Article
Infectious Diseases
Juan David Ramirez, Liyong Cao, Lissa Cruz-Saavedra, Carolina Hernandez, Sergio Castaneda, Marina Munoz, Nathalia Ballesteros, Radhika Banu, Paras Shrestha, Carlos Cordon-Cardo, Emilia Mia Sordillo, Alberto Paniz-Mondolfi
Summary: This study explores the feasibility of using epimastigotes to construct standard curves for quantifying parasitic loads in Chagas disease molecular diagnostics. The results indicate that there are no statistically significant differences in calculating parasitic loads in blood samples, regardless of the life stage used to construct the standard curves. This finding has practical implications for improving Chagas disease molecular diagnostic methods.
INTERNATIONAL JOURNAL OF INFECTIOUS DISEASES
(2022)
Article
Cardiac & Cardiovascular Systems
Maria Carmo P. Nunes, Lewis F. Buss, Jose Luiz P. Silva, Larissa Natany A. Martins, Claudia Di Lorenzo Oliveira, Clareci Silva Cardoso, Bruno Oliveira de Figueiredo Brito, Ariela Mota Ferreira, Lea Campos Oliveira, Ana Luiza Bierrenbach, Fabio Fernandes, Michael P. Busch, Viviane Tiemi Hotta, Luiz Mario Baptista Martinelli, Maria Carolina F. Almeida Soeiro, Adriana Brentegani, Vera M. C. Salemi, Marcia M. Menezes, Antonio Luiz P. Ribeiro, Ester Cerdeira Sabino
Summary: This study provides a comprehensive description of the natural history of T. cruzi seropositivity in a contemporary patient population, highlighting the central importance of anti-T. cruzi antibody titer as a marker of Chagas disease activity and risk of progression.
Article
Biochemistry & Molecular Biology
Naiara Dutra Barroso Gomes, Emanuel Paula Magalhaes, Lyanna Rodrigues Ribeiro, John Washington Cavalcante, Marcelo Morais Gomes Maia, Felipe Ramon Cunha da Silva, Arif Ali, Marcia Machado Marinho, Emmanuel Silva Marinho, Helcio Silva dos Santos, Alice Maria Costa Martins, Ramon Roseo Paula Pessoa Bezerra de Menezes
Summary: This study evaluated the activity of synthetic p-aminochalcones against T. cruzi and found that they have a trypanocidal effect by causing membrane damage and oxidative stress. Their mechanism of action may be related to inhibition of cruzain and TR.
BIOORGANIC CHEMISTRY
(2023)
Article
Chemistry, Physical
Aline Alves da Silva, Pedro Ivo da Silva Maia, Carla Duque Lopes, Sergio de Albuquerque, Marcelo Siqueira Valle
Summary: This study synthesized new thiosemicarbazones as potential drugs for Chagas disease, and found that one of the compounds exhibited better activity compared to the standard drug in experiments.
JOURNAL OF MOLECULAR STRUCTURE
(2021)
Article
Immunology
Melissa D. Klein, Freddy Tinajeros, Maria Del Carmen Menduina, Edith Malaga, Beth J. Condori, Manuela Verastegui, Federico Urquizu, Robert H. Gilman, Natalie M. Bowman
Summary: The study found that older maternal age, family history of Chagas disease, home conditions, lower educational level, and history of living in a rural area were significantly associated with higher odds of maternal infection. Protective factors against transmission included cesarean delivery and family history of Chagas disease, while twins were significantly more likely to be congenitally infected than singleton births.
CLINICAL INFECTIOUS DISEASES
(2021)
Article
Infectious Diseases
A. Abras, C. Ballart, A. Fernandez-Arevalo, T. Llovet, M. Gallego, C. Munoz
Summary: The study evaluated two algorithms for the diagnosis of chronic and congenital Chagas disease, with CMIA showing potential as a single diagnostic test in non-endemic countries and the revised algorithm with the >= 6 S/CO proving to be an efficient method for chronic CD diagnosis. For infants with congenital infection, CMIA could potentially be used as a single test for screening at 10 months or earlier, but further research is needed.
