Article
Biochemistry & Molecular Biology
Martin Kellert, Jan-Simon Jeshua Friedrichs, Nadine Anke Ullrich, Alexander Feinhals, Jonas Tepper, Peter Loennecke, Evamarie Hey-Hawkins
Summary: The development of novel boron-rich compounds for use in boron neutron capture therapy (BNCT) is an important field in cancer treatment. The study reports the design and synthesis of two promising compounds that combine meta-carborane, a water-soluble monosaccharide, and a linking unit for coupling with tumor-selective biomolecules. This approach enables the development of readily obtainable boron-rich agents with optimized properties for potential applications in BNCT.
Article
Biochemistry & Molecular Biology
Sebastian Flieger, Mao Takagaki, Natsuko Kondo, Marlon R. Lutz, Yash Gupta, Hiroki Ueda, Yoshinori Sakurai, Graham Moran, Prakasha Kempaiah, Narayan Hosmane, Minoru Suzuki, Daniel P. Becker
Summary: New carborane-bearing hydroxamate matrix metalloproteinase (MMP) ligands with nanomolar potency against MMP-2, -9 and -13 have been synthesized for boron neutron capture therapy (BNCT). In vitro studies showed that these new MMP ligands had high tumoricidal effects in the BNCT assay. This study highlights the importance of targeting MMP enzymes overexpressed on the surface of tumor cells for BNCT efficacy.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Chemistry, Multidisciplinary
Tainah Dorina Marforio, Edoardo Jun Mattioli, Francesco Zerbetto, Matteo Calvaresi
Summary: Blood transport proteins, especially hemoglobin, have been identified as potential carriers for carboranes, which can improve their solubility and bioavailability. The carborane@protein complexes formed in water are stable and characterized by favorable binding energy. This study suggests an innovative formulation for carboranes by forming a carborane@protein complex prior to administration.
Article
Nanoscience & Nanotechnology
Niranjan Meher, Kyounghee Seo, Sinan Wang, Anil P. Bidkar, Miko Fogarty, Suchi Dhrona, Xiao Huang, Ryan Tang, Charles Blaha, Michael J. Evans, David R. Raleigh, Young-Wook Jun, Henry F. VanBrocklin, Tejal A. Desai, David M. Wilson, Tomoko Ozawa, Robert R. Flavell
Summary: PSMA-targeted poly(lactide-co-glycolide)-block-poly(ethylene glycol) nanoparticles loaded with carborane show strong PSMA binding capability and potential for prostate cancer treatment in vivo.
ACS APPLIED MATERIALS & INTERFACES
(2021)
Article
Chemistry, Physical
Dawid Kozien, Paulina Zeliszewska, Bozena Szermer-Olearnik, Zbigniew Adamczyk, Anna Wroblewska, Agnieszka Szczygiel, Katarzyna Wegierek-Ciura, Jagoda Mierzejewska, Elzbieta Pajtasz-Piasecka, Tomasz Tokarski, Grzegorz Cios, Stanislaw Cudzilo, Zbigniew Pedzich
Summary: This research presents the synthesis of B4C nanoparticles via vapor deposition and investigates their characteristics. The study evaluates the cytotoxicity effect of the synthesized nanoparticles on various cell lines, providing insights into their potential application in boron neutron capture therapy.
Review
Pharmacology & Pharmacy
Anne-Marie Caminade, Max Milewski, Evamarie Hey-Hawkins
Summary: The use of boron clusters in nanoparticles for cancer treatment, particularly in dendrimers, is highlighted in this review. The synthesis methods and biological properties of boronated dendritic structures are discussed, along with their efficiency in animal models and potential for boron neutron capture therapy (BNCT) experiments.
Review
Oncology
Timothy D. Malouff, Danushka S. Seneviratne, Daniel K. Ebner, William C. Stross, Mark R. Waddle, Daniel M. Trifiletti, Sunil Krishnan
Summary: Boron neutron capture therapy (BNCT) is an emerging treatment modality that utilizes boron-10 to target tumors and has shown promising results in various cancer types in clinical studies.
