Article
Chemistry, Medicinal
Xuejing Yao, Guiping Qi, Yaocheng Qu, Shasha Yun, Wenlong Sun, Chungang Liang, Mupeng Du, Zhuanglin Li
Summary: RC28-E, a soluble fusion protein composed of human VEGF receptor and FGFR1, shows high heterogeneity due to complex glycosylation modifications. It demonstrates higher affinity for both VEGF and FGF2 compared to other drugs targeting these factors.
NATURAL PRODUCT COMMUNICATIONS
(2022)
Article
Biochemistry & Molecular Biology
Wulong Lei, Huan Xu, Hao Yao, Lanjiao Li, Menglei Wang, Xiyuan Zhou, Xueqin Liu
Summary: This study confirmed the potential role of 5α-hydroxycostic acid in inhibiting CNV and described its possible dual pathway.
MOLECULAR MEDICINE
(2023)
Article
Pharmacology & Pharmacy
Hui Shi, Yutuo Zhu, Chunyan Xing, Shan Li, Zhishu Bao, Lei Lei, Dan Lin, Yuqin Wang, Hao Chen, Xu Xu
Summary: The DIC@Ava-loaded hydrogel proposed in this study effectively inhibited the formation of corneal neovascularization through the synergistic effects of anti-VEGF and anti-inflammatory action. The hydrogel exhibited good drug release performance and biocompatibility in in vitro and in vivo experiments.
INTERNATIONAL JOURNAL OF PHARMACEUTICS
(2022)
Article
Biochemistry & Molecular Biology
Brooklyn E. Taylor, Chieh A. Lee, Thomas E. Zapadka, Amy Y. Zhou, Katherine G. Barber, Zakary R. R. Taylor, Scott J. Howell, Patricia R. Taylor
Summary: Retinal neovascularization is a common cause of vision loss in diseases such as proliferative diabetic retinopathy, neovascular glaucoma, and age-related macular degeneration. This study found that Interleukin-17A (IL-17A) plays a crucial role in the onset and progression of non-proliferative diabetic retinopathy. The researchers also discovered that IL-17A enhances vascular endothelial growth factor (VEGF) production, promotes retinal endothelial cell proliferation, and enhances VEGF-dependent vascular angiogenesis, ultimately leading to retinal neovascularization.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Psychology, Developmental
Gokce Guldiken, Ali Karayagmurlu, Canan Kucukgergin, Murat Coskun
Summary: This study aimed to investigate the serum levels of VEGF, IGF-1, and FGF-2 in children and adolescents with ASD with and without BD, and their relationships with clinical characteristics. The study found that the ASD + BD group had higher levels of ASD severity, self-harming behavior, sleep disturbance, as well as serum VEGF and FGF-2 levels compared to the control group. There was no significant difference in serum IGF-1 levels between the two groups, and no correlation between growth factor levels and ASD severity in the study group. However, a negative correlation was found between VEGF levels and age at first diagnosis of BD, and a positive correlation between IGF-1 levels and the number of bipolar episodes in the study group.
JOURNAL OF AUTISM AND DEVELOPMENTAL DISORDERS
(2023)
Article
Biochemistry & Molecular Biology
Xi Chen, Xiao Wang, Zedu Cui, Qian Luo, Zihua Jiang, Yuke Huang, Jingyi Jiang, Jin Qiu, Yan Li, Keming Yu, Jing Zhuang
Summary: Activation of microglia is crucial in neovascular retinal diseases and understanding its mechanisms can provide potential therapeutic strategies. Through single-cell RNA sequencing, this study reveals that M1 microglia-derived exosomes enhance activation and proangiogenic ability of resting microglia. The communication is mediated by miRNA miR-155-5p, which promotes microglial activation and initiates inflammatory cascade.
INTERNATIONAL JOURNAL OF BIOLOGICAL SCIENCES
(2023)
Review
Biochemistry & Molecular Biology
Selvaraj Vimalraj
Summary: Angiogenesis is the formation of new blood vessels from existing ones. Abnormal angiogenesis, seen in tumor microenvironments, is characterized by distorted and leaky blood vessels with various shapes and high perfusion efficiency. Tumor angiogenesis plays a crucial role in cancer growth, invasion, and metastasis, and is tightly regulated by signaling networks. Targeting multiple signaling pathways involved in angiogenesis is important for effective antiangiogenic therapy. New therapeutic approaches, such as blocking specific proteins or genes, are being explored to dissect alternative angiogenesis mechanisms in tumor microenvironments.
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
(2022)
Article
Food Science & Technology
Pinghui Wei, Meiqin He, Ying Wang, Guoge Han
Summary: High-fat diet accelerates choroidal neovascularization in age-related macular degeneration. This study investigates the effects of high-fat diet on retinal and retinal pigment epithelium/choroidal acylcarnitine metabolism. The results show that high-fat diet promotes weight gain, dyslipidemia, and neovascular formation, accompanied by different changes in isomerism of metabolites.