CLINICAL MICROBIOLOGY AND INFECTION
(2021)
Article
Microbiology
Jean-Yves Brossas, Ballering Griselda, Margarita Bisio, Jeremy Guihenneuc, Julian Ernesto Nicolas Gulin, Stephane Jaureguiberry, Francois-Xavier Lescure, Arnaud Fekkar, Dominique Mazier, Jaime Altcheh, Luc Paris
Summary: The study evaluated the effectiveness of the Chagas Western Blot IgG assay as a confirmatory serologic test, showing 100% sensitivity, specificity, positive predictive value, and negative predictive value. The method was found to be a simple and quick diagnostic tool for Chagas disease, with potential for use in large-scale studies.
Article
Microbiology
Sergio Castaneda, Marina Munoz, Peter J. Hotez, Maria Elena Bottazzi, Alberto E. Paniz-Mondolfi, Kathryn M. Jones, Rojelio Mejia, Cristina Poveda, Juan David Ramirez
Summary: Chagas disease is caused by Trypanosoma cruzi and has a profound impact on the gastrointestinal tract. Alterations in the gut microbiome caused by the parasite may play a crucial role in host-parasite interactions and immune responses. Understanding this interaction could provide valuable insights into the pathophysiology of the disease and the development of new treatments.
MICROBIOLOGY SPECTRUM
(2023)
Article
Immunology
Eva H. Clark, Carina Marquez, Jeffrey D. Whitman, Caryn Bern
Summary: Chagas disease can have dangerous consequences in people with HIV co-infection. This study provides practical recommendations to improve diagnosis and care for co-infected individuals, including incorporating Chagas disease screening into the initial evaluation for people with HIV. Screening for Chagas disease is important to identify infected individuals and provide timely treatment. Prompt evaluation and treatment should be considered for co-infected individuals with low CD4 cell counts and neurologic or cardiac symptoms.
CLINICAL INFECTIOUS DISEASES
(2022)
Article
Pharmacology & Pharmacy
Leonardo da Silva Lara, Guilherme Curty Lechuga, Lorraine Martins Rocha Orlando, Byanca Silva Ferreira, Bernardo Araujo Souto, Mauricio Silva dos Santos, Mirian Claudia de Souza Pereira
Summary: Chagas disease is a long-standing disease that primarily affects impoverished populations in Latin America. The available drugs have limited effectiveness and intense side effects. This study explores the biological activity of two new series of pyrazole-thiazoline derivatives with potential therapeutic options against Trypanosoma cruzi. These derivatives show potent activity with good oral bioavailability and low cytotoxicity, making them potential candidates for Chagas disease therapy.
Article
Public, Environmental & Occupational Health
Jorge Vasconez-Gonzalez, Juan S. Izquierdo-Condoy, Raul Fernandez-Naranjo, Esteban Gamez-Rivera, Andrea Tello-De-la-Torre, Galo S. Guerrero-Castillo, Carlos Ruiz-Sosa, Esteban Ortiz-Prado
Summary: Chagas disease is a neglected tropical disease caused by Trypanosoma cruzi, transmitted through contact with triatomine insect feces and urine. It infects approximately 6-7 million people worldwide, causing at least 14,000 deaths annually. In Ecuador, it has been reported in 20 out of 24 provinces, with El Oro, Guayas, and Loja being the most affected.
FRONTIERS IN PUBLIC HEALTH
(2023)
Article
Biochemistry & Molecular Biology
Gevanio Bezerra de Oliveira Filho, Marcos Verissimo de Oliveira Cardoso, Aline Caroline da Silva Santos, Thiago Andre Ramos dos Santos, Ana Catarina Cristovao-Silva, Laura Gonzalez Rubio, Luiz da Silva Maia Neto, Paulo Gaio Leite, Fabiana Simao Machado, Luiz Carlos Alves, Fabio Andre Brayner, Valeria Rego Alves Pereira, Ana Cristina Lima Leite
Summary: Chagas disease is causing more deaths in the Americas than any other parasitic disease and is increasingly becoming a global health problem. A novel series of 4-thiazolidinones derivatives have shown increased anti-T. cruzi activity, indicating potential for treating the disease.
