Article
Cell Biology
Ming-Jen Hsu, Han-Kun Chen, Jin-Cherng Lien, Yu-Han Huang, Shiu-Wen Huang
Summary: This study evaluated the anti-angiogenic properties of a new naphthoquinone derivative, PPE8, and explored its mechanisms of action. The results showed that PPE8 reduced proliferation, migration, invasion, and tube formation in human umbilical vein endothelial cells (HUVECs) induced by VEGF-A. It also inhibited micro vessel sprouting and angiogenesis in vivo. Additionally, PPE8 suppressed phosphorylation of VEGFR-2, Src, FAK, ERK1/2, and AKT in HUVECs exposed to VEGF-A, and exhibited significant decline in xenograft tumor growth. These findings suggest that PPE8 may target VEGF-A-VEGFR-2 signaling to reduce angiogenesis, making it a potential drug candidate for angiogenesis-related diseases.
Article
Biochemistry & Molecular Biology
Magda M. F. Ismail, Taghreed Z. Shawer, Rabab S. Ibrahim, Rasha M. Allam, Yousry A. Ammar
Summary: This study aims to explore the VEGFR-2 inhibitory activity of a novel library of quinoxalin-2-one derivatives and found that compound 7f displayed remarkable cytotoxicity against HCT-116 and MCF-7 cell lines. It also showed potential anti-migratory effect and induced apoptosis and cell cycle arrest. Molecular docking confirmed the affinity of these compounds for VEGFR-2 active site.
BIOORGANIC CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Mostafa M. Ghorab, Aiten M. Soliman, Khaled El-Adl, Noura S. Hanafy
Summary: Here, we synthesized a series of new quinazoline sulfonamide conjugates 2-16 and evaluated their potential as anticancer agents by targeting EGFRT790M and VEGFR-2. The compounds were designed based on the structure requirements of the receptors and confirmed using spectral data. They were tested for cytotoxicity against four cancer cell lines and the most active compound (15) showed significant cytotoxic and inhibitory activity against EGFR and VEGFR.
BIOORGANIC CHEMISTRY
(2023)
Article
Oncology
Catarina Nascimento, Andreia Gameiro, Joao Ferreira, Jorge Correia, Fernando Ferreira
Summary: Feline mammary carcinoma is the third most common neoplasia in cats, with highly malignant behavior. The study suggests that VEGF-A and its serum receptors assessment may have potential in the diagnosis and treatment of feline mammary carcinoma.
Article
Biochemistry & Molecular Biology
Moataz A. Shaldam, Hadia Almahli, Andrea Angeli, Rehab Mustafa Badi, Eman F. Khaleel, Abdelrahman I. Zain-Alabdeen, Zainab M. Elsayed, Eslam B. Elkaeed, Rofaida Salem, Claudiu T. Supuran, Wagdy M. Eldehna, Haytham O. Tawfik
Summary: New isatin-based sulphonamides were synthesized as potential dual VEGFR-2 and carbonic anhydrase inhibitors with anticancer activities. The most potent derivatives showed strong VEGFR-2 inhibitory effect but failed to inhibit relevant CA isoforms. Two derivatives were further tested for their impact on cell cycle disturbance and apoptotic potential. Molecular modelling analyses were conducted to assess the binding mode and stability of the target compounds.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2023)
Review
Chemistry, Medicinal
Mahfam Moradi, Alireza Mousavi, Zahra Emamgholipour, Johanna Giovannini, Setareh Moghimi, Fariba Peytam, Amin Honarmand, Stephane Bach, Alireza Foroumadi
Summary: Angiogenesis is crucial for endothelial cell migration, growth, and differentiation, but dysregulated angiogenesis in tumor microenvironments contributes to tumor growth. VEGFR-2 inhibitors, especially quinazoline derivatives, have been approved for cancer treatment, but there are limitations in clinical efficacy and drug resistance. There is a need for the design and synthesis of more selective and effective inhibitors to overcome these challenges.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Review
Cardiac & Cardiovascular Systems
Bronte Miller, Mary Kathryn Sewell-Loftin
Summary: Endothelial cells in the vascular system respond to mechanical forces, playing a critical role in maintaining blood vessel structure and function. Understanding the mechanisms of biomechanical regulation in vascular growth can lead to new therapeutic strategies for different diseases.
