Review
Biochemistry & Molecular Biology
Alexandra L. Zakharenko, Olga A. Luzina, Arina A. Chepanova, Nadezhda S. Dyrkheeva, Nariman F. Salakhutdinov, Olga I. Lavrik
Summary: Tyrosyl-DNA phosphodiesterase 1 (TDP1) is an important repair enzyme that removes various covalent adducts from the DNA. Inhibition of TDP1 can sensitize tumor cells to the action of anticancer drugs. This review provides information about methods for determining TDP1 activity and describes inhibitors of TDP1 derived from natural biologically active substances.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Chemistry, Multidisciplinary
Michelle Jessy Mueller, Andrea Dorst, Constanze Paulus, Imran Khan, Simon Sieber
Summary: This paper reports a chemoselective approach to catch and enrich amine-containing natural products, releasing them as underivatized compounds.
CHEMICAL COMMUNICATIONS
(2022)
Review
Pharmacology & Pharmacy
Federico Cerri, Marco Giustra, Yaprak Anadol, Giulia Tomaino, Paolo Galli, Massimo Labra, Luca Campone, Miriam Colombo
Summary: The exploration of natural extracts for pharmaceutical applications, especially plant extracts, is a promising area of medical research. Avicennia marina has been identified as a potential source of natural substances with strong anti-cancer activity. Formulating A. marina extracts into nanoparticles can enhance selectivity towards cancer cells and reduce side effects.
Review
Medicine, Research & Experimental
Sabah Nisar, Tariq Masoodi, Kirti S. Prabhu, Shilpa Kuttikrishnan, Lubna Zarif, Summaiya Khatoon, Shahid Ali, Shahab Uddin, Ammira Al-Shabeeb Akil, Mayank Singh, Muzafar A. Macha, Ajaz A. Bhat
Summary: This review article presents updated literature on different natural products used as chemotherapy or radiation therapy sensitizers in various solid tumors, highlighting the potential and importance of natural products in cancer treatment.
BIOMEDICINE & PHARMACOTHERAPY
(2022)
Article
Food Science & Technology
Amirhossein Abedini, Parisa Sadighara, Mahmood Alizadeh Sani, David Julian McClements
Summary: Biogenic amines (BAs) are compounds produced in foods containing proteins and amino acids by microorganisms, and the use of food additives can have a significant impact on the quality and safety of food products, affecting the production of BAs in different ways.
Article
Food Science & Technology
Eric Wachtel, Matyas A. Bittenbinder, Bas van de Velde, Julien Slagboom, Axel de Monts de Savasse, Luis L. Alonso, Nicholas R. Casewell, Freek J. Vonk, Jeroen Kool
Summary: The cytotoxicity caused by snake venoms is a serious medical problem. Snake venoms target a range of molecular structures to induce cytotoxic effects. A high-throughput assay using fluorescent ECM substrates was developed to monitor ECM degradation by snake venom toxins. Viperid venoms showed higher proteolytic degradation compared to elapid venoms. The assay allows the study of proteolytic activity towards the ECM in vitro for crude and fractionated venoms.
Article
Engineering, Biomedical
Yen Hoon Luah, Tongjin Wu, Lih Feng Cheow
Summary: This article describes a flow cytometry assay that accurately identifies and sorts functional killer-cell subpopulations in co-cultures. The assay uses the detection of an intracellular fluorescent protein from lysed cells on the surface of the lysing killer cells, and can be integrated with single-cell RNA sequencing to analyze molecular pathways associated with cell cytotoxicity. It may help uncover correlates of functional immune responses.
NATURE BIOMEDICAL ENGINEERING
(2023)
Review
Chemistry, Medicinal
Safia Khan, Ammar A. Al-Fadhli, Supriya Tilvi
Summary: Marine sponges in the Red Sea have been found to produce a variety of cytotoxic compounds with activities against different cancer cell lines, showcasing their high biodiversity and self-protective capabilities against predators.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Baji Baba Shaik, Naresh Kumar Katari, Sreekantha Babu Jonnalagadda
Summary: This article summarizes the role of natural products and their analogs in the development of anti-cancer drugs, especially those derived from plants, marine organisms, and microorganisms.
CHEMISTRY & BIODIVERSITY
(2022)
Article
Biochemistry & Molecular Biology
Peter Ertl
Summary: There are significant differences between substituents present in natural products and those found in synthetic molecules. Natural products have more complex structures with oxygen heteroatoms and stereocenters, while synthetic molecules have nitrogen, sulfur heteroatoms and aromatic rings.
