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Advances in Enzyme Research 2022年第4期10卷 83-100页

作者： Silvia Alejandra Meza-Ireta Blanca Colin-Lozano penélope merino-montiel José Luis Vega-Báez Sara montiel-Smith Facultad de Ciencias Químicas Ciudad Universitaria Benemérita Universidad Autónoma de Puebla Puebla México

Hormone Receptor positive (HR+) breast cancer is the most common malignancy in women. New strategies in the treatments have targeted the estrogen biosynthesis pathways including the inhibition of the aromatase and 17β-HSD1 enzymes. The present work, describes the study of a new family of 9 hybrid compounds derived from estrone attached to a coumarin fragment, linked through different lengths of hydrocarbon chains. The activity of these compounds was evaluated by molecular docking with two relevant enzymes in breast cancer (HR+). It has been proposed nine compounds as 17β-HSD1 inhibitors and six as aromatase inhibitors. We found important interactions with key amino acids at the orthosteric site of each enzyme and their score values compared to the crystallographic ligand. The in silico analysis showed good score values in the proposed compounds, where the steroidal portion presented important interactions with Met374 and Tyr155 in aromatase and in 17β-HSD1 respectively. Highlighting Compounds 2, 5 and 8 with an aromatic ring at the C4 position of the coumarin moiety, which favored arene-H type interactions essential for protein-ligand recognition. In addition, the results related to the 17β-HSD1 enzyme demonstrated how the length of the linker influences the interaction;the best score was found for derivative 8 with a chain of 8 methylenes.

关键词： Estrone Coumarins Aromatase Inhibitors 17β-HSD1 Inhibitors Molecular Docking

Steroidal Plant Growth Promoters vs. Phytopathogens, via Enzymatic Regulation;An in <i>Silico</i>Approach

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Advances in Enzyme Research 2021年第4期9卷 55-71页

作者： Alan Carrasco-Carballo Emiliano Marín-merino penélope merino-montiel Blanca Colin-Lozano Sandra Luz Cabrera Hilerio Jazmin Ciciolil Hilario-Martínez Jesús Sandoval-Ramírez Laboratorio de Elucidación y Síntesis en Química Orgánica Facultad de Ciencias Químicas Benemérita Universidad Autónoma de Puebla Puebla México Laboratorio de Síntesis y Modificación de Productos Naturales Facultad de Ciencias Químicas Benemérita Universidad Autónoma de Puebla Puebla México Laboratorio de Bromatología Facultad de Ciencias Químicas Benemérita Universidad Autónoma de Puebla Puebla México 4Facultad de Estudios Superiores-Zaragoza UNAM CDMX México Facultad de Estudios Superiores-Zaragoza UNAM CDMX México

Steroidal plant growth promoters (SPGP) have been continuously studied due to their high activity increasing biomass and resistance to diverse stress factors. In our hands, a new SPGP family of 22-oxocholestanic compounds stands out at a comparative level to brassinosteroids (BSs). The potential activity of new SPGP against phytopathogens was studied through in silico molecular docking, these assays were performed with relevant ensymes of phytopatogens Chitinase B and 1,3-β-Glucanase. Nine Chitinase B inhibitors and two 1,3-β-Glucanase inhibitors were proposed. The launched study analyzed the interactional and spatial level, determining the presence of interactions with key amino acids in receptors in comparison to reference inhibitors. Even more, the AVR4 and ECP6 effectors were also examined. No compound that blocks ECP6 was found;due to, probably, the influence of its highly hydrophilic environment. In the case of AVR4, two SPGP showed a better docking score (DS) than a chitin fragment (endogenous ligand);this fact demonstrates the latent potential of the 22-oxocholestanic derivatives against phytopathogens, with a specific regulation via proliferation inhibition. Moreover, this SPGP does not affect the symbiotic fungi that are beneficial for the natural plant system.

关键词： 22-Oxocholestanes Brassinosteroids Chitinase B 1 3-β-Glucanase ARV4 ECP6

Molecular Docking Studies of Estrone-Coumarin Derivatives as Aromatase and 17β -HSD1 Inhibitors Related to Hormone Receptor Positive (HR+) Breast Cancer

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Primary lateral sclerosis:more than just an upper motor neuron disease

Advances in Enzyme Research（酶研究进展） 2022年第4期

作者： Silvia Alejandra Meza-Ireta Blanca Colin-Lozano penélope merino-montiel JoséLuisVega-Báez Sara montiel-Smith

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Neural Regeneration Research 2024年第9期19卷 1881-1882页

作者： Ee Ling Tan Jasmin lope Peter Bede Computational Neuroimaging Group(CNG) School of MedicineTrinity College DublinIreland Department of Neurology St James’s HospitalDublinIreland

Advances in clinical care and recent research achievements:Primary lateral sclerosis(PLS)has traditionally been regarded as a pure upper motor neuron condition,a view perpetuated by most medical textbooks.