FRONTIERS IN CARDIOVASCULAR MEDICINE
(2022)
Review
Biochemistry & Molecular Biology
Mohamed Reda Aouad, Meshal A. Almehmadi, Fawzia Faleh Albelwi, Mohamed Teleb, Gina N. Tageldin, Marwa M. Abu-Serie, Mohamed Hagar, Nadjet Rezki
Summary: In this study, the simultaneous inhibition of MMP-2, CA II, and VEGFR-2 using rationally designed triazole hybrids was reported. Among the tested compounds, 8d and 8e showed the most potent anticancer activity and selectivity, significantly affecting cancer cell lines and increasing the expression level of the tumor suppressor p53.
BIOORGANIC CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Menna M. A. Abd El-Mageed, Amal A. M. Eissa, Awatef El-Said Farag, Essam Eldin A. Osman
Summary: A series of novel furan and furo[3,2-e][1,2,4]triazolo[1,5-c]pyrimidine derivatives were designed and synthesized, exhibiting good to moderate VEGFR-2 inhibitory activity. Some compounds showed higher antiproliferative effects on HUVECs compared to sorafenib, with the ability to disrupt cell cycle progression and inhibit cell invasion and migration.
BIOORGANIC CHEMISTRY
(2021)
Article
Multidisciplinary Sciences
Edward Hartsough, Rajani R. J. Shelke, Razie Amraei, Zahra Aryan, Saran Lotfollahzadeh, Nader Rahimi
Summary: Activation and signal transduction of vascular endothelial growth factor receptor-2 (VEGFR-2) play crucial roles in vasculogenesis and pathological angiogenesis. The study reveals that protein arginine methyltransferase 4 (PRMT4) mediates methylation of a specific site on VEGFR-2, which affects VEGFR-2-induced angiogenic responses. This finding may have implications for the development of targeted VEGFR-2 inhibitors.
Review
Chemistry, Medicinal
Thoraya A. Farghaly, Wedian A. Al-Hasani, Hanan Gaber Abdulwahab
Summary: The VEGFR-2 signaling pathway plays a critical role in angiogenesis and has become an important target for treating angiogenesis-related diseases. Current treatment methods may face challenges such as poor response, development of resistance, and serious adverse effects, so combining different treatment methods and utilizing nanomedicine may enhance efficacy, reduce side effects, and lower costs.
EXPERT OPINION ON THERAPEUTIC PATENTS
(2021)
Article
Biochemistry & Molecular Biology
Mingxue Di, Yu Zhang, Renya Zeng, Xiaolin Liu, Weijia Chen, Meng Zhang, Cheng Zhang, Mengmeng Li, Mei Zhang
Summary: The study revealed that the MiR33a-5p/Ets-1/DKK1 signaling pathway is involved in ox-LDL-induced angiogenesis of HUVECs. These new findings provide a rationale and notable method for tumor therapy and cardiovascular protection.
INTERNATIONAL JOURNAL OF BIOLOGICAL SCIENCES
(2021)
Article
Biochemistry & Molecular Biology
Dailin Tan, Yongxu Zhao, Danjun Ma, Fangfang Tong
Summary: FSH regulates endothelial cell migration by binding to FSHR, activating multiple signaling pathways including cAMP-PKA, JAK-STAT, PI3K-AKT, and JNK-MAPK; inhibition of VAV3 or LAMA2 expression attenuates the effect of FSH on endothelial cell migration.
Article
Biotechnology & Applied Microbiology
Qiong Xu, Zequn Liu, Zhi-Qin Zhu, Yue Fan, Rui Chen, Xiao-Hui Xie, Mi Cheng
Summary: GRB7 plays a crucial role in regulating angiogenesis in ovarian cancer by modulating VEGFA expression and affecting endothelial cell behaviors such as proliferation, migration, and invasion. Knockdown of GRB7 could serve as a potential therapeutic target for suppressing tumor angiogenesis in ovarian cancer.
Article
Chemistry, Multidisciplinary
Feiyi Yang, Qian Zhang, Qiuyan Guo, Qingshan Pan, Chunping Wen, Xinya Lv, Wufu Zhu, Pengwu Zheng
Summary: A class of 4-phenoxy-pyridine/pyrimidine derivatives were synthesized and evaluated as potent dual VEGFR-2/c-Met inhibitors. Among them, compound 23k showed excellent anti-cancer cell proliferative activity and low toxicity. Further studies demonstrated that compound 23k induced apoptosis and blocked the cell cycle. Molecular docking and simulation revealed the binding modes of 23k to VEGFR-2 and c-Met.
