Article
Multidisciplinary Sciences
Asal Moradi, Mohammadreza Abdihaji, Sara Barari Kouchaksaraie, Tabarek Abdulrazaq Alkinani, Aida Mahmoudi, Arash Davoudi, William Dashtmiani, Somayeh Mikaeili Ghezeljeh, Shahrzad Aghajani, Reza Ghasemian, Somayeh Maghsoomi Taramsari, Amitis Majlesi, Zahra Mahdavi Niyaki, Ali Salehzadeh
Summary: The study aimed to fabricate Bi2O3/Gln-TSC nanoparticles and investigate their anticancer mechanism. The results showed that Bi2O3/Gln-TSC had significant cytotoxicity against prostate cancer cells and induced apoptosis.
SCIENTIFIC REPORTS
(2022)
Article
Pharmacology & Pharmacy
Tanzeeba Amin, Rajneesh Paul Sharma, Khalid Bashir Mir, Nancy Slathia, Sonali Chhabra, Dolma Tsering, Pankul Kotwal, Madhulika Bhagat, Utpal Nandi, Raman Parkesh, Kamal K. Kapoor, Anindya Goswami
Summary: This study demonstrates that compound 4h binds to AKT-1 and ERK2, inhibiting their activation by blocking ATP binding, leading to apoptosis induction by disrupting mitochondrial membrane potential. It also shows promising anti-tumor activity in mouse models and cancer cells, and exhibits satisfactory pharmacokinetic behavior, making it a potential lead molecule for breast and colorectal cancer treatment by targeting AKT and ERK1/2 kinases simultaneously.
EUROPEAN JOURNAL OF PHARMACOLOGY
(2023)
Article
Cell Biology
Zheng Xu, Hao Wang, Zhiqiang Qin, Feng Zhao, Liuhua Zhou, Luwei Xu, Ruipeng Jia
Summary: The study revealed that activation of the NLRP3 inflammasome played a vital role in promoting the malignant progression of prostate cancer via the activation of caspase-1, providing potential targets for clinical diagnosis and treatment.
CELL DEATH DISCOVERY
(2021)
Article
Materials Science, Biomaterials
Yanan Xue, Honglin Tang, Guangpeng Chen, Yubin Pan, Da Li, Yuan Ping
Summary: Normal prostate tissues usually have higher zinc levels to maintain their unique citrate-producing metabolism, but zinc levels decrease significantly during prostate tumorigenesis. We developed a DUPA-decorated ZIF8 that can deliver Cas9 editor and sgRNA to increase zinc levels and inhibit the function of ZNT1 in prostate cancer cells. Cas9@ZIF8-DUPA nanocomplexes show excellent prostate tumor-targeting ability and have significant antitumor activity in a mouse model. This platform provides a potential therapeutic strategy for prostate cancer treatment.
BIOMATERIALS SCIENCE
(2023)
Article
Chemistry, Inorganic & Nuclear
Fatemeh Mehraban, Fariba Heidari Esfahani, Zahra Mosayebi Dorcheh, Erfaneh Heidari Esfahani, Mansoureh Azadeh, Ali Salehzadeh
Summary: This study evaluated the cytotoxic effect of GaFe2O4@Ag nanocomposite biosynthesized by Spirulina platensis on breast cancer cell line and investigated its influence on apoptosis pathways. The results showed that the nanocomposite exhibited high cytotoxicity against breast cancer cells and induced apoptosis through activation of apoptosis pathways.
INORGANIC CHEMISTRY COMMUNICATIONS
(2023)
Article
Biochemistry & Molecular Biology
Tzu-Jung Yu, Jun-Ping Shiau, Jen-Yang Tang, Ammad Ahmad Farooqi, Yuan-Bin Cheng, Ming-Feng Hou, Chia-Hung Yen, Hsueh-Wei Chang
Summary: Physapruin A (PHA), a compound extracted from Physalis plants, can induce endoplasmic reticulum stress to regulate proliferation and apoptosis of breast cancer cells, which is associated with oxidative stress.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Plant Sciences
Haoliang Ke, Xiuping Wang, Zhen Zhou, Wang Ai, Zhaoyan Wu, Yingwen Zhang
Summary: The study found that WMN effectively inhibits the growth of 4T1-luc2 breast cancer xenografts in mice and promotes the apoptosis of breast cancer cells by upregulating caspase-3 expression.