关键词： sclerosis clinical traditionally

Resveratrol as an inductor of autophagy: is there a unique pathway of activation?

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Neural Regeneration Research 2021年第1期16卷 101-103页

作者： Narayana Pineda-Ramírez penélope Aguilera Laboratorio de Patología Vascular Cerebral.Instituto Nacional de Neurología y Neurocirugía Manuel Velasco Suárez Ciudad de MéxicoMéxico

Autophagy is a process of cellular degradation for the removal of damaged components and eventual recycling of the resulting molecules that help to the maintenance of cellular *** this pathway,proteins with relatively long half-life and whole organelles(e.g.,mitochondria,peroxisomes,and ribosomes)are degraded in the cytoplasm for the continuous turnover of cellular structures to facilitate their ***,the beneficial effect of autophagy goes beyond cellular“cleaning”and resides to a large extent on its ability to recycle cell components back into the ***,autophagy is a fundamental mechanism to regulate cellular functions,including DNA repair,proliferation,differentiation,embryonic development,and the immune response.

关键词： homeostasis activation autophagy

Involvement of glucose transporter overexpression in the protection or damage after ischemic stroke

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Neural Regeneration Research 2022年第4期17卷 783-784页

作者： Iván Alquisiras-Burgos penélope Aguilera Laboratorio de Patología Vascular Cerebral Instituto Nacional de Neurología y Neurocirugía Manuel Velasco SuárezInsurgentes Sur#3877Col.La FamaTlalpanCiudad de MéxicoMéxico

Cerebral ischemia and resultant energy collapse:The ischemic stroke is a complex neurological condition that can be devastating for patients and their *** disease is the second leading cause of death worldwide and is characterized by a sudden decrease in cerebral blood flow due to major blood vessel *** stroke generates two damaged zones with distinctive metabolic *** first is the ischemic core,the region directly irrigated by the occluded artery.A reduction to less than 20%of the baseline blood flow levels defines the area;therefore,depletion of glucose and adenosine triphosphate(ATP)cause an irreversible failure in the energy metabolism that leads to loss of ionic homeostasis,acidosis,and *** second is the region surrounding the ischemic core,called the penumbra,characterized by significantly depressed tissue perfusion that is barely sufficient to support basal oxygen,glucose,and ATP levels.

关键词： metabolism damage homeostasis

The FRB-searching Pipeline of the Tianlai Cylinder Pathfinder Array

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Research in Astronomy and Astrophysics 2024年第8期24卷 113-132页

作者： Zijie Yu Furen Deng Shijie Sun Chenhui Niu Jixia Li Fengquan Wu Wei-Yang Wang Yougang Wang Shifan Zuo Lin Shu Jie Hao Xiaohui Liu Reza Ansari Ue-Li pen Albert Stebbins Peter Timbie Xuelei Chen National Astronomical Observatories Chinese Academy of SciencesBeijing 100101China University of Chinese Academy of Sciences Beijing 100049China Key Laboratory of Radio Astronomy and Technology Chinese Academy of ScienceBeijing 100101China Institute of Astrophysics Central China Normal UniversityWuhan 430079China Institute of Automation Chinese Academy of SciencesBeijing 100190China Guangdong Institute of Artificial Intelligence and Advanced Computing Guangzhou 510535China UniversitéParis-Saclay CNRS/IN2P3IJCLab91405 OrsayFrance Institute of Astronomy and Astrophysics Academia SinicaRoosevelt RoadTaipei 10617TaiwanChina Canadian Institute for Theoretical Astrophysics University of Toronto60 Saint George StreetTorontoON M5S 3H8Canada Department of Physics University of Wisconsin-MadisonMadisonWI 53706USA Fermi National Accelerator Laboratory P.O.Box 500Batavia IL 60510-5011USA Department of Physics College of SciencesNortheastern UniversityShenyang 110819China Center of High Energy Physics Peking UniversityBeijing 100871China

This paper presents the design,calibration,and survey strategy of the Fast Radio Burst(FRB)digital backend and its real-time data processing pipeline employed in the Tianlai Cylinder Pathfinder *** array,consisting of three parallel cylindrical reflectors and equipped with 96 dual-polarization feeds,is a radio interferometer array designed for conducting drift scans of the northern celestial *** FRB digital backend enables the formation of 96 digital beams,effectively covering an area of approximately 40 square degrees with the 3 dB *** pipeline demonstrates the capability to conduct an automatic search of FRBs,detecting at quasi-realtime and classifying FRB candidates *** current FRB searching pipeline has an overall recall rate of88%.During the commissioning phase,we successfully detected signals emitted by four well-known pulsars:PSR B0329+54,B2021+51,B0823+26,and B2020+*** report the first discovery of an FRB by our array,designated as FRB *** also investigate the optimal arrangement for the digitally formed beams to achieve maximum detection rate by numerical simulation.

