Article
Chemistry, Medicinal
Xinnan Li, Xiaotong Ze, Shengnan Zhou, Zhaoxin Hu, Chen He, Yilin Jia, Lihua Liu, Tao Wang, Junda Li, Shengtao Xu, Dong-Hua Yang, Zhe-Sheng Chen, Hequan Yao, Jinyi Xu, Hong Yao
Summary: A novel compound D26, identified through the exploration and optimization of the first-in-class POLRMT inhibitor IMT1B, exhibits a strong antiproliferative effect on cancer cells and decreases mitochondrial-related gene expression. Mechanism studies revealed that D26 arrests the cell cycle at the G1 phase without affecting apoptosis, mitochondrial depolarization, or reactive oxidative stress generation. In vivo studies further demonstrated that D26 has more potent anticancer activity than the lead compound IMT1B, and no toxicity was observed.
JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Medicinal
Yuanyuan Wang, Hao Ma, Jiaxuan Huang, Zhengguang Yao, Jianqiang Yu, Wannian Zhang, Lichao Zhang, Zhibin Wang, Chunlin Zhuang
Summary: A Necroptosis inhibitor, compound 20, was found to effectively protect against programmed cell death and synergize with other inhibitors, providing a lead compound for researching I/R treatment.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Pharmacology & Pharmacy
Shun Zhang, Yan Zhao, Shuyuan Wang, Min Li, Yue Xu, Jianhua Ran, Xiaoqiang Geng, Jinzhao He, Jia Meng, Guangying Shao, Hong Zhou, Zemei Ge, Guangping Chen, Runtao Li, Baoxue Yang
Summary: A novel UT inhibitor was discovered in this study, showing excellent in vitro UT inhibitory activity and potential for treating hyponatremia accompanied with volume expansion without causing apparent toxicity or electrolyte imbalance.
ACTA PHARMACEUTICA SINICA B
(2021)
Article
Chemistry, Medicinal
Pooja V. D. Hegde, Michael D. Howe, Matthew Zimmerman, Helena L. M. Boshoff, Sachin Sharma, Brianna Remache, Ziyi D. Jia, Yan Pan, Anthony C. Baughn, Veronique Dartois, Courtney Aldrich
Summary: Tuberculosis is a deadly infectious disease with limited treatment options. Researchers have developed prodrugs and modified the structure of para-Aminosalicylic acid (PAS) to improve its oral bioavailability and reduce rapid clearance. These innovations have the potential to enhance the therapeutic effectiveness of PAS.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Chemistry, Medicinal
Daisuke Iijima, Hiroshi Sugama, Yoichi Takahashi, Miki Hirai, Yuko Togashi, Jianshu Xie, Jingkang Shen, Ying Ke, Hidenori Akatsuka, Takayuki Kawaguchi, Kei Takedomi, Akiko Kashima, Masashi Nishio, Yosuke Inui, Hikaru Yoneda, Guangxin Xia, Toru Iijima
Summary: Renin inhibitors have been a challenge for the treatment of hypertension and cardiovascular/renal diseases, but researchers have discovered a new compound, 18 (SPH3127), with favorable bioavailability and antihypertensive effects.
JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Willem F. J. Karstens, Wiro M. B. P. Menge, Gijs Martens, Sanne J. N. Op Het Veld, Jacobus Th. H. van Eupen, Marco Demon, Tanja A. E. van Achterberg, Monica J. Arisse-Thijssen, Ellen W. H. Santegoeds-Lenssen, Miranda M. C. van der Lee, Ruud Ubink, Roel J. Arends, Aloys Sesink, Marion Blomenrohr, C. Marco Timmers
Summary: This paper describes the discovery of a novel small molecule TSH-R antagonist, SYD5115 (67), with nanomolar potency. SYD5115 also blocks the synthesis of thyroid hormone T4 induced by stimulating antibodies after a single oral dose. During optimization, issues such as low metabolic stability and potential mutagenicity of the initial compounds had to be addressed.
