Article
Chemistry, Inorganic & Nuclear
Sina Katharina Goetzfried, Paul Kapitza, Caroline Marie Gallati, Anna Nindl, Monika Cziferszky, Martin Hermann, Klaus Wurst, Brigitte Kircher, Ronald Gust
Summary: The study evaluated the significance of halido ligands in halido[3-ethyl-4-phenyl-5-(2-methoxypyridin-5-yl)-1-propyl-1,3-dihydro-2H-imidazol-2-ylidene]gold(I) complexes and their reactivity with model nucleophiles. The rapid reactivity of the complexes with selenocysteine suggests a potential correlation with the inhibition of thioredoxin reductase enzyme activity. Interestingly, the high-cytotoxic [(NHC)(2)Au(i)](+) complex distorted the results, indicating a complex relationship between the reactivity of the Au(I)-X bond and biological activity.
DALTON TRANSACTIONS
(2022)
Article
Pharmacology & Pharmacy
Yunlong Lu, Xinyu Sheng, Chao Liu, Zhenlin Liang, Xin Wang, Lijuan Liu, Zhenfan Wen, Zhibin Yang, Qianming Du, Wukun Liu
Summary: The development of selective estrogen receptor degraders (SERDs) has provided new ideas for the clinical treatment of ER-positive advanced breast cancer. This study combines a clinical SERD candidate-G1T48 with a TrxR inhibitor-NHC-Au(I) to form dual targeting complexes, which showed significant antiproliferative effects by degrading ER and inhibiting TrxR activity. The complexes also induced immunogenic cell death (ICD) through ROS, providing evidence for the role of the ER/TrxR-ROS-ICD axis in ER-positive breast cancer.
PHARMACOLOGICAL RESEARCH
(2023)
Article
Chemistry, Applied
Hawraa S. Al-Buthabhak, Valerio Falasca, Yu Yu, Alexandre N. Sobolev, Brian W. Skelton, Stephen A. Moggach, Vito Ferro, Hani Al-Salami, Murray Baker
Summary: Novel complexes of (NHC)Au(SCOR) were synthesised and characterised using spectroscopic techniques and X-ray diffraction. The results indicated that thiocarboxylate ligands have comparable electron donor ability with NHCs. The complexes were stable at room temperature in solid state but showed disproportionation reactions in solution. The thiocarboxylate ligand in (NHC)Au(SCOR) underwent rapid exchange with other thiocarboxylate or thiolate ligands. Furthermore, these complexes exhibited toxicity against cisplatin-resistant ovarian cancer cells.
APPLIED ORGANOMETALLIC CHEMISTRY
(2022)
Article
Chemistry, Multidisciplinary
Rossana Galassi, Lorenzo Luciani, Valentina Gambini, Silvia Vincenzetti, Giulio Lupidi, Augusto Amici, Cristina Marchini, Junbiao Wang, Stefania Pucciarelli
Summary: Phosphane gold(I) compounds were evaluated for screening on breast cancer cell panels, with compounds showing specific environments and components displaying activity. These compounds exhibited strong cytotoxicity, varying enzymatic activities, and binding properties in different cell lines.
FRONTIERS IN CHEMISTRY
(2021)
Review
Biochemistry & Molecular Biology
Iogann Tolbatov, Alessandro Marrone, Cecilia Coletti, Nazzareno Re
Summary: Computational chemistry approaches have become crucial for the development of novel anticancer metallodrugs, with inorganic and organometallic complexes of transition metals showing increasing potential in cancer treatment. Among them, Au(I) and Au(III) compounds are promising candidates due to their strong affinity to protein residues. Predicting metal complexes' properties requires QM computations, while MM, MD, and docking approaches can provide valuable information on their interaction with biomolecular targets.