FRONTIERS IN ONCOLOGY
(2021)
Article
Engineering, Chemical
Mizuki Kitamatsu, Ken Inoue, Naoki Yamagata, Hiroyuki Michiue
Summary: This study assessed the reactivity between chloroacetyl-modified tripeptides with different amino acid residues and mercaptoundecahydrododecaborate. The results showed that the reactivity varied with the type and number of amino acid residues as well as the length of the alkyl linker. The electrostatic attraction between positively charged amino acid residues and negatively charged mercaptoundecahydrododecaborate was found to play a key role in the accelerated reaction.
Article
Materials Science, Characterization & Testing
Feng Zhao, Kaibo Hu, Chen Shao, Guofan Jin
Summary: This paper designed and synthesized two boron-polymers as fluorescent targeting markers for rapid, accurate, real-time, and inexpensive detection of boron-containing drugs. Both polymers showed high levels of biological activity in terms of cytotoxicity and cell imaging.
Article
Biochemistry & Molecular Biology
Tien-Li Lan, Chun-Fu Lin, Yi-Yen Lee, Ko-Han Lin, Feng-Chi Chang, Shih-Chieh Lin, Jia-Cheng Lee, Fong-In Chou, Jinn-Jer Peir, Hong-Ming Liu, Pei-Fan Mu, Yi-Wei Chen
Summary: Meningiomas are the most common primary intracranial tumors in adults. Surgical resection is the preferred treatment, but for those not suitable for surgery, radiotherapy can be considered. Recurrent meningiomas present a challenge due to their location in previously irradiated areas. This article introduces four patients from Taiwan who were treated with Boron Neutron Capture Therapy (BNCT) for recurrent meningiomas. The study shows promising results, with two stable diseases, one partial response, and one complete response. BNCT is proven effective and safe as an alternative salvage treatment for recurrent meningiomas.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Chemistry, Inorganic & Nuclear
Mingi Kim, Sehee Im, Chan Hee Ryu, Seok Ho Lee, Ju Hyun Hong, Kang Mun Lee
Summary: The research examined the luminescent properties of closo- and nido-carboranyl compounds with different structural effects, revealing their radiative decay mechanisms. The findings indicate distinct differences in the luminescent properties of the different compounds in THF, with significant effects of fluoride ions on the luminescence of closo compounds.
DALTON TRANSACTIONS
(2021)
Review
Microbiology
Liudmila A. Alexandrova, Anastasia L. Khandazhinskaya, Elena S. Matyugina, Dmitriy A. Makarov, Sergey N. Kochetkov
Summary: Tuberculosis is the oldest human infection disease, and a significant number of the world's population is currently infected with Mycobacterium tuberculosis. Despite a decrease in mortality, the emergence of multidrug-resistant strains has created an urgent need for new anti-TB drugs. Nucleoside analogues have shown antimycobacterial activity, but no clinically used drugs based on them exist yet.
Article
Chemistry, Multidisciplinary
Masahiro Nishikawa, Jie Yu, Heon Gyu Kang, Minoru Suzuki, Naoki Komatsu
Summary: Boron neutron capture therapy is an advanced cancer treatment that utilizes nuclear fission of B-10 atom in cancer cells. In this study, anticancer nanoformulations were designed by conjugating a boron cluster moiety and an active targeting moiety to enhance selectivity and retention in tumors. The results showed that the boron cluster moiety facilitated cellular uptake and the nanodrugs exhibited good anticancer efficacy under thermal neutron irradiation.