BIOORGANIC & MEDICINAL CHEMISTRY
(2022)
Article
Chemistry, Analytical
Chunhui Lu, Si Li, Wei Jiang, Qi Liu, Xiaomei Wang, Chen Yang, Quan Wang
Summary: A rapid and sensitive fluorescence-based immunochromatographic test was developed to quantitatively determine chloramphenicol levels in three food products. The method demonstrated high detection sensitivity and specificity, and could be completed for field detection within 30 minutes.
ANALYTICAL METHODS
(2022)
Article
Infectious Diseases
Lorenza Fagnani, Lisaurora Nazzicone, Fabrizia Brisdelli, Luisa Giansanti, Sara Battista, Roberto Iorio, Sabrina Petricca, Gianfranco Amicosante, Mariagrazia Perilli, Giuseppe Celenza, Pierangelo Bellio
Summary: The study indicates that combining antibiotics with amphoteric surfactants is a promising therapeutic option for infections caused by multidrug-resistant S. aureus. Among the compounds tested, L-prolinol amine-oxide C12NOX showed the most promising results. This research provides valuable insights into combating antibiotic resistance in pathogenic bacteria.
Article
Chemistry, Medicinal
Leonor Ferreira, Joao Morais, Marco Preto, Raquel Silva, Ralph Urbatzka, Vitor Vasconcelos, Mariana Reis
Summary: By screening the cytotoxic activity of cyanobacteria, 6 potential novel bioactive molecules were identified, along with 5 potential cytotoxic compounds. In addition, 9 pheophytin and pheophorbide derivatives were tentatively identified.
Article
Biochemistry & Molecular Biology
Hari Krishna Namballa, Pratibha Anchi, Kesari Lakshmi Manasa, Jay Prakash Soni, Chandraiah Godugu, Nagula Shankaraiah, Ahmed Kamal
Summary: In this study, a series of beta-carboline-cinnamide conjugates were synthesized and one compound, 7h, displayed superior HDAC inhibitory activity and antiproliferative activity against cancer cell lines. Compound 7h showed promising potential for further investigation as a novel anti-cancer drug targeting HDACs.
BIOORGANIC CHEMISTRY
(2021)
Article
Construction & Building Technology
Katarina Simic, Ilya T'Jollyn, Willem Faes, Josue Borrajo Bastero, Jelle Laverge, Michel De Paepe
Summary: Despite being considered outdated, gas-fired heating boiler units remain a common source for residential heating energy demand. Current energy performance assessments for residential buildings lack detailed information and a consistent approach. This research aims to determine the necessary level of modeling detail to predict the performance of gas-fired condensing boilers accurately.
ENERGY AND BUILDINGS
(2021)
Article
Chemistry, Physical
A. Yu Sidorenko, Yu M. Kurban, A. F. Peixoto, N. S. Li-Zhulanov, J. E. Sanchez-Velandia, A. Aho, J. Warna, Y. Gu, K. P. Volcho, N. F. Salakhutdinov, D. Yu Murzin, V. E. Agabekov
Summary: A range of SO3H-functionalized solids were studied as catalysts for the cascade Prins-Ritter reaction. The highest selectivity to the desired products was observed on biochar modified with chlorosulfonic acid. The addition of water significantly increased the reaction rate and selectivity.
APPLIED CATALYSIS A-GENERAL
(2023)
Article
Chemistry, Organic
Ekaterina V. Podrezova, Alina A. Okhina, Artem D. Rogachev, Sergey V. Baykov, Andreas Kirschning, Mekhman S. Yusubov, Natalia S. Soldatova, Pavel S. Postnikov
Summary: In this study, a method for the copper-catalyzed N-arylation of hindered oxazolidinones using diaryliodonium salts was described. The method exhibited good to excellent yields for the arylation of 4-alkyloxazolidinones, including sterically hindered isopropyl- and tert-butyl-substituted ones. The method was efficient for a wide range of diaryliodonium salts - symmetric and unsymmetric as well as ortho-substituted derivatives. The developed approach will make an important contribution to the development and preparation of novel drugs and bioactive molecules containing oxazolidinone moieties.
