Article
Biochemistry & Molecular Biology
Rasha M. Hassan, Mona E. Aboutabl, Manuela Bozzi, Mohammed F. El-Behairy, Ahmed M. El Kerdawy, Beatrice Sampaolese, Claudia Desiderio, Federica Vincenzoni, Francesca Sciandra, Iman A. Y. Ghannam
Summary: Novel PPAR alpha agonists 10a and 10i exhibited high activity and hypolipidemic effects, with 10i showing better lipid-lowering activity than 10a. Additionally, both compounds showed antioxidant properties and demonstrated good safety profile in in vivo experiments.
BIOORGANIC CHEMISTRY
(2021)
Article
Chemistry, Multidisciplinary
Marta Redrado, Andrea Benedi, Isabel Marzo, Angel L. Garcia-Otin, Vanesa Fernandez-Moreira, M. Concepcion Gimeno
Summary: A new class of emissive cyclometallated Ir-III-Au-I complexes with a bis(diphenylphosphino) methanide bridging ligand was synthesized successfully. These complexes showed different bioactivity in A549 lung carcinoma cells versus endothelial cells, mainly affecting the mitochondrial and lysosomal distribution within the cells.
CHEMISTRY-A EUROPEAN JOURNAL
(2021)
Article
Endocrinology & Metabolism
Toshiharu Onodera, Dae-Seok Kim, Risheng Ye, May-Yun Wang, Shiuhwei Chen, Bianca C. Field, Leon Straub, Xue-Nan Sun, Chao Li, Charlotte Lee, Megan Paredes, Clair Crewe, Shangang Zhao, Christine M. Kusminski, Ruth Gordillo, Philipp E. Scherer
Summary: The disease progression of metabolic syndrome is associated with the role of adiponectin in pancreatic islets, which maintains normal pancreatic function by regulating the expression of the transcription factors PPARa and HNF4a.
MOLECULAR METABOLISM
(2023)
Article
Chemistry, Medicinal
Gilad Nahari, Ori Braitbard, Liraz Larush, Jacob Hochman, Edit Y. Tshuva
Summary: Orally administered nanoformulated PhenolaTi can protect the drug from decomposition in acidic conditions, showing similar in-vitro cytotoxicity towards colon cancer cells and inhibiting tumor growth in mice when administered in their drinking water. This provides a new convenient and effective mode of cancer treatment through safe titanium-based drugs.
Article
Multidisciplinary Sciences
Mariko Sakamoto, Yoji Murata, Daisuke Tanaka, Yuka Kakuchi, Takeshi Okamoto, Daisuke Hazama, Yasuyuki Saito, Takenori Kotani, Hiroshi Ohnishi, Masayuki Miyasaka, Masato Fujisawa, Takashi Matozaki
Summary: Monotherapy with antibodies targeting SIRP alpha/SIRP beta 1 can induce antitumorigenic macrophages and inhibit tumor growth by promoting killing and phagocytosis of cancer cells by these macrophages. Therefore, SIRP beta 1 is a potential target for cancer immunotherapy.
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
(2022)
Review
Pharmacology & Pharmacy
Xuhui Tong, Yuanyuan Zheng, Yu Li, Yongjian Xiong, Dapeng Chen
Summary: Inflammatory bowel disease (IBD) is a chronic intestinal condition characterized by persistent inflammation, with targeting of cytokines showing efficacy in treatment. Soluble ligands as drug targets are gaining importance, being more accessible compared to receptors, and presenting opportunities for intervention in IBD treatment.
PHARMACOLOGY & THERAPEUTICS
(2021)
Article
Chemistry, Medicinal
Farooq-Ahmad Khan, Nourina Nasim, Yan Wang, Alaa Alhazmi, Mehar Sanam, Zaheer Ul-Haq, Damayanthi Yalamati, Marina Ulanova, Zi-Hua Jiang
Summary: NOD2 is a surveillance receptor of the immune system that recognizes bacterial and viral infections. By strategically re-designing molecules, the beneficial properties of MDP can be utilized for the rational design of new vaccine adjuvants. The novel DMPs trigger higher levels of TNF-alpha release, indicating potential immunomodulatory therapeutic benefits.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Medicinal
Rasha M. Hassan, Islam H. Ali, Mohammed S. Abdel-Maksoud, Heba M. I. Abdallah, Ahmed M. El Kerdawy, Francesca Sciandra, Iman A. Y. Ghannam
Summary: Compound 9q demonstrated potent antihyperlipidemic and antioxidant activities, lowering blood lipid levels and enhancing antioxidant capacity, with improvements in aortic architecture and hepatic steatosis.