CHEMISTRY-A EUROPEAN JOURNAL
(2023)
Article
Biochemistry & Molecular Biology
Chun-Yi Wu, Hsin-Hua Hsieh, Ting-Yu Chang, Jia-Jia Lin, Chin-Ching Wu, Ming-Hua Hsu, Ming-Chia Lin, Shin-Lei Peng
Summary: This study aimed to develop novel AuNPs containing boron and gadolinium for BNCT. The in vitro MR images showed a positive correlation between signal intensity and Gd concentration, allowing clear visualization of tumors. The developed AuNPs show potential for theranostic applications in cancer therapy.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Oncology
Song Wang, Zhengchao Zhang, Lele Miao, Jiaxing Zhang, Futian Tang, Muzhou Teng, Yumin Li
Summary: Boron Neutron Capture Therapy (BNCT) is a new binary radiation therapy that uses neutron capture reaction to kill tumor cells. It has been included in the clinical backup program for the treatment of glioma, melanoma, and other diseases. However, the key challenge of BNCT lies in developing more efficient boron delivery agents to improve targeting and selectivity.
FRONTIERS IN ONCOLOGY
(2023)
Article
Biotechnology & Applied Microbiology
Han-Shin Kim, Eunji Cha, So-Young Ham, Jeong-Hoon Park, SangJin Nam, Hongmok Kwon, Youngjoo Byun, Hee-Deung Park
Summary: Linoleic acid (LA), a plant unsaturated fatty acid, was found to inhibit biofilm formation of Pseudomonas aeruginosa without inhibiting bacterial growth. LA also influenced bacterial motility, extracellular polymeric substance production, and biofilm dispersion by decreasing intracellular cyclic diguanylate concentration through increased phosphodiesterase activity. Additionally, LA induced the expression of genes associated with diffusible signaling factor-mediated quorum sensing that can inhibit or induce the dispersion of P. aeruginosa biofilms.
BIOTECHNOLOGY AND BIOENGINEERING
(2021)
Article
Chemistry, Multidisciplinary
Sangmin Park, Hyeji Shin, Dawon Park, Hyunwoo Kim, Youngjoo Byun, Ki Yong Lee
Summary: The ethyl acetate fraction of Inonotus obliquus significantly inhibited nitric oxide production in LPS-induced murine BV2 microglial cells. Among the isolated triterpenes, compounds 2-4 showed significant reduction in nitric oxide production at a concentration of 30 μM.
MAGNETIC RESONANCE IN CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
One-Sung Park, Jeong Kyu Bang, Kyoung-Seok Ryu, Eunha Hwang, Kwan Soo Hong, Youngjoo Byun, Chaejoon Cheong, Young Ho Jeon
Summary: NERP-2, derived from the VGF neuropeptide precursor, exhibits a partially helical structure in buffer solutions, while showing a more stable helical structure in HFIP or DPC micelle. The NMR spectroscopy determined its 3D structure in both types of solutions, showing predominantly helical structure in HFIP and partial helical structure in DPC solutions. The amphipathic nature of the helical structure suggests potential structural changes in NERP-2 upon receptor binding.
Review
Chemistry, Medicinal
Hyunsoo Ha, Hongmok Kwon, Taehyeong Lim, Jaebong Jang, Song-Kyu Park, Youngjoo Byun
Summary: PSMA-targeted probes based on the Lys-urea-Glu structure have been successfully translated into clinical use, including imaging agents labeled with radionuclides and therapeutic agents with structure modifications in the non-pharmacophore pocket.
EXPERT OPINION ON THERAPEUTIC PATENTS
(2021)
Article
Biochemistry & Molecular Biology
Hongmok Kwon, Hyunsoo Ha, Hayoung Jeon, Jaebong Jang, Sang-Hyun Son, Kiho Lee, Song-Kyu Park, Youngjoo Byun
Summary: Hepsin, a type II transmembrane serine protease, is overexpressed in several types of cancer including prostate cancer. Compound 22a, a p-guanidinophenylalanine-based dipeptide analog, shows strong hepsin-inhibitory activity and selectivity over matriptase, suggesting it could be a potential prototype for structural optimization of hepsin inhibitors.