ORGANIC & BIOMOLECULAR CHEMISTRY
(2023)
Article
Virology
Evgenii S. S. Mozhaitsev, Evgeniy V. V. Suslov, Daria A. A. Rastrepaeva, Olga I. I. Yarovaya, Sophia S. S. Borisevich, Edward M. M. Khamitov, Dmitry S. S. Kolybalov, Sergey G. G. Arkhipov, Nikolai I. I. Bormotov, Larisa N. N. Shishkina, Olga A. A. Serova, Roman V. V. Brunilin, Andrey A. A. Vernigora, Maxim B. B. Nawrozkij, Alexander P. P. Agafonov, Rinat A. A. Maksyutov, Konstantin P. P. Volcho, Nariman F. F. Salakhutdinov
Summary: Although the variola virus has been eradicated, the search for new small molecules with activity against orthopoxviruses is still important, especially due to recent outbreaks of monkeypox. A series of benzoic acid amide derivatives containing an adamantane fragment were obtained, most of which showed activity against vaccinia virus. The leader compound 18a exhibited a high selectivity index (SI = 18,214). The IC50 values of the compounds correlated with the binding energy to the assumed biological target, the p37 viral protein (R-2 = 0.60).
Article
Chemistry, Organic
Alexandra V. Podturkina, Nikolai S. Li-Zhulanov, Konstantin P. Volcho, Nariman F. Salakhutdinov
Summary: Parkinson's disease is a progressive neurodegenerative disorder characterized by movement dysfunction. A new Prottremin derivative was synthesized by opening the epoxide ring with 1-(4-isopropylbenzyl)piperazine, with a product yield of 48% after purification.
Article
Biochemistry & Molecular Biology
Yulia Aleksandrova, Aldar Munkuev, Evgenii Mozhaitsev, Evgenii Suslov, Dmitry Tsypyshev, Kirill Chaprov, Roman Begunov, Konstantin Volcho, Nariman Salakhutdinov, Margarita Neganova
Summary: Novel monoterpene-based hydroxamic acids were synthesized, consisting of compounds with a hydroxamate group directly bound to monoterpene scaffolds or connected through aliphatic or aromatic linkers. Some of these compounds showed powerful HDAC6 inhibitory activity, with a hexa- and heptamethylene linker and (-)-perill fragment exhibiting the most excellent activity. Moderate antiradical activity was also observed. Compounds with an aromatic linker based on para-substituted cinnamic acids demonstrated the ability to suppress aggregation of beta-amyloid peptide 1-42. The lead compound 35a showed neuroprotective effects on in vivo Alzheimer's disease models. This research suggests the potential use of monoterpene-derived hydroxamic acids in Alzheimer's disease treatment.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Biochemistry & Molecular Biology
Dmitry I. Ivankin, Tatyana E. Kornienko, Marina A. Mikhailova, Nadezhda S. Dyrkheeva, Alexandra L. Zakharenko, Chigozie Achara, Johannes Reynisson, Victor M. Golyshev, Olga A. Luzina, Konstantin P. Volcho, Nariman F. Salakhutdinov, Olga I. Lavrik
Summary: A novel series of 3,5-disubstituted thiazolidine-2,4-diones were synthesized and tested for their activity against TDP1. Compounds 20d and 21d showed the highest activity with IC50 values in the submicromolar range. However, these compounds did not exhibit cytotoxicity against HCT-116 (colon carcinoma) and MRC-5 (human lung fibroblasts) cell lines in the concentration range of 1-100 μM, and they also did not sensitize cancer cells to the cytotoxic effect of topotecan.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Biochemistry & Molecular Biology
Tatyana M. M. Khomenko, Alexandra L. L. Zakharenko, Tatyana E. E. Kornienko, Arina A. A. Chepanova, Nadezhda S. S. Dyrkheeva, Anastasia O. O. Artemova, Dina V. V. Korchagina, Chigozie Achara, Anthony Curtis, Johannes Reynisson, Konstantin P. P. Volcho, Nariman F. F. Salakhutdinov, Olga I. I. Lavrik
Summary: A series of new 5-hydroxycoumarin derivatives containing monoterpene moieties were synthesized and shown to have high inhibitory properties against TDP1. The most potent inhibitor was a geraniol derivative 33a with an IC50 of 130 nM. Docking simulations indicated a good fit with TDP1 and blocking of the catalytic pocket. These derivatives sensitized cancer cells to the cytotoxic effect of topotecan.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Editorial Material
Biochemistry & Molecular Biology
Konstantin P. Volcho, Olga I. Lavrik
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Biochemistry & Molecular Biology