MOLECULAR NUTRITION & FOOD RESEARCH
(2023)
Article
Chemistry, Multidisciplinary
Lukasz Oldak, Anna Lesniewska, Beata Zelazowska-Rutkowska, Eryk Latoch, Zenon Lukaszewski, Maryna Krawczuk-Rybak, Ewa Gorodkiewicz
Summary: A new method utilizing biosensors for the simultaneous determination of VEGF-A and FGF-2 in blood serum has been developed. The method offers fast, reliable, and accurate quantification, without the need for large samples or excess reagents.
APPLIED SCIENCES-BASEL
(2022)
Article
Biochemistry & Molecular Biology
Celine Baron-Menguy, Arnaud Bocquet, Alexis Richard, Anne-Laure Guihot, Bertrand Toutain, Pierre Pacaud, Celine Fassot, Gervaise Loirand, Daniel Henrion, Laurent Loufrani
Summary: The study found that sildenafil can enhance revascularization after ischemia, improve tissue blood flow and promote arteriogenesis. These effects are associated with the activation of PI3K, Akt, and eNOS, but not with VEGF.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Review
Biochemistry & Molecular Biology
Friederike Freiin von Hoevel, Ekaterini Kefalakes, Claudia Grothe
Summary: FGF-2 exists in multiple isoforms of different molecular weights in various animals, playing important roles in cell growth, migration, and maturation, and influencing the functions and disease models of organ systems such as the cardiovascular system, bone formation, and the nervous system.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Engineering, Environmental
Zhongxing Chen, Xinjie Mao, Xiuhong Ye, Siheng Li, Tianlu Wu, Qing Wang, Jun Zhang, Lu Chen, Nana Tang, Huanhuan He, Zhen Wang, Colm McAlinden, Qinmei Wang, Shihao Chen, Rongrong Gao, Jinhai Huang
Summary: In this study, a bioactive epitope of HRH peptide was conjugated to NapFF peptide to produce amphiphilic peptides which self-assemble into nanofibers. The nanofibrous structure efficiently improved the bioactivity of the HRH peptide and showed excellent anti-angiogenic activity at lower concentrations in vitro and in vivo alkali burn CoNV model. Repeated subconjunctival injection of NapFFHRH did not induce acute irritative reactions or have any detrimental effect on the retina, indicating its potential as a promising strategy for CoNV.
CHEMICAL ENGINEERING JOURNAL
(2021)
Review
Biochemistry & Molecular Biology
Bo-Hyun Moon, Younghwa Kim, Soo-Young Kim
Summary: Neovascular age-related macular degeneration (nAMD) is a major cause of blindness in the elderly population. Anti-VEGF drugs have made managing nAMD more feasible, but their effectiveness is limited and can decline over time. There is a need for continuous improvement in the efficacy and safety of these drugs.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Review
Chemistry, Medicinal
Die Jiang, Ting Xu, Lei Zhong, Qi Liang, Yonghe Hu, Wenjing Xiao, Jianyou Shi
Summary: Angiogenesis is a vital biological process for body growth and development, wound healing, and tissue formation. Dysregulation of VEGFR signaling can lead to diseases, making it a crucial research area for disease treatment. Currently, anti-VEGF drugs used in ophthalmology have limitations, and there is a need to develop small molecule inhibitors of VEGFR for the targeted treatment of ocular neovascularization diseases.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Tami Livnat, Yehonatan Weinberger, Jose A. Fernandez, Alaa Bashir, Gil Ben-David, Dahlia Palevski, Sarina Levy-Mendelovich, Gili Kenet, Ivan Budnik, Yael Nisgav, John H. Griffin, Dov Weinberger
Summary: The study demonstrated that 3K3A-APC induced regression of pre-existing CNV and reduced VEGF levels, highlighting its potential as a novel treatment for CNV and other ocular pathologies. The results suggest that the anticoagulant properties of APC are not necessary for its activities in the retina, and that VEGF reduction may contribute to the protective effects of APC and 3K3A-APC.
Article
Pharmacology & Pharmacy
Xuezhi Zhuo, Vito Fodera, Per Larsson, Zarah Schaal, Christel A. S. Bergstrom, Korbinian Lobmann, Aleksei Kabedev
Summary: Our previous work demonstrated that beta-lactoglobulin-stabilized amorphous solid dispersion (ASD) loaded with 70 % indomethacin remains stable for over 12 months. We further investigated the stabilization mechanisms by testing five other drug molecules and using experimental techniques and molecular dynamics simulations. The results showed that steric confinement, hydrogen bonding, and the glass transition temperature of the drug molecule play important roles in stabilizing ASDs with high drug loadings.
