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Insights into the structural biology of G-protein coupled receptors impacts drug design for central nervous system neurodegenerative processes

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Neural Regeneration Research 2013年第24期8卷 2290-2302页

作者： Farfán-García Eunice Dalet Trujillo-Ferrara José Guadalupe Castillo-Hernández María del Carmen Guerra-Araiza Christian Humberto soriano-ursúa marvin antonio Escuela Superior de Medicina Instituto Politécnico Nacional. Plan de San Luis y Díaz Mirón s/n Col. Casco de Santo Tomas

In the last few years, there have been important new insights into the structural biology of G-protein coupled receptors. It is now known that allosteric binding sites are involved in the affinity and selec- tivity of ligands for G-protein coupled receptors, and that signaling by these receptors involves both G-protein dependent and independent pathways. The present review outlines the physiological and pharmacological implications of this perspective for the design of new drugs to treat disorders of the central nervous system. Specifically, new possibilities are explored in relation to allosteric and or- thosteric binding sites on dopamine receptors for the treatment of Parkinson＇s disease, and on muscarinic receptors for Alzheimer＇s disease. Future research can seek to identify ligands that can bind to more than one site on the same receptor, or simultaneously bind to two receptors and form a dimer. For example, the design of bivalent drugs that can reach homo/hetero-dimers of D2 dopa- mine receptor holds promise as a relevant therapeutic strategy for Parkinson＇s disease. Regarding the treatment of Alzheimer＇s disease, the design of dualsteric ligands for mono-oligomeric mus- carinic receptors could increase therapeutic effectiveness by generating potent compounds that could activate more than one signaling pathway.

关键词： neural regeneration G-Protein coupled receptors structural biology drug design neurodegenera-tive disorders , oligomedzation biased signaling Parkinson's disease Alzheimer's disease dopa-mine receptors muscarinic receptors grants-supported paper neuroregeneration

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Polyphenols as potential enhancers of stem cell therapy against neurodegeneration

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Neural Regeneration Research 2022年第10期17卷 2093-2101页

作者： Diana Rodríguez-Vera antonio Abad-García Nancy Vargas-Mendoza Rodolfo Pinto-Almazán Eunice D.Farfán-García José A.Morales-González marvin A.soriano-ursúa Sección de Estudios de Posgrado e Investigación.Escuela Superior de Medicina Instituto Politécnico NacionalMéxico CityMéxico Unidad de Investigación Hospital Regional de Alta Especialidad IxtapalucaCarretera Federal México-Puebla km 34.5State of MéxicoMéxico

The potential of polyphenols for treating chronic-degenerative diseases(particularly neurodegenerative diseases)is ***,the selection of the best polyphenol for each treatment,the mechanisms by which they act,and their efficacy are frequently *** this review,the basics and the advances in the field,as well as suggestions for using natural and synthetic polyphenols alone or in a combinatorial strategy with stem cell assays,are compiled and ***,stem cells exhibit several responses when polyphenols are added to their environment,which could provide us with knowledge for advancing the elucidation of the origin of *** also,polyphenols are being included in the innovative strategies of novel therapies for treating neurodegenerative diseases as well as metabolic diseases related to *** this regard,flavonoid compounds are suggested as the best natural polyphenols due to their several mechanisms for acting in ameliorative effects;but increasing reports are involving other *** if some facts limiting bioactivity prevent them from conventional use,some natural polyphenols and derivatives hold the promise for being improved compounds,judged by their induced *** current results suggest polyphenols as enhancers of stem cell therapy against the targeted diseases.