BIOORGANIC & MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Medicinal
Heecheol Kim, Minjung Kim, Kyujin Oh, Sohee Lee, Sunyoung Lim, Sangdon Lee, Young Hoon Kim, Kwee Hyun Suh, Kyung Hoon Min
Summary: G-protein-coupled receptor 119 (GPR119) shows great potential as a targeted therapy for type II diabetes. Thieno[3,2-d]pyrimidine derivatives were discovered as potent GPR119 agonists through a bioisosteric replacement strategy, with the sulfonylphenyl thieno[3,2-d]pyrimidine scaffold being introduced. The representative derivative 43 exhibited excellent pharmacokinetic profiles in rodents and significantly improved glucose tolerance in vivo, lowering blood glucose levels in both mice and rats in OGTT study.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Editorial Material
Biology
Sacha Bourgeois-Gironde, Elsa Addessi, Thomas Boraud
Summary: The paper examines whether non-human primates exhibit economic behavior by evaluating various studies on individual cognitive abilities, collective organization, and comparison across species. It considers the emergence of economic organizations among groups of non-human primates, cognitive abilities linked to economic decision-making, performance comparisons across species, and the need to improve models for ecological data. Overall, the reviewed articles provide positive answers and perspectives supporting the existence of economic behaviors among non-human primates.
PHILOSOPHICAL TRANSACTIONS OF THE ROYAL SOCIETY B-BIOLOGICAL SCIENCES
(2021)
Article
Behavioral Sciences
Davide Bono, Michel Belyk, Matthew R. Longo, Frederic Dick
Summary: The phrase "on the tip of my tongue" accurately describes the sensorimotor functions of the tongue, which are essential for speech and other behaviors but often overlooked in scientific research. This review summarizes a wide range of studies conducted on non-primates, non-human primates, and human primates to provide a comprehensive description of the cortical representation of the tongue's somatosensory inputs and motor outputs across different phylogenetic domains.
NEUROSCIENCE AND BIOBEHAVIORAL REVIEWS
(2022)
Article
Biochemistry & Molecular Biology
Yuanyuan Du, Zhen Liang, Shusen Wang, Dong Sun, Xiaofeng Wang, Soon Yi Liew, Shuaiyao Lu, Shuangshuang Wu, Yong Jiang, Yaqi Wang, Boya Zhang, Wenhai Yu, Zhi Lu, Yue Pu, Yun Zhang, Haiting Long, Shanshan Xiao, Rui Liang, Zhengyuan Zhang, Jingyang Guan, Jinlin Wang, Huixia Ren, Yanling Wei, Jiaxu Zhao, Shicheng Sun, Tengli Liu, Gaofan Meng, Le Wang, Jiabin Gu, Tao Wang, Yinan Liu, Cheng Li, Chao Tang, Zhongyang Shen, Xiaozhong Peng, Hongkui Deng
Summary: In this study, human chemically induced pluripotent stem cell-derived islets (hCiPSC-islets) were used to treat diabetes in non-human primates. The results showed that a one-dose infusion of hCiPSC-islets effectively restored insulin secretion and improved glycemic control. This study demonstrates the feasibility of hCiPSC-islets for diabetic treatment in a preclinical context.
Article
Pharmacology & Pharmacy
Wei Cong, Huaxing Shen, Xiufei Liao, Mengjun Zheng, Xianglong Kong, Zhe Wang, Si Chen, Yulei Li, Honggang Hu, Xiang Li
Summary: Stapled peptides with enhanced pharmacological profiles have potential as therapeutic molecules due to their resistance to proteolysis and ability to enter cells. In this study, a double-stapled peptide FRNC-1 effectively inhibited the bone resorption capacity of mature osteoclasts in vitro through specific inhibition of phosphorylated GSK-3b. FRNC-1 displayed improved helical contents and resistance to proteolysis compared to its linear form. Additionally, FRNC-1 effectively prevented osteoclast activation and improved bone density for ovariectomized mice after intravenous and oral administration.
ACTA PHARMACEUTICA SINICA B
(2023)
Article
Clinical Neurology
Julia Chocarro, Alberto J. Rico, Goiaz Ariznabarreta, Elvira Roda, Adriana Honrubia, Maria Collantes, Ivan Penuelas, Alfonso Vazquez, Ana Rodriguez-Perez, Jose L. Labandeira-Garcia, Miquel Vila, Jose L. Lanciego
Summary: By triggering a time-dependent accumulation of neuromelanin within dopaminergic neurons in macaques, researchers have successfully developed and characterized an animal model of Parkinson's disease that mimics the known neuropathology of the disorder with unprecedented accuracy. They have also demonstrated that intracellular aggregation of endogenous alpha-synuclein is triggered by neuromelanin accumulation, suggesting that reducing neuromelanin levels may be a promising approach for novel PD therapeutics.
