduction Shanghai Ninth People’s HospitalShanghai Jiao Tong University School of MedicineShanghai 200011China College of Pharmacy Ningxia Medical UniversityYinchuan 750004China Department of Pancreatic Surgery Shanghai General HospitalShanghai Key Laboratory of Pancreatic DiseaseInstitute of Pancreatic DiseaseShanghai Jiao Tong University School of MedicineShanghai 200080China

Pancreatic cancer,one of the most aggressive malignancies,has no effective treatment due to the lack of targets and drugs related to tumour ***6 can promote the migration of pancreatic cancer and could be a potential target for antimetastasis of pancreatic ***,highly selective and potency SIRT6 inhibitor that can be used in vivo is yet to be ***,we developed a noveSIRT6 allosteric inhibitor,compound 11e,with maximal inhibitory potency and an IC_(50) value of 0.98±0.13μmol/***,compound 11e exhibited significant selectivity against other histone deacetylases(HADC1-11 and SIRT1-3)at concentrations up to 100μmol/*** allosteric site and the molecular mechanism of inhibition were extensively elucidated by cocrystal complex structure and dynamic structural ***,we confirmed the antimetastatic function of such inhibitors in four pancreatic cancer cell lines as well as in two mouse models of pancreatic cancer liver *** our knowledge,this is the first study to reveal the in vivo effects of SIRT6 inhibitors on liver metastatic pancreatic *** not only provides a promising lead compound for subsequent inhibitor developmentargeting SIRT6 but also provides a potential approach to address the challenge of metastasis in pancreatic cancer.

关键词： SIRT6 Inhibitor Allosteric Selectivity Cocrystal Pancreatic cancer metastasis

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Relaxant Effects of Matrine on Aortic Smooth Muscles of Guinea Pigs

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Biomedical and Environmental Sciences 2009年第4期22卷 327-332页

作者： JIE ZHENG PING ZHENG XU ZHOU LIN YAN RU ZHOU XUE-YAN FU GUI-DONG DAI Department of Pharmacology School of Basic medical Science Department of Physiology School of Basic Medical Science ningxia Research Institute of Medicine & Pharmacy Ningxia Medical University Yinchuan 750004 Ningxia China

Objective To determine whether matrine, a kind of traditional Chinese medicinal alkaloid, can relax the aortic smooth muscles isolated from guinea pigs and to investigate the mechanism of its relaxant effects. Methods Phenylephrine or potassium chloride concentration-dependent relaxation response of aortic smooth muscles to matrine was studied in the precontracted guinea pigs. Results Matrine （1×10^-4 mol/L -3.3×10^-3 mol/L） relaxed the endothelium-denuded aortic rings pre-contracted sub-maximally with phenylephrine, in a concentration-dependent manner, and its pre-incubation （3.3× 10^- 3 mol/L） produced a significant rightward shift in the phenylephrine dose-response curve, but had no effects on the potassium chloride-induced contraction. The anti-contractile effect of matrine was not reduced by the highly selective ATP-dependent K^＋ channel blocker glibenclamide （10.5 mol/L）, either by the non-selective K^＋channel blocker tetraethylammonium （10^-3 mol/L）, or by the β-antagonist propranolol （10^-5 mol/L）. In either ＂normal＂ or ＂Ca^2＋-free＂ bathing medium, the phenylephrine-induced contraction was attenuated by matrine （3.3×10^-3 mol/L）, indicating that the vasorelaxation was due to inhibition of intracellular and extracellular Ca^2＋ mobilization. Conclusion Matrine inhibits phenylephrine-induced contractions by inhibiting activation of α-adrenoceptor and interfering with the release of intracellular Ca^2＋ and the influx of extracellular Ca^2＋.

关键词： Matrine Aorta Vascular smooth muscle Relaxation Guinea-pigs Calcium

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