Review
Biochemistry & Molecular Biology
Kalin Wilson, Eileen Shiuan, Dana M. Brantley-Sieders
Summary: Over 25 years of research have identified EphA2 receptor tyrosine kinase as a promising molecular target for cancer treatment. Various targeting strategies, including drugs like dasatinib, therapeutic antibodies, and approaches harnessing antitumor immunity against EphA2-expressing cancer cells, have shown potential in preclinical studies. Completed and ongoing clinical trials are highlighting the promise and challenges of targeting EphA2 in cancer therapy.
Article
Chemistry, Medicinal
Carlo Baggio, Parima Udompholkul, Luca Gambini, Maurizio Pellecchia
Summary: This study discovered a novel agent, targefrin, that binds to EphA2-LBD and shows promising anti-cancer effects in cell-based assays and a mouse model.
JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Parima Udompholkul, Carlo Baggio, Luca Gambini, Yu Sun, Ming Zhao, Robert M. Hoffman, Maurizio Pellecchia
Summary: The study demonstrated that multimerization of a synthetic agent targeting EphA2 could enhance agonistic activity towards the receptor, suggesting potential diagnostic and therapeutic applications in EphA2-expressing tumors.
Article
Chemistry, Medicinal
Sara La Manna, Marilisa Leone, Flavia Anna Mercurio, Daniele Florio, Daniela Marasco
Summary: Researchers have designed several peptidomimetics to mimic the function of SOCS3 protein, with one chimeric peptide showing anti-inflammatory and antioxidant properties. The length and position of the cyclic analogues were found to play a crucial role in their structure and function.
Review
Food Science & Technology
Tiantian Tian, Wansheng Xie, Luxuan Liu, Siting Fan, Heqian Zhang, Zhiwei Qin, Chao Yang
Summary: In recent years, the emergence and development of antimicrobial peptides have been driven by the increasing drug resistance to traditional antibiotics. These peptides have gained considerable attention from scientists due to their high potency in combatting infectious pathogens. This review provides a summary of the mechanisms of action and structure-activity relationship of antimicrobial peptides, as well as their biological applications in various fields.
CRITICAL REVIEWS IN FOOD SCIENCE AND NUTRITION
(2023)
Article
Chemistry, Medicinal
Qianqian Gan, Kai Cui, Qi Cao, Ning Zhang, Min-Fu Yang, Xing Yang
Summary: The potential use of EphA2 as a target for detecting PSMA-negative prostate cancer has been demonstrated, and a radiolabeled ligand [F-18]AlF-ETN with high contrast has been developed for specifically imaging EphA2 expressing prostate cancer.
JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Elmer Zapata-Mercado, Gabriel Biener, Daniel M. McKenzie, William C. Wimley, Elena B. Pasquale, Valerica Raicu, Kalina Hristova
Summary: This study investigates the correlation between EphA2 signaling properties and the size of the EphA2 oligomers induced by different ligands. It is found that the size distribution of EphA2 oligomers is correlated with the efficacy of EphA2 phosphorylation, but independent of the efficacy of AKT inhibition and ligand bias coefficients.
JOURNAL OF BIOLOGICAL CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Ying Bu, Yingnan Liu, Hongwei Luan, Wenhui Zhu, Xuepeng Li, Jianrong Li
Summary: Six novel umami peptides were isolated, purified, and identified from Thai fish sauce in this study. Molecular docking and the three dimensional quantitative structure-activity relationship model revealed the association between the structure and activity of umami peptides, with a significant spatial effect observed for long chain peptides.
Article
Infectious Diseases
Yaxian Lin, Siyan Liu, Xinping Xi, Chengbang Ma, Lei Wang, Xiaoling Chen, Zhanzhong Shi, Tianbao Chen, Chris Shaw, Mei Zhou
Summary: Antimicrobial peptide Brevinin-2GUb, extracted from Hylarana guentheri, has modest antimicrobial activity and can be optimized by shortening the peptide while maintaining its bioactivity, with keeping a complete hydrophobic face and increasing net charges being key factors for antimicrobial activity. The analog tB2U-6K showed improved activity against bacteria, including Gram-negative bacteria, clinical isolates, and fungi, addressing aspects of antibiotic resistance.