CHEMICO-BIOLOGICAL INTERACTIONS
(2021)
Article
Microbiology
Isabela Ribeiro, Bethania Blum, Jayme Fernandes, Glaucia Santina, Makoto Asada, Michael Everson, Edgar Schuck, Ethel Feleder, Eric Evene, Virginie Gualano
Summary: The study evaluated the pharmacokinetics and safety interactions of BNZ and E1224 in healthy volunteers. The results showed changes in RVZ concentration parameters when both compounds were coadministered, but both compounds were well tolerated and no clinically relevant safety interactions were observed.
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY
(2021)
Article
Chemistry, Medicinal
Sheila Cruz Araujo, Rafaela Molina de Angelo, Henrique Barbosa, Thais Alves Costa-Silva, Andre Gustavo Tempone, Joao Henrique Ghilardi Lago, Kathia Maria Honorio
Summary: Chagas disease remains a major public health problem, particularly in Latin America and other endemic regions. Current drug treatments have limitations, and there is an urgent need for new therapeutic options. This study utilized virtual screening techniques to identify 11 potential inhibitors with significant activity against T. cruzi.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Medicine, General & Internal
Ana Carolina Oliveira, Amanda Roberta Revoredo Vicentino, Daniele Andrade, Isabela Resende Pereira, Leonardo Saboia-Vahia, Otacilio da Cruz Moreira, Carla Eponina Carvalho-Pinto, Julia Barbalho da Mota, Leonardo Maciel, Glaucia Vilar-Pereira, Joao B. Pesquero, Joseli Lannes-Vieira, Pierre Sirois, Antonio Carlos Campos de Carvalho, Julio Scharfstein
Summary: We investigated the role of B1R receptor in the development of Chagas disease caused by Trypanosoma cruzi. Our findings suggest that blocking the B1R receptor can reduce heart parasitism and cardiac injury in acute and chronic Chagas disease.
JOURNAL OF CLINICAL MEDICINE
(2023)
Article
Chemistry, Medicinal
Soledad Natalia Gonzalez, Jonathan J. Mills, Dante Maugeri, Christopher Olaya, Breana L. Laguera, Jeffrey R. Enders, Julian Sherman, Ana Rodriguez, Joshua G. Pierce, Juan Jose Cazzulo, Edward L. D'Antonio
Summary: The study discovered a competitive inhibitor Compound B targeting ribose 5-phosphate isomerase type B (RPI-B), which exhibited significant trypanocidal activity against T. cruzi infective life-stages. By targeting the active site residue Cys-69, this inhibitor provided a proof-of-concept for the development of next generation inhibitors with potential prodrug groups to treat Chagas' disease in the future.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2021)
Article
Biochemistry & Molecular Biology
Nieves Martinez-Peinado, Clara Martori, Nuria Cortes-Serra, Julian Sherman, Ana Rodriguez, Joaquim Gascon, Jordi Alberola, Maria-Jesus Pinazo, Alheli Rodriguez-Cortes, Julio Alonso-Padilla
Summary: The study found that 17-DMAG has a strong inhibitory effect on T. cruzi, particularly during the intracellular replicative stage of the parasite. Molecular docking results suggest that 17-DMAG may bind T. cruzi Hsp90 homologue Hsp83 with good affinity. However, evaluation in a mouse model of chronic T. cruzi infection did not show parasite growth inhibition, highlighting challenges in transitioning from in vitro assays to preclinical drug development stages.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Biochemistry & Molecular Biology