Article
Neurosciences
P. Christiaan Klink, Jean-Francois Aubry, Vincent P. Ferrera, Andrew S. Fox, Sean Froudist-Walsh, Bechir Jarraya, Elisa E. Konofagou, Richard J. Krauzlis, Adam Messinger, Anna S. Mitchell, Michael Ortiz-Rios, Hiroyuki Oya, Angela C. Roberts, Anna Wang Roe, Matthew F. S. Rushworth, Jerome Sallet, Michael Christoph Schmid, Charles E. Schroeder, Jordy Tasserie, Doris Y. Tsao, Lynn Uhrig, Wim Vanduffel, Melanie Wilke, Igor Kagan, Christopher Petkov
Summary: Brain perturbation studies focus on non-invasive methods, with non-human primates serving as a research model for neurobiological systems and providing various perturbation methods. These methods can be combined with neuroimaging to facilitate research in the field.
Article
Ophthalmology
Xu Jia, Ziyu Yu, Jian Wu, Simeng Hou, Yifan Du, Yingting Zhu, Zhidong Li, Shu Tu, Ling Zhao, Wenru Su, Ningli Wang, Yehong Zhuo
Summary: This study aimed to assess the longitudinal changes in retinal nerve fiber layer thickness and relative optic nerve head parameters in non-human primates with spontaneous glaucoma. The results showed that glaucomatous eyes had decreased retinal nerve fiber layer thickness and phase retardation, with the most significant decrease observed in the whole retinal area and temporal region. Additionally, there were significant differences in lamina cribrosa parameters between glaucoma primates and normal primates.
OPHTHALMIC RESEARCH
(2023)
Review
Cell & Tissue Engineering
Tomonori Nakamura, Kohei Fujiwara, Mitinori Saitou, Tomoyuki Tsukiyama
Summary: Human development has been studied for over a century, with mice commonly used as a model due to technical difficulties and ethical issues surrounding human embryogenesis. However, species-specific differences between rodents and primates have become more apparent, leading to an increased focus on Non-human primates (NHPs) as models for human development. Research on gene modification technology for NHPs and studies on early embryogenesis in primates are progressing, shaping future perspectives in the field.
Article
Veterinary Sciences
D. E. Kelley, C. L. Hodo, A. Aceino, S. D. Lawhon, K. Hinrichs, S. P. Brinsko
Summary: A 16-year-old Westphalian mare aborted a dead fetus at 7 months of gestation, showing diffusely thickened chorioallantois with Bacillus safensis isolated from the fetal lungs and mare's uterus. This is the first case of equine abortion associated with B. safensis infection.
EQUINE VETERINARY EDUCATION
(2021)
Article
Parasitology
Italo B. Zecca, Carolyn L. Hodo, Sarah Slack, Lisa Auckland, Sandy Rodgers, Keswick C. Killets, Ashley B. Saunders, Sarah A. Hamer
VETERINARY PARASITOLOGY
(2020)
Article
Veterinary Sciences
Italo B. Zecca, Carolyn L. Hodo, Hilary M. Swarts, Thomas W. DeMaar, Karen F. Snowden, Heather L. Prestridge, Jessica E. Light, Sarah A. Hamer
Summary: The federally endangered ocelot population in south Texas, USA is declining, with one third of the sampled ocelots showing evidence of Trypanosoma cruzi infection or exposure. Some infected ocelots exhibited cardiac lesions, indicating a significant impact of this parasite on vulnerable populations.
JOURNAL OF WILDLIFE DISEASES
(2021)
Article
Infectious Diseases
Rachel E. Busselman, Alyssa C. Meyers, Italo B. Zecca, Lisa D. Auckland, Andres H. Castro, Rebecca E. Dowd, Rachel Curtis-Robles, Carolyn L. Hodo, Ashley B. Saunders, Sarah A. Hamer
Summary: The study monitored a cohort of 64 dogs in kennels in Texas, USA, and found a high risk of Chagas disease infection among dogs, particularly in areas where triatomine vectors are present. The research indicated that there is a 30.7% risk for dogs to acquire T. cruzi infection within one year.