NEW JOURNAL OF CHEMISTRY
(2022)
Correction
Biochemistry & Molecular Biology
Mohamed Marzouk, Shimaa M. Khalifa, Amal H. Ahmed, Ahmed M. Metwaly, Hala Sh. Mohammed, Hanan A. A. Taie
BIOORGANIC CHEMISTRY
(2024)
Article
Biochemistry & Molecular Biology
Gerardo Andres Libreros-Zuniga, Danilo Pava e Pavao, Vinicius de Morais Barroso, Nathalya Cristina de Moraes Roso Mesquita, Saulo Fehelberg Pinto Braga, Glaucius Oliva, Rafaela Salgado Ferreira, Kelly Ishida, Marcio Vinicius Bertacine Dias
Summary: Tuberculosis is a major global cause of death, and the emergence of drug-resistant strains has increased the burden of this disease. New alternative therapies are constantly needed, and recent research has identified small molecules as potential inhibitors of Ldts in M. tuberculosis, which have antimycobacterial activity.
BIOORGANIC CHEMISTRY
(2024)
Article
Biochemistry & Molecular Biology
Xiao-Dong Wang, Yong-Si Liu, Ming-Hao Hu
Summary: In this study, a selffolded fluorescent probe was designed to selectively illuminate G4s by unfolding its intramolecular aggregation mediated by G4 binding. This probe showed more controllable background emission and promising ability to track G4 forming dynamics compared to previous disaggregation-induced emission (DIE) probes.
BIOORGANIC CHEMISTRY
(2024)
Article
Biochemistry & Molecular Biology
Yu Xiang, Zhuo Yuan, Qichuan Deng, Linshen Xie, Dongke Yu, Jianyou Shi
Summary: This review provides a brief description of the diagnosis, pathogenesis, and potential therapeutic inhibitors for renal fibrosis. Currently, there are no clear therapeutic targets or drugs for renal fibrosis; however, some natural products may have potential efficacy for treating renal fibrosis.
BIOORGANIC CHEMISTRY
(2024)
Article
Biochemistry & Molecular Biology
Simone Giovannuzzi, Anna Nikitjuka, Bruna Rafaela Pereira Resende, Michael Smietana, Alessio Nocentini, Claudiu T. Supuran, Jean-Yves Winum
Summary: Boron-based compounds have been extensively studied in medicinal chemistry, playing a crucial role in designing small molecule drugs for various diseases. Boron is particularly valuable in developing inhibitors for metalloenzymes carbonic anhydrases, and it can modulate ligand recognition ability and selectivity. Recent advancements have led to the discovery of novel boron-based inhibitors that can inhibit carbonic anhydrases through a Lewis acid-base mechanism. Further research is needed to fully explore the potential of boron-based inhibitors and advance their clinical applications.
BIOORGANIC CHEMISTRY
(2024)
Article
Biochemistry & Molecular Biology
Xinxin Liu, Lei Chen, Ze Chen
Summary: This study developed a nanostructured photosensitizer loaded with oxygen-throttling drug and demonstrated its enhanced cytotoxicity against tumor cells under hypoxic conditions. Animal experiments showed the enhanced tumor targeting capability of the photosensitizer and its inhibitory effect on tumor growth.
BIOORGANIC CHEMISTRY
(2024)
Article
Biochemistry & Molecular Biology
Shuai Jiang, Wen-Yan Li, Zai-Feng Yuan, Qin-Shi Zhao
Summary: This study isolated two new dimeric Lycopodium alkaloids and twelve previously undescribed Lycopodium alkaloids from Lycopodiastrum casuarinoides. The structures of these compounds were determined and their inhibitory activities on the Cav3.1 channel were evaluated.
BIOORGANIC CHEMISTRY
(2024)
Article
Biochemistry & Molecular Biology
Yan Yang, Dong-Xiao Yan, Rui-Xue Rong, Bing-Ye Shi, Man Zhang, Jing Liu, Jie Xin, Tao Xu, Wen-Jie Ma, Xiao-Liu Li, Ke-Rang Wang
Summary: In this study, a series of nucleolar fluorescent probes based on naphthalimide derivatives were designed and synthesized, which could achieve clear nucleolar staining in living cells. The results showed that these probes exhibited good targeting to the cell nucleolus and could bind to RNA and enhance fluorescence. This has positive implications for the diagnosis and treatment of nucleolus-related diseases.