BIOORGANIC CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Deepa R. Parmar, Jigar Y. Soni, Ramakrishna Guduru, Rahul H. Rayani, Rakesh V. Kusurkar, Anand G. Vala, Sahista N. Talukdar, Ibrahim H. Eissa, Ahmed M. Metwaly, Ahmed Khalil, Vishwanath Zunjar, Satyanarayana Battula
Summary: A series of novel thiourea compounds were designed and synthesized, with compound 3B showing potent anticancer activity against various cancer cell lines. Several compounds demonstrated significant cytotoxicity across different cancer cell lines.
BIOORGANIC CHEMISTRY
(2021)
Article
Engineering, Chemical
Mohamed Shaker S. Adam, Ahmed Khalil
Summary: This research focuses on the synthesis, characterization, and reactivity of three new mononuclear complexes and their catalytic and biological properties. The results show that the VOSn in L catalyst exhibited high catalytic efficiency and significant antimicrobial, antioxidant, and anticancer activities. These findings have important implications for industrial catalysis and clinical applications.
JOURNAL OF THE TAIWAN INSTITUTE OF CHEMICAL ENGINEERS
(2022)
Article
Infectious Diseases
Taehyeong Lim, So-Young Ham, SangJin Nam, Myoungsun Kim, Ki Yong Lee, Hee-Deung Park, Youngjoo Byun
Summary: This article reviews recent studies on small molecules targeting the RhlI/RhlR system in P. aeruginosa, discussing their in vitro and in vivo biological activities. The article focuses on structure-activity relationship studies and the outlook for next-generation anti-biofilm agents.
Review
Biochemistry & Molecular Biology
Shinyoung Lee, Hyunsoo Ha, Jaebong Jang, Youngjoo Byun
Summary: The activation of the P2X7 receptor (P2X7R) by elevated levels of extracellular ATP (eATP) in the brain is associated with neuroinflammation, which plays a role in depression. Therefore, targeting P2X7R has become an attractive approach for developing novel antidepressant agents. Several CNS-penetrating P2RX7 antagonists have been developed by multinational pharmaceutical companies and evaluated in clinical trials. This review summarizes the recent progress in the development of P2X7R antagonists for depression treatment.
CURRENT MEDICINAL CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Ahmed Khalil, Amany S. El-Khouly, Eslam B. Elkaeed, Ibrahim H. Eissa
Summary: This study investigated the interaction between Sofosbuvir and HCV NS5B polymerase using molecular modeling and computational methods. The results demonstrated that the tested compounds correctly bind to the active sites with good binding affinities. The substituents had a mild effect on the binding mode, with increased hydrophobicity leading to better binding affinities. Drug likeness and toxicity studies suggested that the examined derivatives have potential as safe drugs. Molecular dynamics simulations and energy stability studies further confirmed the stability of the compound.
Article
Geriatrics & Gerontology
Ji Yun Park, Haneur Lee, Eun Seon Song, Yun Haeng Lee, Myeong Uk Kuk, Gahyun Ko, Hyung Wook Kwon, Youngjoo Byun, Joon Tae Park
Summary: This study reveals a novel mechanism in which modulation of p38 MAPK activity leads to the improvement of senescence through functional restoration of lysosomes and mitochondria.
REJUVENATION RESEARCH
(2022)
Article
Chemistry, Medicinal
Ji-Hun Park, Xuran Zhang, Hyunsoo Ha, Jung Kim, Joon Choi, Kyung-Han Lee, Youngjoo Byun, Yearn Choe
Summary: This study aimed to develop a radioligand for positron emission tomography (PET) imaging of Hepsin, a potential biomarker for prostate cancer. Through the synthesis and evaluation of various ligands, a promising PET radioligand with high binding affinity and selectivity for Hepsin was selected. The radioligand exhibited high binding to prostate cancer cells and showed promising imaging results in a prostate tumor mouse model.