JOURNAL OF ETHNOPHARMACOLOGY
(2021)
Article
Chemistry, Medicinal
Paulina Strzyga-Lach, Alicja Chrzanowska, Ewelina Kiernozek-Kalinska, Barbara Zyzynska-Granica, Katarzyna Podsadni, Piotr Podsadni, Anna Bielenica
Summary: Halogenated thiourea derivatives were synthesized and evaluated for cytotoxic activity against various cancer cell lines. These compounds showed favorable selectivity and had better efficacy than cisplatin in most cases. Mechanistic studies revealed that the compounds induced apoptosis, inhibited IL-6 secretion, and increased ROS production in tumor cells. They also affected cell cycle distribution, leading to cell cycle arrest. These findings suggest that these thiourea derivatives have potential as anticancer agents.
ARCHIV DER PHARMAZIE
(2023)
Article
Biochemistry & Molecular Biology
Ikumi Nakashima, Shoji Saito, Eiichi Akahoshi, Shigeki Yagyu, Mitsuko Sugano-Ishihara, Yozo Nakazawa
Summary: Breast cancer is a complex disease with unique molecular subtypes. The combination of tumor-tropic lipid nanoparticles and inducible caspase-9 mRNA shows promise as a potential treatment strategy for refractory breast cancer.
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
(2022)
Article
Oncology
Omaima Mohamed AboulWafa, Hoda Mohamed Gamal El-Din Daabees, Eman Salah Ezz-ElDien
Summary: This study aimed to design, synthesize, and screen novel quinazolinone-based oxobutanenitrile derivatives for their in vitro anti-breast cancer activity. The tested compounds exhibited better EGFR and ARO inhibition than other compounds, and some showed significant overexpression of caspase-9 in treated MCF-7 breast cell line samples. One compound induced the greatest activation of caspase-9, while another compound resulted in pre-G1 apoptosis and cell cycle arrest in MCF-7 and MDA-MB-231 cells. Docking results revealed that one compound had comparable ARO binding affinities to letrozole. Overall, these compounds have therapeutic importance and offer potential for the development of apoptotic quinazolinone-based ARO and EGFR inhibitors.
ANTI-CANCER AGENTS IN MEDICINAL CHEMISTRY
(2022)
Article
Chemistry, Medicinal
Nora Alshuail, Zeyad Alehaideb, Sahar Alghamdi, Rasha Suliman, Hamad Al-Eidi, Rizwan Ali, Tlili Barhoumi, Mansour Almutairi, Mona Alwhibi, Bandar Alghanem, Abir Alamro, Amani Alghamdi, Sabine Matou-Nasri
Summary: The dichloromethane extract from Achillea fragrantissima flowers showed potential therapeutic effects against triple-negative breast cancer by inducing apoptosis.
Article
Pharmacology & Pharmacy
Allan Radaic, Nam E. Joo, Soo-Hwan Jeong, Seong- Yoo, Nicholas Kotov, Yvonne L. Kapila
Summary: The study demonstrated the potential anticancer effects of phosphatidylserine-caped gold nanoparticles on breast and prostate cancer cells by inducing apoptosis, suggesting a novel therapeutic approach for cancer treatment.
Article
Pharmacology & Pharmacy
Nabil A. Alhakamy, Shaimaa M. Badr-Eldin, Hibah M. Aldawsari, Anas Alfarsi, Thikryat Neamatallah, Solomon Z. Okbazghi, Usama A. Fahmy, Osama A. A. Ahmad, Basma G. Eid, Wael Ali Mahdi, Adel F. Alghaith, Sultan Alshehri, Shadab Md
Summary: FLV-loaded emulsomes were formulated and optimized to improve formulation efficiency for prostate cancer treatment. The optimized FLV-loaded emulsomes demonstrated significant antitumor activity in prostate cancer cells.
Review
Chemistry, Multidisciplinary
Fan Yang, Sahana N. Bettadapura, Mark S. Smeltzer, Hua Zhu, Shanzhi Wang
Summary: This review discusses the roles of the gasdermin protein family in anti-cancer functions and various antitumor drugs that could activate the pyroptosis pathways.