关键词： Alzheimer’s disease chronic degenerative diseases combinatorial therapy metabolism neurodegenerative diseases neuronal damage neuroprotection Parkinson’s disease polyphenols stem cell assays

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Global longitudinal strain is superior to ejection fraction for detecting myocardial dysfunction in end-stage renal disease with hyperparathyroidism

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World Journal of Cardiology 2022年第4期14卷 239-249页

作者： Maria Fernanda Carrasco-Ruiz antonio Ruiz-Rivera marvin A soriano-ursúa Carlos Martinez-Hernandez Leticia Manuel-Apolinar Carmen Castillo-Hernandez Gustavo Guevara-Balcazar Eunice D Farfán-García Ana Mejia-Ruiz Ivan Rubio-Gayosso Teresa Perez-Capistran Department of Physiology Escuela Superior de MedicinaInstituto Politécnico NacionalCiudad de México 11340Mexico Department of Cardiology Instituto Mexicano del Seguro SocialCiudad de México 06720Mexico Endocrine Research Unit Instituto Mexicano del Seguro SocialCiudad de México 06720Mexico Department of Cardiovascular Pharmacology Instituto Politécnico NacionalCiudad de México 11340Mexico Department of Biochemistry Escuela Superior de MedicinaInstituto Politécnico NacionalCiudad de México 11340Mexico Education Research Comisión Nacional Para la Mejora Continua de la EducaciónCiudad de México 03900Mexico Postgraduate Studies and Research Section Escuela Superior de MedicinaInstituto Politécnico NacionalCiudad de México 11340Mexico Department of Physiology Instituto Politécnico NacionalMexico City 11340Ciudad de MéxicoMexico

BACKGROUND The estimation of left ventricular ejection fraction(LVEF)by 2D echocardiography(2D-ECHO)is the most used tool to assess LV systolic function(LVSF).Global longitudinal strain(GLS)has recently been suggested as a superior method for several *** study explored the association and prevalence of LV systolic dysfunction(LVSD)by using these methods in patients with end-stage renal disease(ESRD)and severe hyperparathyroidism(SHPTH);both associated with cardiovascular events(CEs).AIM To evaluate the myocardial function in patients with ESRD and SHPTH by using the GLS and LVEF measured through conventional *** In 62 patients with ESRD and SHPTH,asymptomatic,and without a history of CEs,LVSF was evaluated by 2D-ECHO,obtaining the EF,by the Simpson biplane method,and GLS by speckle *** The total patients with ESRD had a preserved LVEF(>50%)but abnormal GLS(<13.55%).Additionally,multivariate analysis showed an independent association of GLS and serum parathyroid hormone(PTH),LV mass index,and ***,PTH was independently associated with lateral e'wave and tricuspid regurgitation *** In patients with SHPTH linked to ESRD,the use of GLS by 2D-ECHO is a more sensitive tool than LVEF for detecting LVSD.

关键词： Left ventricular hypertrophy Systolic dysfunction Global longitudinal strain End-stage renal disease Parathormone

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Scope of translational medicine in developing boroncontaining compounds for therapeutics

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World Journal of Translational Medicine 2017年第1期6卷 1-9页

作者： Ana Karen García-ávila Eunice Dalet Farfán-García Juan Alberto Guevara-Salazar José Guadalupe Trujillo-Ferrara marvin antonio soriano-ursúa Department of Biochemistry and Section of Post Graduate Studies and Research Escuela Superior de MedicinaInstituto Politécnico Nacional Department of Physiology and Section of Post Graduate Studies and Research Escuela Superior de MedicinaInstituto Politécnico Nacional

The ubiquitousness of naturally occurring boron-containing compounds(BCCs) has led to their constant contact with ***,many synthetic BCCs have been elaborated for a broad spectrum of purposes,especially boric,boronic and borinic *** BCCs were once employed primarily as antiseptics and later as antibiotics,they have become an increasingly relevant therapeutic ***,this potential of BCCs has been drastically limited due to some unfortunate intra-hospital accidents in the 1940 s and 1950 *** increasing use of BCCs as insecticides,antimicrobials,and other agents is providing new insights into their role in the physiology of several living species and in the pathophysiology of *** is becoming clear that BCCs act through a wide range of mechanisms,as do their corresponding boron-free *** comparing BCCs and similar boron-free compounds,in many cases the former show advantages in the medical *** current minireview focuses on how BCCs have been developed by means of translational medicine,a process connecting biomedical research with clinical *** process of discovery is currently in an exponential stage.