Article
Food Science & Technology
Le Ba Vinh, Yoo Kyong Han, Si Young Park, Young Jun Kim, Nguyen Viet Phong, Eunji Kim, Bong-geun Ahn, Yong Woo Jung, Youngjoo Byun, Young Ho Jeon, Ki Yong Lee
Summary: In our research, we discovered that an ethanol extract from the roots of Astragalus membranaceus has a significant inhibitory effect on interleukin-33 (IL-33), suggesting potential pharmacological anti-allergic effects.
JOURNAL OF FUNCTIONAL FOODS
(2023)
Article
Geriatrics & Gerontology
Myeong Uk Kuk, Haneur Lee, Eun Seon Song, Yun Haeng Lee, Ji Yun Park, Subin Jeong, Hyung Wook Kwon, Youngjoo Byun, Sang Chul Park, Joon Tae Park
Summary: Senescence is caused by alterations in cellular organelles and is the primary cause of aging and aging-related diseases. Recent studies have revealed that oncogene-induced senescence is driven by activation of serine/threonine protein kinases (AKT1, AKT2, and AKT3). In this study, GDC0068 was found to have a senescence-ameliorating effect by restoring lysosomal and mitochondrial function through modulation of AKT activity.
EXPERIMENTAL GERONTOLOGY
(2023)
Article
Allergy
Seung Won Lee, Hayeon Kim, Youngjoo Byun, Yoo Sang Baek, Cheol Ung Choi, Jae Hyun Kim, Kyungim Kim
Summary: This study examined the association between newly diagnosed atopic dermatitis (AD) in adults and subsequent cardiovascular diseases (CVDs). The results indicated that AD was associated with an increased risk of angina pectoris, myocardial infarction, ischemic and hemorrhagic stroke.
ALLERGY ASTHMA & IMMUNOLOGY RESEARCH
(2023)
Article
Chemistry, Medicinal
Shuang Mei, Su Jiang, Yuting Wang, Han Jing, Peng Yang, Miao-Miao Niu, Jindong Li, Kai Yuan, Yan Zhang
Summary: This study identifies a dual-targeting peptide, AP-1, that effectively inhibits variants of concern (VOCs) of SARS-CoV-2 without impairing host cell viability. The findings suggest that AP-1 could be a promising broad-spectrum agent for treating emerging VOCs of SARS-CoV-2.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Hyeonjun Lee, Ju Yeon Lee, Hyunsoo Jang, Hye Young Cho, Minhee Kang, Sang Hyun Bae, Suin Kim, Eunji Kim, Jaebong Jang, Jin Young Kim, Young Ho Jeon
Summary: By using liquid chromatography-tandem mass spectrometry and nuclear magnetic resonance experiments, we identified new chemical moieties that bind to the target sites of the protein of interest, allowing for reversible binding and protein degradation. This method has the potential to expand the application of PROTAC technology.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Yingying Li, Xiyou Du, Xinru Kong, Yuelin Fang, Zhijing He, Dongzhu Liu, Hang Wu, Jianbo Ji, Xiaoye Yang, Lei Ye, Guangxi Zhai
Summary: This study proposes a novel nanoplatform based on the autophagy cascade to overcome the obstacles in chemo-immunotherapy. The platform combines chemotherapy and starvation therapy to initiate pro-death autophagy and enhance antigen presentation, while also remodeling the immunosuppressive tumor microenvironment. Furthermore, the study discovers a new therapeutic direction for the respiration inhibitor 3-bromopyruvic acid (3BP) in cancer treatment. Overall, this study offers an opportunity to improve antitumor efficacy and boost immune responses.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Bingsi Wang, Mingxu Ma, Yusen Dai, Pengfei Yu, Liang Ye, Wenyan Wang, Chunjie Sha, Huijie Yang, Yingjie Yang, Yunjing Zhu, Lin Dong, Shujuan Wei, Linlin Wang, Jingwei Tian, Hongbo Wang