Article
Chemistry, Medicinal
Zhibin Yang, Mianli Bian, Lin Lv, Xingyu Chang, Zhenfan Wen, Fuwei Li, Yunlong Lu, Wukun Liu
Summary: In this study, a series of novel NHC-Au(I) complexes derived from 4,5-diarylimidazole and glycyr-rhetinic acid (GA) were designed and synthesized. Among them, complex 4C exhibited excellent tumor targeting and antitumor activity, inducing immunogenic cell death (ICD) in hepatocellular carcinoma (HCC) cells. Furthermore, 4C effectively inhibited TrxR enzyme activity, increased reactive oxygen species (ROS) expression, disrupted redox homeostasis, caused mitochondrial dysfunction and endoplasmic reticulum stress (ERS), and led to the release of damage-associated molecular patterns (DAMPs) in HCC cells. Importantly, 4C showed a strong ICD-inducing effect in a vaccination mouse model and activated antitumor immunity in a tumor-bearing C57BL/6 mouse model, consistent with the in vitro results. In conclusion, Au(I) complexes with HCC-targeted capability have the potential for effective tumor immunotherapy.
JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Multidisciplinary
Michele De Franco, Marina Saab, Marina Porchia, Cristina Marzano, Steven P. Nolan, Fady Nahra, Kristof Van Hecke, Valentina Gandin
Summary: A series of NHC-based selenourea Ag(I) and Au(I) complexes were found to possess outstanding anticancer potential, overcoming drug resistance through selective inhibition of TrxR.
CHEMISTRY-A EUROPEAN JOURNAL
(2022)
Article
Chemistry, Multidisciplinary
Junliang Liu, Yusuke Sato, Viveka K. Kulkarni, Angus I. Sullivan, Wenyu Zhang, Cathleen M. Crudden, Jason E. Hein
Summary: Atomically precise gold nanoclusters (AuNCs) are interesting nanomaterials with potential applications in catalysis, bioimaging, and optoelectronics. However, the synthetic methods for AuNCs lack in situ and real-time reaction monitoring, limiting the understanding of their formation mechanisms and hindering optimization. In this study, the utility of HPLC-MS as a monitoring methodology in the synthesis of two NHC-protected gold nanoclusters was demonstrated, providing new insights into the reaction dynamics and rapid optimization.
Article
Multidisciplinary Sciences
Mohamed H. Baren, Seham A. Ibrahim, Munirah M. Al-Rooqi, Saleh A. Ahmed, Mohammed M. El-Gamil, Hend A. Hekal
Summary: In this study, a new series of α-aminophosphonates derivatives were synthesized and evaluated for their anticancer activities. Some compounds exhibited stronger inhibitory activity than Doxorubicin, and were found to potentially function as VEGFR2 and FGFR1 inhibitors.
SCIENTIFIC REPORTS
(2023)
Article
Chemistry, Multidisciplinary
Mingkai Chen, Wenqiang Cao, Junping Wang, Fei Cai, Liwen Zhu, Li Ma, Tianfeng Chen
Summary: This study demonstrates a new strategy to selectively inhibit thioredoxin reductase by constructing an electrophilic center, and confirms that this strategy can significantly improve the anticancer effect.
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
(2022)
Article
Chemistry, Inorganic & Nuclear
Thomas Scattolin, Andrea Piccin, Matteo Mauceri, Flavio Rizzolio, Nicola Demitri, Vincenzo Canzonieri, Fabiano Visentin
Summary: Newly synthesized palladium allyl complexes exhibit lower antiproliferative activity, with similar anticancer activity in two ovarian cancer cell lines, suggesting a different mechanism of action compared to platinum-based anticancer drugs. Some compounds show lower cytotoxicity on normal cells and higher selectivity towards cancer cells. Comparing the IC50 values of NHC/PTA complexes and their trifluoromethyl congeners indicates similar antiproliferative activity against cancer cells, but the absence of the CF3 group decreases selectivity towards them.
Article
Chemistry, Physical
Md. Mahbubur Rahman, Pengcheng Gao, Qun Zhao, Roger Lalancette, Roman Szostak, Michal Szostak
Summary: Cationic Au(i)-NHC complexes have emerged as important catalysts for alkyne & pi;-activation reactions in organic synthesis due to their high stability and reactivity. We report the synthesis and characterization of [Au(NHC)Cl] complexes featuring a new [Au(Np-#)Cl] catalyst, which exhibits higher reactivity and broad applicability. This catalyst has been successfully used in the direct late-stage derivatization of complex pharmaceuticals.
