Article
Chemistry, Medicinal
Yang Zheng, Magali van den Kerkhof, Tiffany van der Meer, Sheraz Gul, Maria Kuzikov, Bernhard Ellinger, Iwan J. P. de Esch, Marco Siderius, An Matheeussen, Louis Maes, Geert Jan Sterk, Guy Caljon, Rob Leurs
Summary: The discovery of 5-phenylpyrazolopyrimidinone analogs as a novel series of antitrypanosomal agents shows promise for developing new medications to treat Human African Trypanosomiasis (HAT). The most potent compound, 30, has a low toxicity potential and exhibits high in vitro and in vivo antitrypanosomal activity against T. b. brucei.
JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Medicinal
Karol R. Francisco, Ludovica Monti, Wenqian Yang, Hayoung Park, Lawrence J. Liu, Kaitlyn Watkins, Dilini K. Amarasinghe, Marianna Nalli, Carlos Roberto Polaquini, Luis O. Regasini, Antonio Eduardo Miller Crotti, Romano Silvestri, Lizandra Guidi Magalha, Conor R. Caffrey
Summary: Trypanosoma brucei is a parasitic protozoan that causes Human African Trypanosomiasis. A study evaluated the antitrypanosomal activity of curcuminoids and analogs against T. b. brucei and found that certain dibenzylideneacetone (DBA) compounds exhibited potent activity. Further research on DBA analogs identified compounds with low EC50 values and high selectivity indices. These findings suggest that DBAs could serve as a starting point for developing new small molecule therapies for HAT.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2023)
Article
Chemistry, Medicinal
Lorena Zara, Francesca Moraca, Jacqueline E. Van Muijlwijk-Koezen, Barbara Zarzycka, Robert Abel, Iwan J. P. de Esch
Summary: This study evaluated a method for predicting drug affinity in the treatment of African trypanosomiasis. The researchers found that this method accurately predicted the activity of different proteins and overcame challenges such as protein flexibility and sequence conservation. Therefore, this method holds promise for designing more selective inhibitors for African trypanosomes.
ACS MEDICINAL CHEMISTRY LETTERS
(2022)
Article
Biochemistry & Molecular Biology
Roberto Docampo, Anibal Eugenio Vercesi
Summary: This review discusses the mechanisms of mitochondrial oxidant generation and removal, and the involvement of Ca2+ in trypanosome cell death, highlighting the need for further studies on ROS generation, defense mechanisms, and mitochondrial permeability transition pore in trypanosomatids.
ANTIOXIDANTS & REDOX SIGNALING
(2022)
Editorial Material
Infectious Diseases
Abebaw Tiruneh, Endalew Zemene, Zeleke Mekonnen
Summary: Strongyloidiasis is the most neglected of the neglected tropical diseases in Ethiopia due to lack of clear category within the NTDs, underestimation of disease magnitude, and issues with the use of ivermectin for control and elimination. It is essential to use sensitive diagnostic tools and reliable evidence for the control and elimination programs of strongyloidiasis in Ethiopia.
INFECTIOUS DISEASES OF POVERTY
(2021)
Article
Multidisciplinary Sciences
Justin Y. Toh, Agathe Nkouawa, Saul Rojas Sanchez, Huafang Shi, Nikolay G. Kolev, Christian Tschudi
Summary: By targeting 86 transcripts through RNAi, 22 genes that positively or negatively regulate the progression towards infectivity in Trypanosoma brucei have been identified, including the previously unknown nucleic acid binding proteins CSD1 and CSD2. The study suggests a considerable overlap between the genes that regulate stumpy bloodstream form Trypanosoma and those that govern the development of metacyclic form parasites.
SCIENTIFIC REPORTS
(2021)
Review
Immunology
Nava Raj Poudyal, Kimberly S. Paul
Summary: This review discusses the availability and uptake mechanisms of fatty acids in Trypanosoma brucei. Fatty acids can be synthesized by the parasite or acquired from the host's surroundings. Fatty acids are crucial for the growth and survival of the parasite and are implicated in the survival of specific proteins. The relative contribution of parasite-derived and host-derived fatty acids to T. brucei biology and the molecular mechanisms of fatty acid uptake are still poorly understood.