Summary: Breast cancer is a common malignant tumor in women, and drug resistance remains a clinical challenge. In this study, a novel compound, G-5b, was developed with potent antagonistic and degradation activities comparable to the current drug fulvestrant. G-5b also showed improved stability and solubility. Mechanistically, G-5b engages the proteasome pathway to degrade ER, inhibiting the ER signaling pathway and inducing apoptosis and cell cycle arrest. In animal models, G-5b exhibited superior pharmacokinetics and pharmacodynamics properties. Overall, G-5b is a promising long-acting SERD worthy of further investigation and optimization.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Karoline B. Waitman, Larissa C. de Almeida, Marina C. Primi, Jorge A. E. G. Carlos, Claudia Ruiz, Thales Kronenberger, Stefan Laufer, Marcia Ines Goettert, Antti Poso, Sandra V. Vassiliades, Vinicius A. M. de Souza, Monica F. Z. J. Toledo, Neuza M. A. Hassimotto, Michael D. Cameron, Thomas D. Bannister, Leticia Costa-Lotufo, Joa o A. Machado-Neto, Mauricio T. Tavares, Roberto Parise-Filho
Summary: A series of hybrid inhibitors combining pharmacophores of known kinase inhibitors and benzohydroxamate HDAC inhibitors were synthesized and evaluated for their anticancer activity and pharmacokinetic properties. Compounds 4d-f exhibited promising cytotoxicity against hematological cells and moderate activity against solid tumor models. Compound 4d showed potent inhibition of multiple kinase targets and had stable interactions with HDAC and members of the JAK family. These compounds showed selective cytotoxicity with minimal effects on non-tumorigenic cells and favorable pharmacokinetic profiles.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Michal Sulik, Diana Fontinha, Dietmar Steverding, Szymon Sobczak, Michal Antoszczak, Miguel Prudencio, Adam Huczynski
Summary: This study describes the synthesis of the first-in-class ivermectin derivatives obtained through derivatization of the C13 position, along with the unexpected rearrangement of the macrolide ring. These derivatives show potential for antiparasitic activity and are important for the development of new antiparasitic agents.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Jun Liu, Qiu-Xian Chen, Wen-Fu Wu, Dong Wang, Si -Yu Zhao, Jia-Hao Li, Yi-Qun Chang, Shao-Gao Zeng, Jia-Yi Hu, Yu-Jie Li, Jia-Xin Du, Shu-Meng Jiao, Hai-Chuan Xiao, Qiang Zhang, Jun Xu, Jian-Fu Zhao, Hai -Bo Zhou, Yong-Heng Wang, Jian Zou, Ping-Hua Sun
Summary: A new anti-infective drug strategy has been discovered to attenuate virulence and modulate inflammation caused by drug-resistant Pseudomonas aeruginosa infections. Compound 5f inhibits biofilm formation, macrophage migration, and inflammatory response induced by P. aeruginosa, showing potential as a novel candidate against drug-resistant infections.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Liuzeng Chen, Ke Wang, Lingyun Wang, Wei Wang, Lifan Wang, Jia Li, Xiaohan Liu, Mengya Wang, Banfeng Ruan
Summary: In this study, a series of novel anti-inflammatory compounds were designed and synthesized based on the natural product pterostilbene skeleton. Among them, compound 8 showed the highest activity and exhibited its effects through inhibition of pro-inflammatory cytokines by blocking the NF-KB/MAPK signaling pathway. Compound 8 also demonstrated a good relieving effect on acute colitis in mice and showed good safety in acute toxicity experiments.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Si-Min Liang, Gui-Bin Liang, Hui-Ling Wang, Hong Jiang, Xian-Li Ma, Jian-Hua Wei, Ri-Zhen Huang, Ye Zhang
Summary: A series of novel multi-target antitumor agents were designed, synthesized, and evaluated. Some compounds exhibited significant antitumor activity and one compound showed excellent efficacy, limited toxicity, and low resistance. Further mechanism studies revealed that the compound exerted antitumor effects through multiple pathways.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)