CATALYSIS SCIENCE & TECHNOLOGY
(2023)
Review
Oncology
Ernesto Rufino-Felipe, Raul Colorado-Peralta, Viviana Reyes-Marquez, Hugo Valdes, David Morales-Morales
Summary: In the past 20 years, N-Heterocyclic Carbene (NHC) ligands have been widely used in biological and medicinal chemistry due to their ability to synthesize a vast number of topologies. Fluorinated-NHC transition metal complexes, with fluorine or fluorinated fragments on their NHC moieties, have gained attention for their enhanced biological properties and potential in developing novel metallodrugs, particularly in cancer treatment.
ANTI-CANCER AGENTS IN MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Multidisciplinary
Prafulla K. Behera, Lakshmikanta Maity, Sraddhya Roy, Ananya Das, Priyanka Sahu, Hemanta K. Kisan, Avtar Changotra, Anvarhusein A. Isab, Mohammed Benyounes Fettouhi, Aparajita Bairagi, Nabanita Chatterjee, Joydev Dinda
Summary: This study reports the easy synthesis, structural features, theoretical studies, and extensive bioactivity of Ag and Au compounds prepared from a specific precursor. These compounds exhibit significant cytotoxicity against various cancer cells, particularly lung cancer cells (A549). Further research reveals that the compounds play a role in the mitochondrial reactive oxygen species (ROS)-dependent intrinsic apoptotic pathway.
NEW JOURNAL OF CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Pau Font, Nikolaos V. Tzouras, Argyro T. Papastavrou, Georgios C. Vougioukalakis, Xavi Ribas
Summary: The Lewis-acidic nature and robustness of NHC-Au(I) complexes make them highly effective catalysts for various reactions involving polyunsaturated substrates. Recently, the use of external oxidants or catalysts with pendant coordinating groups has allowed for exploration of Au(I)/Au(III) catalysis. In this study, N-heterocyclic carbene (NHC)-based Au(I) complexes with and without pendant coordinating groups were synthesized and characterized, and their reactivity in the presence of different oxidants was investigated. The results showed that the NHC ligand was oxidized to form NHC=O azolone products when iodosylbenzene-type oxidants were used, and quantitative recovery of gold in the form of Au(0) nuggets was achieved. The synthesized Au(0) nuggets were characterized to have purities above 90% using SEM and EDX-SEM. This study challenges the perceived robustness of the NHC-Au bond and presents a novel methodology for producing Au(0) nuggets.
Article
Biochemistry & Molecular Biology
Mustafa Erkan Ozgur, Ahmet Ulu, Canbolat Gurses, Imren Ozcan, Samir Abbas Ali Noma, Suleyman Koytepe, Burhan Ates
Summary: The present study aimed to determine the cytotoxicity of chromium(III) oxide micro particles (Cr2O3-Ps) in rainbow trout spermatozoa. The results showed that exposure to Cr2O3-Ps led to a decrease in spermatozoa velocities, antioxidant activities, and an increase in DNA damages. These findings are of significant importance for fish reproduction in aquatic environments.
BIOLOGICAL TRACE ELEMENT RESEARCH
(2023)
Article
Chemistry, Physical
Gamze Dik, Ahmet Ulu, Orhan Orcun Inan, Selcuk Atalay, Burhan Ates
Summary: Enzyme immobilization using a novel magnetic carrier improved enzyme stability and activity. The immobilized enzyme displayed enhanced activity under a weak magnetic field and retained significant activity even after multiple cycles of use.