Article
Chemistry, Medicinal
Kien Tran, Alexandre Murza, Xavier Sainsily, Eugenie Delile, Pierre Couvineau, Jerome Cote, David Coquerel, Maude Peloquin, Mannix Auger-Messier, Michel Bouvier, Olivier Lesur, Philippe Sarret, Eric Marsault
Summary: ELABELA (ELA) is the second endogenous ligand of the apelin receptor (APJ). The shortest bioactive C-terminal fragment ELA23-32, with high affinity for APJ, produces cardiorenal effects similar to those of ELA in vivo. Studies suggest that ELA and apelin-13 may interact differently with APJ, and aromatic residues at the Phe31 or Pro32 position are important for receptor activation.
JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Cell Biology
Huiyun Yang, Guanjie Qin, Zan Luo, Xiangyun Kong, Chunqiao Gan, Ruyun Zhang, Wei Jiang
Summary: This study investigated the relationship between methylation of MFSD4A and its expression in nasopharyngeal carcinoma (NPC), and found that MFSD4A affects NPC progression by degrading EPHA2. Clinical research showed that high expression of MFSD4A or low expression of EPHA2 is associated with better prognosis for NPC patients.
CELL DEATH & DISEASE
(2022)
Article
Biochemistry & Molecular Biology
Fu-Ling Chang, Cheng-Chung Lee, Keng-Chang Tsai, Tsai-Yu Lin, Chen-Wei Chiang, Shiow-Lin Pan, Yu-Ching Lee
Summary: In this study, a novel antibody-drug conjugate (ADC) specifically targeting EphA2 in pancreatic cancer cells was developed. The ADC showed impressive tumor-killing response, inhibiting tumor cell growth and promoting apoptosis. The results suggest the potential of further developing the ADC to have a broader and more potent therapeutic impact on pancreatic cancer and other EphA2-related cancers.
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
(2023)
Article
Biochemistry & Molecular Biology
Zhaoxuan Li, Jingling Liu, Jie You, Xin Li, Zongsuo Liang, Junli Du
Summary: To understand the influence mechanism of interactions between different monomer units of proanthocyanidins (PAs) on biological activity, researchers proposed a path analysis model. This model considers not only the correlation between each monomer unit and activity, but also the correlation with its related monomer units. It can determine the action mode of each monomer unit affecting the activity by comparing the direct and total indirect effects. The model's advantage is demonstrated through an analysis of Rhodiola crenulata PA monomer units' influence on antioxidant and anti-diabetes activities.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Biochemistry & Molecular Biology
Karol Wtorek, Alessia Ghidini, Luca Gentilucci, Anna Adamska-Bartlomiejczyk, Justyna Piekielna-Ciesielska, Chiara Ruzza, Chiara Sturaro, Girolamo Calo, Stefano Pieretti, Alicja Kluczyk, John McDonald, David G. Lambert, Anna Janecka
Summary: Recently, two novel chimeric peptides, KW-495 and KW-496, were developed as mixed opioid/NOP agonists. KW-495 showed low nM affinity as a mixed MOP/NOP agonist, while KW-496 became a dual KOP/MOP agonist. In in vivo experiments, KW-495 exhibited antinociceptive effects in mice and was sensitive to opioid receptor antagonists.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Review
Food Science & Technology
Lu Xiang, Zhichang Qiu, Renjie Zhao, Zhenjia Zheng, Xuguang Qiao
Summary: Food-derived antihypertensive peptides have gained attention in functional foods due to their high biological activity, low toxicity, and easy metabolism in the human body. However, there is still limited understanding of ACE inhibitory peptides and their knowledge gaps. This paper focuses on the food sources and production methods of ACE inhibitory peptides, as well as their transport and underlying mechanisms. Additionally, the structure-activity relationships and other bio-functional properties of ACE inhibitory peptides are discussed.
CRITICAL REVIEWS IN FOOD SCIENCE AND NUTRITION
(2023)