Anna A. Shtro, Artem M. Klabukov, Anzhelika V. Garshinina, Anastasia V. Galochkina, Yulia V. Nikolaeva, Tatyana M. Khomenko, Danila E. Bobkov, Aleksey A. Lozhkov, Konstantin V. Sivak, Kirill S. Yakovlev, Andrey B. Komissarov, Sophia S. Borisevich, Konstantin P. Volcho, Nariman F. Salakhutdinov
Summary: This article discusses the mechanism of action of compound K142 against respiratory syncytial virus (RSV), showing that its interaction with RSV surface proteins is crucial for its antiviral activity. However, in vivo studies have indicated weak antiviral activity, suggesting the need for further modifications to enhance its efficacy.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Biochemistry & Molecular Biology
Elmira Gibadullina, Margarita Neganova, Yulia Aleksandrova, Hoang Bao Tran Nguyen, Alexandra Voloshina, Mikhail Khrizanforov, Thi Thu Nguyen, Ekaterina Vinyukova, Konstantin Volcho, Dmitry Tsypyshev, Anna Lyubina, Syumbelya Amerhanova, Anna Strelnik, Julia Voronina, Daut Islamov, Rakhmetulla Zhapparbergenov, Nurbol Appazov, Beauty Chabuka, Kimberley Christopher, Alexander Burilov, Nariman Salakhutdinov, Oleg Sinyashin, Igor Alabugin
Summary: This study explores the biological activity of a family of new hybrid molecules that combine sterically hindered phenols (SHPs) with additional urea/thiourea fragments. It finds that these compounds exhibit cytotoxic activity against tumor cells and have dual properties of pronounced antioxidant activity and increased reactive oxygen species generation. Molecular docking analysis reveals a potential target for these compounds. The most promising compounds can induce apoptosis in cancer cells through the intrinsic mitochondrial pathway.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Chemistry, Analytical
Alina A. Okhina, Tatyana E. Kornienko, Artem D. Rogachev, Olga A. Luzina, Nelly A. Popova, Valery P. Nikolin, Alexandra L. Zakharenko, Nadezhda S. Dyrkheeva, Andrey G. Pokrovsky, Nariman F. Salakhutdinov, Olga I. Lavrik
Summary: We developed and validated an LC-MS/MS method for quantification of OL9-116 in mouse whole blood and studied its pharmacokinetics. OL9-116 was stable in vitro in whole blood. After oral administration of OL9-116 at a dose of 150 mg/kg, the maximum concentration in the blood was reached after 2-4 hours and then distributed and eliminated. Co-administration of topotecan 3 hours after OL9-116 showed the most pronounced antitumor effect compared to simultaneous or individual administration of both compounds.
JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS
(2023)
Article
Oncology
Yulia Aleksandrova, Aldar Munkuev, Evgenii Mozhaitsev, Evgeniy Suslov, Konstantin Volcho, Nariman Salakhutdinov, Margarita Neganova
Summary: Researchers have explored the use of hydroxamic acids with specific chemical structures to address the issue of multidrug resistance in chemotherapy. They found that one particular hydroxamic acid, 18c, can synergize with cisplatin to enhance its anticancer effect and overcome cisplatin resistance.
Article
Biochemistry & Molecular Biology
Jonathan P. Dolan, Sanaz Ahmadipour, Alice J. C. Wahart, Aisling Ni Cheallaigh, Suat Sari, Chatchakorn Eurtivong, Marcelo A. Lima, Mark A. Skidmore, Konstantin P. Volcho, Johannes Reynisson, Robert A. Field, Gavin J. Miller
Summary: This study used virtual screening and experimental validation to discover a new compound that can inhibit the synthesis of alginate in Pseudomonas aeruginosa. The compound showed stronger inhibition than existing inhibitors, offering a potential pathway for the development of new selective antibacterial drugs.
RSC CHEMICAL BIOLOGY
(2023)
Article
Chemistry, Analytical
Nikita Basov, Artem D. Rogachev, Maria A. Aleshkova, Evgeny Gaisler, Yulia S. Sotnikova, Yuri Patrushev, Tatiana G. Tolstikova, Olga I. Yarovaya, Andrey G. Pokrovsky, Nariman F. Salakhutdinov
Summary: The paper introduces an LC-MS/MS-based approach for targeted screening of polar and non-polar metabolites. A synthesized monolithic column and different eluents are used to separate metabolites in two modes. The method allows for detection of a wide range of metabolites in a short time and can identify metabolites related to radiation exposure and tissue damage in dried blood spot samples.
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)