FRONTIERS IN CELLULAR AND INFECTION MICROBIOLOGY
(2022)
Article
Immunology
Manon Geerts, Nick Van Reet, Sander Leyten, Raf Berghmans, Kat S. Rock, Theresa H. T. Coetzer, Lauren E-A Eyssen, Philippe Buscher
Summary: The newly developed T. b. gambiense inhibition ELISA (g-iELISA) based on the principle of antibody binding showed high specificity and sensitivity, making it suitable for regional laboratories in gHAT endemic countries for monitoring and surveillance.
CLINICAL INFECTIOUS DISEASES
(2021)
Review
Chemistry, Multidisciplinary
Garima Joshi, Sheikh Shahnawaz Quadir, Khushwant S. Yadav
Summary: Neglected tropical diseases, a set of 20 deadliest endemic diseases, affect nearly 1 billion people worldwide, mostly in developing countries, leading to poverty. These diseases present unique challenges for effective prevention and treatment methods. The use of nanocarriers in research and development is seen as a promising approach to fight infections by incorporating established drugs into them.
JOURNAL OF CONTROLLED RELEASE
(2021)
Article
Biochemical Research Methods
William Breslin, Doan Pham
Summary: Machine learning models are used to predict the biological activities related to certain diseases, aiming to address the lack of financial resources for drug development in developing countries.
BMC BIOINFORMATICS
(2023)
Review
Pharmacology & Pharmacy
Leonardo L. G. Ferreira, Josue de Moraes, Adriano D. Andricopulo
Summary: Neglected tropical diseases, such as leishmaniasis and schistosomiasis, continue to be a public health challenge in developing countries. However, advancements in drug discovery using modern strategies have shown promise in addressing these diseases by combining medicinal chemistry and parasite biology.
DRUG DISCOVERY TODAY
(2022)
Article
Microbiology
Joseph T. Smith Jr, Brianna Tylec, Arunasalam Naguleswaran, Isabel Roditi, Laurie K. Read
Summary: This study reveals the importance of mitochondrial mRNA editing in the developmental regulation of Trypanosoma brucei. The researchers found that temperature reduction and depletion of the differentiation-repressive kinase RDK1 can affect the metabolism of Trypanosoma brucei by altering the editing of mitochondrial cytochrome mRNAs.
Review
Cell Biology
Bibo Li
Summary: Telomeres and subtelomeres play crucial roles in maintaining chromosome stability and adapting to environmental changes, particularly in the case of the Trypanosoma brucei parasite. The similarities and differences in telomere factors between T. brucei, human, and yeast cells are important for understanding genome stability mechanisms.
FRONTIERS IN CELL AND DEVELOPMENTAL BIOLOGY
(2021)
Article
Microbiology
Emilia Jane McLaughlin, Karinna Rubio-Pena, Annick Dujeancourt-Henry, Lucy Glover
Summary: This study aimed to disrupt monoallelic VSG expression and found that the DNA sequence of the ectopic VSG is lost in a transcription-dependent manner following DSB-triggered VSG switching. The loss of the ectopic VSG does not disrupt the number or variety of templates used for BES DSB repair, revealing strict mechanisms within the cell to reinforce monoallelic expression during antigenic variation.
Review
Microbiology
Franciely G. Goncalves, Patricia S. Rosa, Andrea de F. F. Belone, Leia B. Carneiro, Vania L. Q. de Barros, Rosineide F. Bispo, Yally A. da S. Sbardelott, Sebastiao A. V. M. Neves, Amy Y. Vittor, William J. Woods, Gabriel Z. Laporta
Summary: Lobomycosis is a chronic disease endemic to the Amazon rainforest in Brazil, caused by Lacazia loboi. The lack of disease control program and therapeutic protocol has led to unknown disease prevalence and unmet needs of affected individuals. However, an effective therapy has been discovered through extensive research, opening new avenues for future studies. It is recommended that lobomycosis be reported as a disease to ensure accurate measurement of disease prevalence and provide free access to treatment for affected individuals.