ARCHIV DER PHARMAZIE
(2022)
Article
Oncology
Yi-Hsuan Huang, Sung-How Sue, Zih-Syuan Wu, Shih-Ming Huang, Shih-Yu Lee, Zhi-Fu Wu
Summary: This study investigated the effects of tramadol on breast cancer cells and found that it inhibited cell growth, migration, colony formation, and invasion. Combination therapy with tramadol and doxorubicin showed synergistic effects. Tramadol may be a potential candidate for combination therapy, especially for triple-negative breast cancer.
FRONTIERS IN ONCOLOGY
(2022)
Review
Chemistry, Inorganic & Nuclear
D. Mouchel Dit Leguerrier, R. Barre, J. K. Molloy, F. Thomas
Summary: Lanthanides complexes are widely used in medicine and biology due to their unique properties for magnetic resonance imaging and luminescence. Recent advances in utilizing redox-reactive ligands have overcome the limitations of lanthanides in redox monitoring, expanding their applications in detecting biological relevant ROS, RNS and redox status.
COORDINATION CHEMISTRY REVIEWS
(2021)
Article
Chemistry, Multidisciplinary
Qiyuan Zhou, Shu Chen, Zoufeng Xu, Gongyuan Liu, Shuyuan Zhang, Zhigang Wang, Man-Kit Tse, Shek-Man Yiu, Guangyu Zhu
Summary: This study reports the synthesis of Pt-IV complexes bearing axial pyridines through ligand exchange reactions. It was discovered that these axial pyridines can be quickly released after reduction, indicating their potential as axial leaving groups. Two multitargeted Pt-IV prodrugs containing bioactive pyridinyl ligands, a PARP inhibitor and an EGFR tyrosine kinase inhibitor, were successfully obtained using this method. These conjugates show great potential for overcoming drug resistance, with the latter inhibiting the growth of Pt-resistant tumor in vivo. This research expands the synthetic methods for Pt-IV prodrugs and increases the range of bioactive axial ligands that can be conjugated to a Pt-IV center.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
(2023)
Review
Pharmacology & Pharmacy
Agata Zamborlin, Valerio Voliani
Summary: Angiogenesis and metastasis are two interdependent cancer hallmarks, and developing effective antiangiogenesis/antimetastasis agents is crucial for cancer treatment. Gold nanoparticles (GNPs) show promise in this area due to their unique physical and physiological properties. In this review, recent therapeutical strategies for addressing angiogenesis and metastasis are discussed, and the antiangiogenic/antimetastatic activity of GNPs is critically reviewed using in vitro and in vivo evaluations. Perspectives on the contribution of GNPs to cancer management are also provided.
DRUG DISCOVERY TODAY
(2023)
Review
Oncology
Tiange Chi, Mina Wang, Xu Wang, Ke Yang, Feiyu Xie, Zehuan Liao, Peng Wei
Summary: PPARs are lipid sensors and metabolic regulators, with PPAR-γ showing potential in inhibiting cell proliferation, inducing apoptosis, and disrupting inflammation. However, safety concerns including drug interactions need to be addressed for clinical applications.
FRONTIERS IN ONCOLOGY
(2021)
Article
Biochemistry & Molecular Biology
Yue Li, Mengjia Lv, Meiling Shen, Xi Gu, Li Zhang, Xingyong Liu, Jing Chen, Likun Gong, Zhili Zuo
Summary: Non-alcoholic fatty liver disease (NAFLD) is the most common chronic liver disease worldwide, characterized by dysregulated glucose homeostasis and lipid accumulation. PPAR alpha has been identified as a potential target for NAFLD treatment, and new 3H-benzo[b][1,4]diazepine PPAR alpha agonists were discovered using pharmacophore modeling, molecular docking, and bioassays. Compound LY-2 showed promising results in promoting the expression of PPAR alpha downstream gene and may serve as a novel lead compound for the development of potent PPAR alpha agonists.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2023)
Article
Neurosciences
Carl G. Gottschalk, Malabendu Jana, Avik Roy, Dhruv R. Patel, Kalipada Pahan
Summary: Research suggests that gemfibrozil can protect dopaminergic neurons in an animal model of PD, increase neurotransmitters in the striatum, and improve locomotor activities.
JOURNAL OF NEUROSCIENCE
(2021)