Article
Materials Science, Biomaterials
Aziz Pasahan, Resit Sevimli, Nilufer Kivilcim, Idil Karaca Acari, A. Sebnem Erenler, Selda Sezer, H. Turgut Durmat, Mustafa Huz, Tuba Unver, Turgay Seckin, Nusret Akpolat, Suleyman Koytepe, Ahmet Gultek, Burhan Ates, Ismet Yilmaz
Summary: “Implants with enhanced antibacterial and surface properties were prepared by replacing traditional titanium and titanium alloys in the field of biomedical materials. The chondroitin sulfate sol-gel coatings showed thermal stability and biocompatibility, making them a promising alternative for dental and orthopedic applications.”
INTERNATIONAL JOURNAL OF POLYMERIC MATERIALS AND POLYMERIC BIOMATERIALS
(2023)
Article
Chemistry, Multidisciplinary
Oznur Dogan Ulu, Ali Kurucay, Burhan Ates, Ismail Ozdemir
Summary: In this study, six new Ag(I)-NHC complexes were synthesized and their structures were determined using spectroscopic methods and elemental analysis. These complexes showed good antibacterial activity against two bacterial strains and exhibited promising anticancer effects against a breast adenocarcinoma cell line.
Article
Pharmacology & Pharmacy
Lokman Hekim Tanriverdi, Onural Ozhan, Ahmet Ulu, Azibe Yildiz, Burhan Ates, Nigar Vardi, Haci Ahmet Acet, Hakan Parlakpinar
Summary: The MrgD receptor agonist ALA and Mas receptor agonist AVE0991 have been found to protect against hypertension induced by the renin-angiotensin system. In this study, ALA and AVE0991 were shown to lower blood pressure, improve vascular responses, and reduce inflammation and oxidative stress in Ang II-induced hypertension in rats.
FUNDAMENTAL & CLINICAL PHARMACOLOGY
(2023)
Article
Chemistry, Applied
Idil Karaca Acari, Gamze Dik, Busra Bakar, Ahmet Ulu, Yunus Onal, Burhan Ates
Summary: Immobilizing the alpha-amylase (Amy) enzyme using carbon and graphene quantum dot (QD) structures has been found to significantly enhance its catalytic activity and stability. This study investigated the immobilization of Amy enzyme using QDs prepared from Hypericum perforatum L. flowers (QD-1) and Hypericum capitatum seeds (QD-2). The immobilized enzymes exhibited higher activity efficiency and improved stability against various factors such as metal ions, organic solvents, and trypsin digestion. The findings suggest that these prepared carriers could be valuable for producing stable and active immobilized Amy enzymes for industrial applications.
TOPICS IN CATALYSIS
(2023)
Article
Chemistry, Applied
Tuba Tarhan, Gamze Dik, Ahmet Ulu, Bilsen Tural, Servet Tural, Burhan Ates
Summary: The immobilization strategy of L-ASNase onto Fe3O4@Au-carboxymethyl chitosan magnetic nanoparticles (MNPs) through adsorption was investigated. The immobilized enzyme showed improved biochemical properties, such as optimum pH and temperature, reusability, and thermal stability. The KM and Vmax values indicated good substrate affinity, and the immobilized enzyme retained a high level of activity even after multiple cycles and exposure to high temperatures. This study highlights the potential of MNPs as a support for developing economical and sustainable immobilized enzyme systems.
TOPICS IN CATALYSIS
(2023)
Article
Biochemistry & Molecular Biology
Busra Bakar, Emre Birhanli, Ahmet Ulu, Filiz Boran, Ozfer Yesilada, Burhan Ates
Summary: In this study, the feasibility of immobilizing a Trametes trogii laccase enzyme on Fe3O4/PVP magnetic nanoparticles (MNPs) was explored. The characterization and successful immobilization of laccase enzyme were verified. The Fe3O4/PVP/Lac showed remarkable thermal stability and good operational stability, with high decolorization efficiency of textile dyes in wastewater. This study suggests a promising way to solve the challenges of high cost and low operational stability in laccase-based dye removal.