Article
Chemistry, Medicinal
Dana M. Klug, Laura Tschiegg, Rosario Diaz, Domingo Rojas-Barros, Guiomar Perez-Moreno, Gloria Ceballos, Raquel Garcia-Hernandez, Maria Santos Martinez-Martinez, Pilar Manzano, Luis Miguel Ruiz, Conor R. Caffrey, Francisco Gamarro, Dolores Gonzalez Pacanowska, Lori Ferrins, Miguel Navarro, Michael P. Pollastri
JOURNAL OF MEDICINAL CHEMISTRY
(2020)
Article
Biochemistry & Molecular Biology
Maria Dichiara, Benedetto Amata, Rita Turnaturi, Agostino Marrazzo, Emanuele Amata
ACS CHEMICAL NEUROSCIENCE
(2020)
Article
Chemistry, Medicinal
Westley F. Tear, Seema Bag, Rosario Diaz-Gonzalez, Gloria Ceballos-Perez, Domingo I. Rojas-Barros, Carlos Cordon-Obras, Guiomar Perez-Moreno, Raquel Garcia-Hernandez, Maria Santos Martinez-Martinez, Luis Miguel Ruiz-Perez, Francisco Gamarro, Dolores Gonzalez Pacanowska, Conor R. Caffrey, Lori Ferrins, Pilar Manzano, Miguel Navarro, Michael P. Pollastri
JOURNAL OF MEDICINAL CHEMISTRY
(2020)
Article
Chemistry, Medicinal
Melissa J. Buskes, Monica Clements, Kelly A. Bachovchin, Hitesh B. Jalani, Allison Leonard, Seema Bag, Dana M. Klug, Baljinder Singh, Robert F. Campbell, Richard J. Sciotti, Nelly El-Sakkary, Conor R. Caffrey, Michael P. Pollastri, Lori Ferrins
ACS MEDICINAL CHEMISTRY LETTERS
(2020)
Article
Chemistry, Medicinal
Baljinder Singh, Jean A. Bernatchez, Laura-Isobel McCall, Claudia M. Calvet, Jasmin Ackermann, Julia M. Souza, Diane Thomas, Everton M. Silva, Kelly A. Bachovchin, Dana M. Klug, Hitesh B. Jalani, Seema Bag, Melissa J. Buskes, Susan E. Leed, Norma E. Roncal, Erica C. Penn, Jessey Erath, Ana Rodriguez, Richard J. Sciotti, Robert F. Campbell, James McKerrow, Jair L. Siqueira-Neto, Lori Ferrins, Michael P. Pollastri
ACS MEDICINAL CHEMISTRY LETTERS
(2020)
Article
Biochemistry & Molecular Biology
Rita Turnaturi, Lorella Pasquinucci, Santina Chiechio, Margherita Grasso, Agostino Marrazzo, Emanuele Amata, Maria Dichiara, Orazio Prezzavento, Carmela Parenti
ACS CHEMICAL NEUROSCIENCE
(2020)
Article
Chemistry, Medicinal
Emanuele Amata, Maria Dichiara, Davide Gentile, Agostino Marrazzo, Rita Turnaturi, Emanuela Arena, Alfonsina La Mantia, Barbara Rita Tomasello, Rosaria Acquaviva, Claudia Di Giacomo, Antonio Rescifina, Orazio Prezzavento
ACS MEDICINAL CHEMISTRY LETTERS
(2020)
Article
Biophysics
Agostino Marrazzo, Cristina Torrisi, Carla Barbaraci, Emanuele Amata, Francesco Castelli, Maria Grazia Sarpietro
Summary: The compounds (+)-MR200 and (-)-MRV3 are selective cs1 antagonists with analgesic effects, playing a role in central sensitization and pain hypersensitivity, suggesting their potential use for treating persistent pain conditions. The study also assessed their membrane absorption ability by studying their interactions with DMPC using DSC and LB methods.