关键词： Boron Boron-containing compounds Drug development Toxicity Medicinal chemistry Pharmacology

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Alternative uses of lumen apposing metal stents

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World Journal of Gastroenterology 2020年第21期26卷 2715-2728页

作者： Prabin Sharma Thomas R McCarty Ankit Chhoda antonio Costantino Caroline Loeser Thiruvengadam Muniraj marvin Ryou Christopher C Thompson Department of Gastroenterology and Hepatology Yale-New Haven Health-Bridgeport HospitalBridgeportCT 06610United States Division of Gastroenterology Hepatology and EndoscopyBrigham and Women’s HospitalHarvard Medical SchoolBostonMA 02115United States Department of Internal Medicine Yale-New Haven Health-Bridgeport HospitalBridgeportCT 06708United States Section of Digestive Diseases Yale University School of MedicineNew HavenCT 06520United States

The advent of lumen apposing metal stents(LAMS)has revolutionized the management of many complex gastroenterological conditions that previously required surgical or radiological *** procedures have garnered popularity due to their minimally invasive nature,higher technical and clinical success rate and lower rate of adverse *** virtue of their unique design,LAMS provide more efficient drainage,serve as conduit for endoscopic access,are associated with lower rates of leakage and are easy to be *** used for drainage of pancreatic fluid collections,the use of LAMS has been extended to gallbladder and biliary drainage,treatment of luminal strictures,creation of gastrointestinal fistulae,pancreaticobiliary drainage,improved access for surgically altered anatomy,and drainage of intra-abdominal and pelvic abscesses as well as post-surgical fluid *** new indications of endosonographic techniques and LAMS continue to evolve,this review summarizes the current role of LAMS in the management of these various complex conditions and also highlights clinical pearls to guide successful placement of LAMS.

关键词： Lumen apposing metal stents Walled off necrosis Gallbladder drainage Biliary drainage Gastric access temporary for endoscopy Gastric outlet obstruction Therapeutic endoscopy

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Endoscopic ultrasound fine needle aspiration vs fine needle biopsy in solid lesions:A multi-center analysis

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World Journal of Clinical Cases 2021年第34期9卷 10507-10517页

作者： Diogo Turiani Hourneaux Moura Thomas R McCarty Pichamol Jirapinyo Igor Braga Ribeiro Galileu Ferreira Ayala Farias antonio Coutinho Madruga-Neto marvin Ryou Christopher C Thompson Gastrointestinal Endoscopy Unit University of Sao Paulo School of MedicineSão PauloSP 05403-010Brazil Division of Gastroenterology Hepatology and EndoscopyBrigham and Women’s HospitalHarvard Medical SchoolBostonMA 02115United States Division of Gastrointestinal Endoscopy University of São Paulo Medical SchoolSão PauloSP 01246-903Brazil

BACKGROUND While endoscopic ultrasound(EUS)-guided fine needle aspiration(FNA)is considered a preferred technique for tissue sampling for solid lesions,fine needle biopsy(FNB)has recently been *** To compare the accuracy of FNB vs FNA in determining the diagnosis of solid *** A retrospective,multi-center study of EUS-guided tissue sampling using FNA vs FNB *** outcomes included diagnostic test characteristics(i.e.,sensitivity,specificity,accuracy),use of rapid on-site evaluation(ROSE),and adverse *** analyses were performed by type of lesion and diagnostic yield with or without ROSE.A multivariable logistic regression was also *** A total of 1168 patients with solid lesions(n=468 FNA;n=700 FNB)underwent EUS-guided *** age was 65.02±12.13 ***,sensitivity,specificity and accuracy were superior for FNB vs FNA(84.70%vs 74.53%;99.29%vs 96.62%;and 87.62%vs 81.55%,respectively;P0.05).Multivariate analysis showed no significant predictor for better *** subgroup analyses,FNB was superior to FNA for non-pancreatic lesions;however,there was no difference between the techniques among pancreatic *** adverse event was reported in each *** FNB is superior to FNA with equivalent diagnostic test characteristics compared to FNA+ROSE in the diagnosis of non-pancreatic solid *** results suggest that EUS-FNB may eliminate the need of ROSE and should be employed as a first-line method in the diagnosis of solid lesions.

关键词： Endoscopic ultrasound-guided tissue acquisition Fine needle aspiration Fine needle biopsy Solid lesions Endoscopic ultrasound Cancer

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