Sebastian Koehler, Michael Gargano, Nicolas Matentzoglu, Leigh C. Carmody, David Lewis-Smith, Nicole A. Vasilevsky, Daniel Danis, Ganna Balagura, Gareth Baynam, Amy M. Brower, Tiffany J. Callahan, Christopher G. Chute, Johanna L. Est, Peter D. Galer, Shiva Ganesan, Matthias Griese, Matthias Haimel, Julia Pazmandi, Marc Hanauer, Nomi L. Harris, Michael J. Hartnett, Maximilian Hastreiter, Fabian Hauck, Yongqun He, Tim Jeske, Hugh Kearney, Gerhard Kindle, Christoph Klein, Katrin Knoflach, Roland Krause, David Lagorce, Julie A. McMurry, Jillian A. Miller, Monica C. Munoz-Torres, Rebecca L. Peters, Christina K. Rapp, Ana M. Rath, Shahmir A. Rind, Avi Z. Rosenberg, Michael M. Segal, Markus G. Seidel, Damian Smedley, Tomer Talmy, Yarlalu Thomas, Samuel A. Wiafe, Julie Xian, Zafer Yueksel, Ingo Helbig, Christopher J. Mungall, Melissa A. Haendel, Peter N. Robinson
Summary: The Human Phenotype Ontology (HPO) serves as a global standard for phenotype exchange, with recent major extensions in neurology, nephrology, immunology, pulmonology, and other fields. Efforts have been made to improve computational definitions of phenotypic abnormalities across HPO and multiple phenotype ontologies for animal disease models, benefiting software accuracy and cross-species phenotype matching. Recent initiatives include translating HPO into indigenous languages and advancing its use in electronic health record systems.
NUCLEIC ACIDS RESEARCH
(2021)
Article
Microbiology
Nieves Martinez-Peinado, Nuria Cortes-Serra, Julian Sherman, Ana Rodriguez, Juan M. Bustamante, Joaquim Gascon, Maria-Jesus Pinazo, Julio Alonso-Padilla
Summary: Chagas disease, caused by the parasite Trypanosoma cruzi, has its greatest burden in Latin America. Existing treatments present toxicity and variable efficacy, highlighting the urgent need for new therapeutic strategies. Drug repositioning offers a fast and low-cost approach to identify safer and more effective chemotherapies for Chagas disease.
Correction
Genetics & Heredity
Antonio Atalaia, Rachel Thompson, Alberto Corvo, Leigh Carmody, Davide Piscia, Leslie Matalonga, Alfons Macaya, Angela Lochmuller, Bertrand Fontaine, Birte Zurek, Carles Hernandez-Ferrer, Carola Reinhard, David Gomez-Andres, Jean-Francois Desaphy, Katherine Schon, Katja Lohmann, Matthew J. Jennings, Matthis Synofzik, Olaf Riess, Rabah Ben Yaou, Teresinha Evangelista, Thiloka Ratnaike, Virginie Bros-Facer, Gulcin Gumus, Rita Horvath, Patrick Chinnery, Steven Laurie, Holm Graessner, Peter Robinson, Hanns Lochmuller, Sergi Beltran, Gisele Bonne
Summary: A correction to this paper has been published and is accessible through the original article.
ORPHANET JOURNAL OF RARE DISEASES
(2021)
Article
Genetics & Heredity
Daniel Danis, Julius O. B. Jacobsen, Leigh C. Carmody, Michael A. Gargano, Julie A. McMurry, Ayushi Hegde, Melissa A. Haendel, Giorgio Valentini, Damian Smedley, Peter N. Robinson
Summary: The SQUIRLS algorithm tackles the challenge of assessing candidate splice variants by calculating information content, evaluating changes in regulatory sequences, and training random-forest classifiers to achieve high accuracy. It provides tabular output files for integration into diagnostic pipelines and visualizations, showcasing superior accuracy in rank analysis.