COLLOIDS AND SURFACES B-BIOINTERFACES
(2021)
Article
Chemistry, Medicinal
Antonino Nicolo Fallica, Carla Barbaraci, Emanuele Amata, Lorella Pasquinucci, Rita Turnaturi, Maria Dichiara, Sebastiano Intagliata, Marzia Bruna Gariboldi, Emanuela Marras, Viviana Teresa Orlandi, Claudia Ferroni, Cecilia Martini, Antonio Rescifina, Davide Gentile, Greta Varchi, Agostino Marrazzo
Summary: The potential anticancer effect of fluoroquinolone antibiotics has been revealed, especially in triple-negative and doxorubicin-resistant breast cancer cells. In addition, some fluoroquinolone nitric oxide hybrids showed significant antimicrobial effects, particularly against Staphylococcus aureus, when released upon light irradiation.
JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Medicinal
Carla Barbaraci, Giovanni Giurdanella, Claudia Giovanna Leotta, Anna Longo, Emanuele Amata, Maria Dichiara, Lorella Pasquinucci, Rita Turnaturi, Orazio Prezzavento, Ivana Cacciatore, Elisa Zuccarello, Gabriella Lupo, Giovanni Mario Pitari, Carmelina Daniela Anfuso, Agostino Marrazzo
Summary: The drug (S)-(-)-MRJF22 shows promising antiangiogenic and antimigratory effects, making it a potential candidate for novel antimetastatic therapy in patients with uveal melanoma.
JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Correction
Chemistry, Medicinal
Antonino Nicoloo Fallica, Carla Barbaraci, Emanuele Amata, Lorella Pasquinucci, Rita Turnaturi, Maria Dichiara, Sebastiano Intagliata, Marzia Bruna Gariboldi, Emanuela Marras, Viviana Teresa Orlandi, Claudia Ferroni, Cecilia Martini, Antonio Rescifina, Davide Gentile, Greta Varchi, Agostino Marrazzo
JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Rita Turnaturi, Santina Chiechio, Lorella Pasquinucci, Salvatore Spoto, Giuliana Costanzo, Maria Dichiara, Silvia Piana, Margherita Grasso, Emanuele Amata, Agostino Marrazzo, Carmela Parenti
Summary: Although opioids and NSAIDs have many side effects, the development of new analgesics and the investigation of new mechanisms provide promising alternatives for persistent pain treatment.
Editorial Material
Chemistry, Medicinal
Maria Dichiara, Emanuele Amata
Summary: Integrating efforts from pharmacologists and biologists into sustained innovation from synthetic chemists is crucial for the progress of H2S research and the development of H2S therapeutics for clinical use.
FUTURE MEDICINAL CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Giuseppe Romeo, Valeria Ciaffaglione, Emanuele Amata, Maria Dichiara, Loredana Calabrese, Luca Vanella, Valeria Sorrenti, Salvo Grosso, Agata Grazia D'Amico, Velia D'Agata, Sebastiano Intagliata, Loredana Salerno
Summary: Targeting both HO-1 and sigma R proteins simultaneously may provide an effective strategy for treating prostate and brain cancers, leading to increased antiproliferative activity. By synthesizing novel hybrid compounds, further optimization of structure can be achieved to develop more potent anticancer agents.
Correction
Chemistry, Medicinal
Antonino Nicoloo Fallica, Carla Barbaraci, Emanuele Amata, Lorella Pasquinucci, Rita Turnaturi, Maria Dichiara, Sebastiano Intagliata, Marzia Bruna Gariboldi, Emanuela Marras, Viviana Teresa Orlandi, Claudia Ferroni, Cecilia Martini, Antonio Rescifina, Davide Gentile, Greta Varchi, Agostino Marrazzo
JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Chemistry, Organic
Geeta Devi Yadav, Pooja Chaudhary, Balaram Pani, Surendra Singh
Summary: Chiral transition metal complexes with privileged ligands are efficient catalysts for various asymmetric organic transformations. Transition metal complexes of C1-symmetric pyrrolidine-based ligands have been widely used in asymmetric organic reactions. However, a comprehensive review article on the transition metal complexes of chiral C1-symmetric pyrrolidine-based ligands derived from (L)-proline has not been published.
TETRAHEDRON LETTERS
(2024)