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
(2024)
Article
Pharmacology & Pharmacy
Sebastian Schmidt, Ulrike Holzgrabe
Summary: The binding of drugs to plasma proteins, such as human serum albumin (HSA), is crucial for determining pharmacokinetic parameters. This study investigated the enantioselective binding of S- and R-ketamine to HSA. It was found that ketamine has weak affinity to HSA, with no significant differences in binding behavior between the individual enantiomers and the racemate. The aromatic ring and N-methyl group were identified as the most strongly involved structural moieties in the binding of ketamine to HSA.
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
(2024)
Article
Pharmacology & Pharmacy
Yuchen Zhao, Han Wang, Lin Jin, Ziwei Zhang, Lianghu Liu, Mengqi Zhou, Xianzheng Zhang, Lingling Zhang
Summary: Interleukins (ILs) are important for communication between immune cells and non-immune cells, but dysregulation of ILs expression is a characteristic of autoinflammatory diseases. Drugs targeting ILs have significant clinical benefits, but may also cause adverse reactions. Fusion protein technology, with its ability to enhance therapeutic efficacy, has been explored for developing anti-inflammatory drugs. This review discusses the efficacy of fusion protein drugs developed with ILs or their receptors in treating autoinflammatory diseases, highlighting the potential of this technology in future anti-inflammatory drug development.
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
(2024)
Article
Pharmacology & Pharmacy
Serena Bertoni, Elena Simone, Stefano Sangiorgi, Beatrice Albertini, Nadia Passerini
Summary: This study investigated the correlation between the structure and release properties of solid lipid microparticles (MPs) with different liquid additives. The additives accelerated the conversion of the unstable alpha-form of tristearin to the stable beta-polymorph and caused structural modifications in the MPs. The presence of additives prolonged the drug release in water and resulted in higher release profiles in biorelevant media. The findings suggest that the release behavior can be influenced by the polymorphism and supramolecular-level structural modification of lipid formulations containing crystal modifiers.
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
(2024)
Article
Pharmacology & Pharmacy
Juulia Jarvinen, Ahmed B. Montaser, Santosh Kumar Adla, Jukka Leppanen, Marko Lehtonen, Kati-Sisko Vellonen, Tuomo Laitinen, Aaro Jalkanen, William F. Elmquist, Juri Timonen, Kristiina M. Huttunen, Jarkko Rautio
Summary: This study attempted to alter the brain distribution pattern of Palbociclib by creating and assessing two novel prodrugs. Although the prodrug design did not significantly improve Palbociclib brain delivery, the study provides valuable insights for future prodrug development and drug delivery strategies targeting specific transporters.
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
(2024)
Review
Pharmacology & Pharmacy
Miao Wang, Xinyu Ma, Shiyu Zong, Yaqiong Su, Rui Su, Hong Zhang, Yang Liu, Chunliu Wang, Ye Li
Summary: This article discusses the potential and limitations of nasal administration in central nervous system drug delivery. Nasal gel viscosity can alleviate the impact of nasal mucociliary clearance on drug delivery, and materials such as gellan gum, chitosan, carbomer, cellulose, and poloxamer can be used to prepare nasal gels.
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
(2024)
Article
Pharmacology & Pharmacy
Bjarke Strom Larsen, Eric Kissi, Liebert Parreiras Nogueira, Natalja Genina, Ingunn Tho
Summary: This study investigates the influence of drug load and polymer molecular weight on the structure of 3D printed tablets. The results show that drug load and polymer molecular weight have a significant impact on the porosity and size of the tablets, while the effect of drug load on the total porosity of the tablets is minimal.
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
(2024)
Article
Pharmacology & Pharmacy
Zhentao Qiao, Fuhang Wang, Dongjian Han, Yuansong Zhuang, Qingjiao Jiang, Yi Zhang, Miaomiao Liu, Quanxu An, Zhiwei Wang, Deliang Shen
Summary: In this study, it was demonstrated that periadventitial delivery of rapamycin-fibrin glue (RPM-FG) can inhibit intimal hyperplasia (IH) in a rat carotid artery injury model without compromising re-endothelialization. This provides a promising direction for the future development of a safe, effective, and minimally invasive perivascular drug delivery method to treat vascular disease.
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
(2024)
Article
Pharmacology & Pharmacy
Neele Puhlmann, Rodrigo Vidaurre, Klaus Kuemmerer
Summary: Active pharmaceutical ingredients and their metabolites and transformation products are pollutants that can harm human and environmental health. Designing greener APIs is an effective strategy to address this issue. The drug discovery and development process can incorporate environmental parameters to achieve this design, and this process is highly flexible.
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
(2024)