AMERICAN JOURNAL OF HUMAN GENETICS
(2021)
Correction
Genetics & Heredity
Daniel Danis, Julius O. B. Jacobsen, Leigh C. Carmody, Michael A. Gargano, Julie A. McMurry, Ayushi Hegde, Melissa A. Haendel, Giorgio Valentini, Damian Smedley, Peter N. Robinson
AMERICAN JOURNAL OF HUMAN GENETICS
(2021)
Article
Genetics & Heredity
Peter Horak, Malachi Griffith, Arpad M. Danos, Beth A. Pitel, Subha Madhavan, Xuelu Liu, Cynthia Chow, Heather Williams, Leigh Carmody, Lisa Barrow-Laing, Damian Rieke, Simon Kreutzfeldt, Albrecht Stenzinger, David Tamborero, Manuela Benary, Padma Sheila Rajagopal, Cristiane M. Ida, Harry Lesmana, Laveniya Satgunaseelan, Jason D. Merker, Michael Y. Tolstorukov, Paulo Vidal Campregher, Jeremy L. Warner, Shruti Rao, Maya Natesan, Haolin Shen, Jeffrey Venstrom, Somak Roy, Kayoko Tao, Rashmi Kanagal-Shamanna, Xinjie Xu, Deborah Ritter, Kym Pagel, Kilannin Krysiak, Adrian Dubuc, Yassmine M. Akkari, Xuan Shirley Li, Jennifer Lee, Ian King, Gordana Raca, Alex H. Wagner, Marylin M. Li, Sharon E. Plon, Shashikant Kulkarni, Obi L. Griffith, Debyani Chakravarty, Dmitriy Sonkin
Summary: Professional societies have published guidelines for the clinical interpretation of somatic variants, but they lack a direct, systematic, and comprehensive set of standards and rules for classification. This leads to inconsistent classification and affects patient care, emphasizing the need for addressing this issue.
GENETICS IN MEDICINE
(2022)
Article
Medicine, General & Internal
Rachel R. Deer, Madeline A. Rock, Nicole Vasilevsky, Leigh Carmody, Halie Rando, Alfred J. Anzalone, Marc D. Basson, Tellen D. Bennett, Timothy Bergquist, Eilis A. Boudreau, Carolyn T. Bramante, James Brian Byrd, Tiffany J. Callahan, Lauren E. Chan, Haitao Chu, Christopher G. Chute, Ben D. Coleman, Hannah E. Davis, Joel Gagnier, Casey S. Greene, William B. Hillegass, Ramakanth Kavuluru, Wesley D. Kimble, Farrukh M. Koraishy, Sebastian Kohler, Chen Liang, Feifan Liu, Hongfang Liu, Vithal Madhira, Charisse R. Madlock-Brown, Nicolas Matentzoglu, Diego R. Mazzotti, Julie A. McMurry, Douglas S. McNair, Richard A. Moffitt, Teshamae S. Monteith, Ann M. Parker, Mallory A. Perry, Emily Pfaff, Justin T. Reese, Joel Saltz, Robert A. Schuff, Anthony E. Solomonides, Julian Solway, Heidi Spratt, Gary S. Stein, Anupam A. Sule, Umit Topaloglu, George D. Vavougios, Liwei Wang, Melissa A. Haendel, Peter N. Robinson
Article
Genetics & Heredity
Ferdinand Dhombres, Patricia Morgan, Bimal P. Chaudhari, Isabel Filges, Teresa N. Sparks, Pablo Lapunzina, Tony Roscioli, Umber Agarwal, Shagun Aggarwal, Claire Beneteau, Pilar Cacheiro, Leigh C. Carmody, Sophie Collardeau-Frachon, Esther A. Dempsey, Andreas Dufke, Michael Henri Duyzend, Mirna el Ghosh, Jessica L. Giordano, Ragnhild Glad, Ieva Grinfelde, Dominic G. Iliescu, Markus S. Ladewig, Monica C. Munoz-Torres, Marzia Pollazzon, Francesca Clementina Radio, Carlota Rodo, Raquel Gouveia Silva, Damian Smedley, Jagadish Chandrabose Sundaramurthi, Sabrina Toro, Irene Valenzuela, Nicole A. Vasilevsky, Ronald J. Wapner, Roni Zemet, Melissa A. Haendel, Peter N. Robinson
Summary: Technological advances in genome sequencing and prenatal imaging have improved our ability to recognize and diagnose Mendelian conditions prenatally. The Human Phenotype Ontology (HPO) has expanded its representation of prenatal phenotypes, supporting precision genetic diagnostics and prenatal care.