PLOS NEGLECTED TROPICAL DISEASES
(2021)
Article
Genetics & Heredity
Nejla Ozirmak Lermi, Stanton B. Gray, Charles M. Bowen, Laura Reyes-Uribe, Beth K. Dray, Nan Deng, R. Alan Harris, Muthuswamy Raveendran, Fernando Benavides, Carolyn L. Hodo, Melissa W. Taggart, Karen Colbert Maresso, Krishna M. Sinha, Jeffrey Rogers, Eduardo Vilar
Summary: The study focused on Lynch Syndrome (LS), a genetic condition that increases the risk of developing colorectal cancer, and analyzed a non-human primate (NHP) model for studying hereditary colorectal cancer. By comparing different types of CRC in humans with tumors developed in monkeys, the study aimed to determine the accuracy of using this NHP model for studying early cancer development, treatment options, and prevention approaches in both hereditary and sporadic colorectal cancer.
Article
Infectious Diseases
Juan M. Bustamante, Angel M. Padilla, Brooke White, Lisa D. Auckland, Rachel E. Busselman, Stephanie Collins, Elizabeth L. Malcolm, Briana F. Wilson, Ashley B. Saunders, Sarah A. Hamer, Rick L. Tarleton
Summary: The trypanocidal compound benznidazole (BNZ) was tested for its ability to prevent new infections in dogs. The study found that the current prophylaxis regimen did not impact the incidence of new infections. Further research is needed to determine if a more rigorous and potent dosing regimen can achieve immediate benefits of prophylaxis.
PLOS NEGLECTED TROPICAL DISEASES
(2022)
Article
Immunology
Molly E. Bunkofske, Natasha Perumal, Brooke White, Eva-Maria Strauch, Rick Tarleton
Summary: Infection with Trypanosoma cruzi induces CD8+ T cell responses targeting epitopes in the large trans-sialidase (TS) gene family, but these responses are not essential for immune control. A screen for alternative CD8+ T cell targets identified a previously uncharacterized epitope, MUCKb25, within mucin family proteins. However, the MUCKb25-specific response was dispensable for infection control and vaccination to generate MUCK-specific CD8+ T cells failed to confer protection. These findings highlight the limited effector potential of CD8+ T cells in T. cruzi-infected mice. Journal of Immunology, 2023, 210: 420-430.
JOURNAL OF IMMUNOLOGY
(2023)
Article
Parasitology
Jessica Y. Rodriguez, Kevin J. Cummings, Carolyn L. Hodo, Sarah A. Hamer
Summary: The prevalence of intestinal parasites among Texas shelter dogs was estimated using centrifugal fecal flotation and saline sedimentation techniques. Risk factors for infection were identified, and the addition of fecal sedimentation increased the number of parasite species detected and the number of dogs diagnosed with common intestinal parasites. Texas shelter dogs carry a high burden of intestinal parasites, including those of zoonotic importance.
PARASITOLOGY RESEARCH
(2023)
Article
Microbiology
Juan M. Bustamante, Brooke E. White, Gregory K. Wilkerson, Carolyn L. Hodo, Lisa D. Auckland, Wei Wang, Stephanie McCain, Sarah A. Hamer, Ashley B. Saunders, Rick L. Tarleton
Summary: This study demonstrates that higher dose, intermittent administration of benznidazole can effectively treat Trypanosoma cruzi infection. Administration twice a week, for more than 4 months, provides the best chance for parasitological cure.
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY
(2023)
Article
Pathology
Gayathriy Balamayooran, Eric Snook, Maryanne Tocidlowski, Joe Flanagan, Will Sims, Gayman Helman, Martha Hensel, Carolyn L. Hodo, Alexis A. Templeton, Maritza Anguiano, Erin E. Edwards, Jay Hoffman, Brian F. Porter, Katia R. Groch, Gabriel Gomez, Josue Diaz-Delgado
Summary: The dramatic declines in amphibians worldwide show the urgent need for a better understanding of diseases affecting these species. The study found infectious/inflammatory conditions to be the main cause of death in anurans, while infectious diseases were the main CD-MPF in caudatans.
JOURNAL OF COMPARATIVE PATHOLOGY
(2021)
Review
Veterinary Sciences
Alexander Aceino, Unity Jeffery, Julie Piccione, Carolyn L. Hodo
Summary: This article discussed a case of systemic mastocytosis in a Greyhound dog, presenting with diffuse edema and hemorrhage, which is an unusual manifestation. The diagnosis involved multiple methods, including physical examination and laboratory tests, and the limitations of diagnostic criteria and their application were also discussed.
JOURNAL OF VETERINARY DIAGNOSTIC INVESTIGATION
(2021)