BIOORGANIC CHEMISTRY
(2024)
Article
Biochemistry & Molecular Biology
Yongxi Dong, Fang Wang, Jinlan Wen, Yongqing Mao, Shanhui Zhang, Tiemei Long, Zhangxiang Yang, Lei Li, Jiquan Zhang, Li Dong, Gang Liu, Jianwei Xu
Summary: The hybrid molecules of Scutellarein and Tertramethylpyrazine show excellent neuroprotective and antiplatelet effects in the treatment of ischemic stroke. Compound 1e is particularly effective, enhancing cell membrane permeability and inhibiting cell uptake, as well as significantly reducing cerebral infarction volume.
BIOORGANIC CHEMISTRY
(2024)
Article
Biochemistry & Molecular Biology
Yu Chen, Yuanyuan Ying, Jonathan Lalsiamthara, Yuheng Zhao, Saber Imani, Xin Li, Sijing Liu, Qingjing Wang
Summary: This paper examines the role and metabolic regulation of NAD+ in bacteria, highlighting its impact on physiology and virulence. It explores enzymes associated with NAD+ metabolism as potential targets for antibacterial drugs and vaccine candidates. Additionally, it scrutinizes the medical potential of NAD+ and provides insights for its application in biomedicine.
BIOORGANIC CHEMISTRY
(2024)
Article
Biochemistry & Molecular Biology
Jon Macicior, Daniel Fernandez, Silvia Ortega-Gutierrez
Summary: Hutchinson-Gilford progeria syndrome (HGPS), also known as progeria, is a rare genetic disease that causes premature aging and significantly reduces life expectancy. Currently, there is only one approved drug for treating progeria, but its efficacy is limited. Progerin levels are believed to be the most important biomarker related to disease severity.
BIOORGANIC CHEMISTRY
(2024)
Article
Biochemistry & Molecular Biology
Fuko Hirano, Naoya Kondo, Yusuke Murata, Aya Sudani, Takashi Temma
Summary: Fluorinated alpha-methyl 3BPA derivatives showed improved water solubility, tumor targetability, and biodistribution compared to 3BPA and BPA, resulting in significantly improved tumor-to-normal tissue ratios.
BIOORGANIC CHEMISTRY
(2024)
Article
Biochemistry & Molecular Biology
Ying Shi, Jiaqin Tang, Shumeng Zhi, Ruiqi Jiang, Qing Huang, Lei Sun, Zhizhong Wang, Yanran Wu
Summary: Necroptosis is a type of cell death associated with various diseases. In this study, we identified a small molecule inhibitor, SY-1, that effectively blocks necroptosis by inhibiting the phosphorylation of RIP1/RIP3/MLKL pathway. SY-1 also showed protective effects against TNF-induced hypothermia and improved survival in mice with SIRS. These findings highlight the potential therapeutic applications of SY-1.
BIOORGANIC CHEMISTRY
(2024)
Article
Biochemistry & Molecular Biology
Andrea Bagan, Sonia Abas, Judith Pala-Pujadas, Alba Irisarri, Christian Grinan-Ferre, Merce Pallas, Itziar Muneta-Arrate, Carolina Muguruza, Luis F. Callado, Belen Perez, Elies Molins, Jose A. Morales-Garcia, Carmen Escolano
Summary: Recent studies have identified the modulation of imidazoline I-2 receptors (I-2-IR) by selective ligands as a potential strategy for treating neurodegenerative diseases. This study reports a family of bicyclic alpha-iminophosphonates that show high affinity and selectivity for I-2-IR and demonstrates their neuroprotective and anti-inflammatory effects in in vitro and in vivo models. The findings emphasize the importance of exploring structurally novel I-2-IR ligands for therapeutic strategies in neurodegeneration.
BIOORGANIC CHEMISTRY
(2024)
Article
Biochemistry & Molecular Biology
Qiuping Xiang, Tianbang Wu, Cheng Zhang, Chao Wang, Hongrui Xu, Qingqing Hu, Jiankang Hu, Guolong Luo, Xiaoxi Zhuang, Xishan Wu, Yan Zhang, Yong Xu
Summary: This study reports the discovery of a 1-(indolizin-3-yl)ethan-1-one derivative as a potent and selective CBP bromodomain inhibitor for AML drug development.
BIOORGANIC CHEMISTRY
(2024)