AMERICAN JOURNAL OF MEDICAL GENETICS PART C-SEMINARS IN MEDICAL GENETICS
(2022)
Correction
Genetics & Heredity
Peter Horak, Malachi Griffith, Arpad M. Danos, Beth A. Pitel, Subha Madhavan, Xuelu Liu, Cynthia Chow, Heather Williams, Leigh Carmody, Lisa Barrow-Laing, Damian Rieke, Simon Kreutzfeldt, Albrecht Stenzinger, David Tamborero, Manuela Benary, Padma Sheila Rajagopal, Cristiane M. Ida, Harry Lesmana, Laveniya Satgunaseelan, Jason D. Merker, Michael Y. Tolstorukov, Paulo Vidal Campregher, Jeremy L. Warner, Shruti Rao, Maya Natesan, Haolin Shen, Jeffrey Venstrom, Somak Roy, Kayoko Tao, Rashmi Kanagal-Shamanna, Xinjie Xu, Deborah I. Ritter, Kym Pagel, Kilannin Krysiak, Adrian Dubuc, Yassmine M. Akkari, Xuan Shirley Li, Jennifer Lee, Ian King, Gordana Raca, Alex H. Wagner, Marylin M. Li, Sharon E. Plon, Shashikant Kulkarni, Obi L. Griffith, Debyani Chakravarty, Dmitriy Sonkin
GENETICS IN MEDICINE
(2022)
Article
Multidisciplinary Sciences
Daniel Danis, Julius O. B. Jacobsen, Alex H. Wagner, Tudor Groza, Martha A. Beckwith, Lauren Rekerle, Leigh C. Carmody, Justin Reese, Harshad Hegde, Markus S. Ladewig, Berthold Seitz, Monica Munoz-Torres, Nomi L. Harris, Jordi Rambla, Michael Baudis, Christopher J. Mungall, Melissa A. Haendel, Peter N. Robinson
Summary: The Global Alliance for Genomics and Health is developing standards for sharing disease and phenotype information. The Phenopacket Schema is a flexible standard that can represent clinical data for various types of human diseases. It allows for additional constraints to ensure uniform data collection for specific goals.
Article
Medicine, Research & Experimental
Claudia Gomes, Rosauro Varo, Miquel Duran-Frigola, Antonio Sitoe, Rubio Bila, Sonia Machevo, Alfredo Mayor, Quique Bassat, Ana Rodriguez
Summary: Malaria can progress from an uncomplicated infection to a life-threatening severe disease. Early symptoms are often nonspecific, making it difficult to identify patients at high risk. By analyzing the transcriptomic response of human brain microvascular endothelial cells to Plasmodium falciparum-infected erythrocytes, several biomarkers have been identified to distinguish uncomplicated from severe malaria, as well as to differentiate children with cerebral malaria within the severe malaria group.
Article
Biochemical Research Methods
Guy Karlebach, Leigh Carmody, Jagadish Chandrabose Sundaramurthi, Elena Casiraghi, Peter Hansen, Justin Reese, Christopher J. Mungall, Giorgio Valentini, Peter N. Robinson
Summary: This article proposes a method called isoform interpretation to infer isoform-specific functions using expectation-maximization. It predicts specific functional annotations for 85,617 isoforms of 17,900 protein-coding genes and outperforms other methods in comparison to manually annotated results.