关键词： instrumentation interferometers-methods data analysis-(stars )pulsars general-telescopes

财政风险补偿与知识产权质押融资——政策、机制与评估

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世界经济文汇 2024年第1期37卷 105-120页

作者：韩庆潇亓鹏中国人民银行山东省分行 250021 中国人民银行莱芜分行

本文通过构建包含金融摩擦的银企关系模型,分析了知识产权质押融资风险补偿机制的作用机理,并运用多期的双重差分模型验证了其作用效果。研究发现,高风险与轻资产的特征皆是科技型企业融资困境产生的重要原因,且前者的不利影响更加明显... 详细信息

本文通过构建包含金融摩擦的银企关系模型,分析了知识产权质押融资风险补偿机制的作用机理,并运用多期的双重差分模型验证了其作用效果。研究发现,高风险与轻资产的特征皆是科技型企业融资困境产生的重要原因,且前者的不利影响更加明显;风险补偿机制能够以财政资金分担部分风险,有效缓解科技型企业贷款高风险问题,从而显著提升了知识产权质押融资水平,表现为贷款规模和占比的明显增加;大中型银行以及企业创新水平较高地区具备开展知识产权质押融资业务的良好基础,因此进一步强化了风险补偿机制的作用效果。

关键词：知识产权质押融资风险补偿基金科技型企业

The short form of the SUR1 and its functional implications in the damaged brain

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Neural Regeneration Research 2022年第3期17卷 488-496页

作者： Iván Alquisiras-Burgos Javier Franco-Pérez Moisés Rubio-Osornio penélope Aguilera Laboratorio de Patología Vascular Cerebral Instituto Nacional de Neurología y Neurocirugía“Manuel Velasco Suárez”CDMXMexico Laboratorio de Formación Reticular Instituto Nacional de Neurología y Neurocirugía“Manuel Velasco Suárez”CDMXMexico Laboratorio Experimental de Enfermedades Neurodegenerativas Instituto Nacional de Neurología y Neurocirugía“Manuel Velasco Suárez”CDMXMexico.

Sulfonylurea receptor(SUR) belongs to the adenosine 5′-triphosphate(ATP)-binding cassette(ABC) transporter family;however,SUR is associated with ion channels and acts as a regulatory subunit determining the opening or closing of the ***8 and Abcc9 genes code for the proteins SUR1 and SUR2,*** SUR1 transcript encodes a protein of 1582 amino acids with a mass around 140–177 k Da expressed in the pancreas,brain,heart,and other *** is well known that SUR1 assembles with Kir6.2 and TRPM4 to establish K_(ATP) channels and non-selective cation channels,***8 and 9 are alternatively spliced,and the resulting transcripts encode different isoforms of SUR1 and SUR2,which have been detected by different experimental ***,the use of binding assays to sulfonylureas and Western blotting has allowed the detection of shorter forms of SUR(-65 k Da).Identity of the SUR1 variants has not been clarified,and some authors have suggested that the shorter forms are ***,immunoprecipitation assays have shown that SUR2 short forms are part of a functional channel even coexisting with the typical forms of the receptor in the *** evidence confirms that the structure of the short forms of the SURs is fully functional and does not lose the ability to interact with the *** structural changes in short forms of SUR modify its affinity to ATP,regulation of its expression might represent an advantage in pathologies where ATP concentrations decrease and a therapeutic target to induce ***,the expression of SUR1 variants might be induced by conditions associated to the decrease of energetic substrates in the brain(*** stroke and epilepsy).In this review,we want to contribute to the knowledge of SUR1 complexity by analyzing evidence that shows the existence of short SUR1 variants and its possible implications in brain function.

关键词： brain edema epilepsy Parkinson's disease stroke sulfonylurea receptor 1 SUR1 traumatic brain injury TRPM4

2024年全国笔类文具产品质量检验检测合格名单（第一季度）

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中国制笔 2024年第2期 66-69页

作者： National Light Industry Fountain pen Ballpoint pen Quality Supervision and Testing Center 全国轻工业自来水笔圆珠笔质量监督检测中心

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