BIOCATALYSIS AND BIOTRANSFORMATION
(2023)
Article
Biochemistry & Molecular Biology
Yetkin Gok, Parham Taslimi, Betul Sen, Selma Bal, Aydin Aktas, Muhittin Aygun, Morteza Sadeghi, Ilhami Gulcin
Summary: This work focuses on the synthesis, characterization, crystal structure, and biological activity of a new series of PEPPSI type Pd(II)NHC complexes. The complexes were characterized using NMR, FTIR, and elemental analysis, and the crystal structure of complex 1c was determined through X-ray diffraction. The complexes showed potent inhibitory effects on acetyl-cholinesterase, butyrylcholinesterase, and carbonic anhydrases. Molecular docking studies identified specific complexes that exhibited significant inhibition against the target enzymes.
BIOORGANIC CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Hafsa Iqbal, Tashfeen Akhtar, Muhammad Haroon, Aydin Aktas, Ehsaan Tahir, Muhammad Ehsan
Summary: The molecular hybrid approach is used to synthesize thiazole-based chalcones in a simple and cost-effective manner. The synthesized compounds show promising a-amylase inhibition and antioxidant activity. They are also found to be safe for use compared to the standard Triton X. Molecular docking simulations confirm the in vitro amylase inhibition results and identify a compound with the lowest IC50 value.
CHEMISTRY & BIODIVERSITY
(2023)
Article
Chemistry, Inorganic & Nuclear
Ramazan Zengin, Yetkin Gok, Yeliz Demir, Betul Sen, Tugba Taskin-Tok, Aydin Aktas, Ozlem Demirci, Ilhami Gulcin, Muhittin Aygun
Summary: In this study, a series of symmetric and unsymmetric N-heterocyclic carbene (NHC) precursors based on benzimidazol-2-ylidene were synthesized and their structures were characterized. The enzyme inhibition activities of these compounds against acetylcholinesterase (AChE) and carbonic anhydrases (hCAs) were investigated, showing potent inhibitory effects. These results have potential implications for the development of new drug candidates for the treatment of Alzheimer's disease and glaucoma.
JOURNAL OF FLUORINE CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Ayten Behcet, Parham Taslimi, Betul Sen, Tugba Taskin-Tok, Aydin Aktas, Yetkin Gok, Muhittin Aygun, Ilhami Gulcin
Summary: This study synthesized a series of new palladium-based complexes and characterized them using various analysis techniques. The complexes showed strong inhibitory actions against metabolic enzyme activities.
JOURNAL OF BIOCHEMICAL AND MOLECULAR TOXICOLOGY
(2023)
Article
Chemistry, Physical
Kemal Yavuz, Samir Abbas Ali Noma, Betuel Sen, Tugba Taskin-Tok, Aydin Aktas, Burhan Ates, Bilgen Osman, Muhittin Aygun, Yetkin Gok
Summary: This study presents the synthesis of a series of 4-(methylthio)benzyl substituted benzimidazolium salts, which have been found to be potent inhibitors of xanthine oxidase (XO) and acetylcholinesterase (AChE) enzymes. These compounds show promising potential for the treatment of gout and Alzheimer's disease.
JOURNAL OF MOLECULAR STRUCTURE
(2023)
Article
Food Science & Technology
Gamze Dik, Busra Bakar, Ahmet Ulu, Sueleyman Koytepe, Burhan Ates
Summary: The study found that starch nanoparticles (SNPs) can be an effective carrier for immobilizing enzymes, improving the stability and reusability of xylanase (Xyl). The immobilized Xyl on SNPs exhibited enhanced pH stability, thermal stability, and operational stability. Furthermore, Xyl@SNPs demonstrated a lower Km value and increased substrate affinity, leading to improved clarity of orange juice.
Article
Biochemistry & Molecular Biology
Erkan Oner, Yetkin Gok, Yeliz Demir, Tugba Taskin-Tok, Aydin Aktas, Ilhami Gulcin, Serap Yalin
Summary: This study presents the synthesis and characterization of a series of benzimidazolium salts, and investigates their enzyme inhibition abilities against acetylcholinesterase and carbonic anhydrase. The results show that these salts have potent inhibition effects. The pharmacokinetic properties of the compounds were also predicted.
CHEMISTRY & BIODIVERSITY
(2023)
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)