Article
Genetics & Heredity
Vida Ravanmehr, Hannah Blau, Luca Cappelletti, Tommaso Fontana, Leigh Carmody, Ben Coleman, Joshy George, Justin Reese, Marcin Joachimiak, Giovanni Bocci, Peter Hansen, Carol Bult, Jens Rueter, Elena Casiraghi, Giorgio Valentini, Christopher Mungall, Tudor Oprea, Peter N. Robinson
Summary: The research presents an approach based on natural language processing and machine learning to investigate the relations between protein kinases (PKs) and cancers, predicting the efficacy of inhibiting certain PKs to treat specific cancers. Results show that associations between PKs and specific cancers can be accurately predicted in advance, supporting the design of clinical trials for cancer therapy.
NAR GENOMICS AND BIOINFORMATICS
(2021)
Article
Chemistry, Medicinal
Shibin Zhao, Julian Maceren, Mia Chung, Samantha Stone, Raphael Geiben, Melissa L. Boby, Bradley S. Sherborne, Derek S. Tan
Summary: Antibiotic resistance is a major threat to public health, with Gram-negative bacteria presenting unique challenges due to their low permeability and efflux pumps. Limited understanding of the chemical rules for overcoming these barriers hinders antibacterial drug discovery. Efforts to address this issue, such as screening compound libraries and using cheminformatic analysis, have led to the design of sulfamidoadenosines with diverse substituents, showing potential utility in accumulation in Escherichia coli.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Jichun Li, Qing Li, Shuai Xia, Jiahuang Tu, Longbo Zheng, Qian Wang, Shibo Jiang, Chao Wang
Summary: This study successfully developed a short peptide mimetic as a MERS-CoV fusion inhibitor by reproducing the key recognition features of the HR2 helix. The resulting 23-mer lipopeptide showed comparable inhibitory effect to the 36-mer HR2 peptide HR2P-M2. This has important implications for developing short peptide-based antiviral agents to treat MERS-CoV infection.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Krista Jaunsleine, Linda Supe, Jana Spura, Sten van Beek, Anna Sandstrom, Jessica Olsen, Carina Halleskog, Tore Bengtsson, Ilga Mutule, Benjamin Pelcman
Summary: Beta(2)-adrenergic receptor agonists can stimulate glucose uptake by skeletal muscle cells and are therefore potential treatments for type 2 diabetes. The chirality of compounds has a significant impact on the activity of these agonists. This study found that certain synthesized compounds showed higher glucose uptake activity. These findings provide important information for the design of novel beta(2)AR agonists for T2D treatment.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Xin Xu, Jia Chen, Guan Wang, Xiaojuan Zhang, Qiang Li, Xiaobo Zhou, Fengying Guo, Min Li
Summary: The study focuses on EZH2, a promising therapeutic target for various types of cancers. Researchers designed and synthesized a series of novel derivatives aiming to enhance the EZH2 inhibition activity. Among them, compound 28 displayed potent EZH2 inhibition activity and showed high anti-proliferative effects in lymphoma cell lines and xenograft mouse models. The study suggests that compound 28 has potential as a therapeutic candidate for EZH2-associated cancers.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Wei Zhang, Wei Liu, Ya-Dong Zhao, Li-Zi Xing, Ji Xu, Rui-Jun Li, Yun-Xiao Zhang
Summary: This study developed a series of aromatic amide derivatives based on Rhein and investigated their inhibitory activity against alpha-Syn aggregation. Two of these compounds showed promising potential in treating Parkinson's disease by stabilizing alpha-Syn's conformation and disassembling alpha-Syn oligomers and fibrils.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Mani Sharma, S. S. S. S. Sudha Ambadipudi, Neeraj Kumar Chouhan, V. Lakshma Nayak, Srihari Pabbaraja, Sai Balaji Andugulapati, Ramakrishna Sistla
Summary: Therapeutically active lipids in drug delivery systems can enhance the safety and efficacy of treatment. The liposome formulation created using synthesized biologically active lipids showed additive anti-cancer effects and reduced tumorigenic potential.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