ACTA PHARMACOLOGICA SINICA
(2022)
Article
Cell Biology
Li-hao Zhao, Quan Li, Zhi-Jun Huang, Mi-Xue Sun, Jing-jing Lu, Xiao-hua Zhang, Gang Li, Fang Wu
Summary: NSD2 plays an oncogenic role in CRC by regulating H3K36me2 and the expression of multiple oncogenes, making it a promising therapeutic target.
CELL DEATH & DISEASE
(2021)
Article
Biochemistry & Molecular Biology
El-Shaimaa A. Arafa, Manal Ali Buabeid, Waseem Hassan, Ghulam Murtaza, Tahir Ali Chohan, Hammad Ahmed
Summary: The study revealed that paraphenylenediamine (PPD) is a highly toxic compound, causing 100% mortality rate and significant effects on the liver, kidneys, and heart. Virgin Coconut Oil (VCO) as a potential antidote, can significantly reduce mortality rate and have a modulatory effect on organ markers.
CURRENT PHARMACEUTICAL BIOTECHNOLOGY
(2021)
Review
Pharmacology & Pharmacy
Zoya Iqbal, El-Shaimaa A. Arafa, Zaeema Kanwal, Ghulam Murtaza
Summary: Nanotechnology, particularly the use of radiolabeled nanocarriers, has shown promising potential in early diagnosis, accurate detection, and treatment of diseases like cancer. The ability to create nanocarriers for targeted drug delivery and molecular imaging has the potential to greatly influence disease management in the near future. The unique advantages of various imaging modalities, such as PET and SPECT, have played a significant role in visualizing biological processes at molecular and cellular levels non-invasively.
JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
(2021)
Review
Food Science & Technology
Aida Abd El-Wahed, Nermeen Yosri, Hanem H. Sakr, Ming Du, Ahmed F. M. Algethami, Chao Zhao, Ahmed H. Abdelazeem, Haroon Elrasheid Tahir, Saad H. D. Masry, Mohamed M. Abdel-Daim, Syed Ghulam Musharraf, Islam El-Garawani, Guoyin Kai, Yahya Al Naggar, Shaden A. M. Khalifa, Hesham R. El-Seedi
Summary: Wasps can be solitary or social, with social wasps using venom to protect their colonies and solitary wasps using it to capture prey. The bioactive constituents in wasp venom have anticancer, antimicrobial, and anti-inflammatory effects, but challenges remain in synthesizing these compounds.
Article
Biology
Hany H. Arab, Ahmed M. Ashour, Abdulmalik M. Alqarni, El-Shaimaa A. Arafa, Ahmed M. Kabel
Summary: The immunosuppressant cyclosporine A can cause renal damage, while camel milk, as a natural substance, has the potential to alleviate cyclosporine-induced renal injury. Camel milk can lower levels of nephrotoxicity markers, inhibit renal inflammation, and enhance renal antioxidant capacity.
Article
Chemistry, Physical
Ahmed H. Abdelazeem, Asmaa G. Safi El-Din, Hany H. Arab, Mohammed T. El-Saadi, Samir M. El-Moghazy, Noha H. Amin
Summary: Two novel series of compounds were synthesized and evaluated in vitro and in vivo, with compounds 10e and 10c showing the highest activity against COX-2/sEH enzymes. In vivo screening assays confirmed their superior anti-inflammatory and analgesic activity compared to other derivatives.
JOURNAL OF MOLECULAR STRUCTURE
(2021)
Article
Biochemistry & Molecular Biology
Lamya H. Al-Wahaibi, Bahaa G. M. Youssif, Ehab S. Taher, Ahmed H. Abdelazeem, Antar A. Abdelhamid, Adel A. Marzouk
Summary: A novel series of tri-aryl imidazole derivatives carrying benzene sulfonamide moiety were designed for their selective inhibitory activity against hCA IX and XII. Among them, six compounds showed potent and selective CA IX inhibition, with 5g and 5b demonstrating higher antiproliferative activity compared to other tested compounds. Docking studies of these two compounds revealed their favorable binding interactions with CA-IX, similar to that of ligand 9FK. Molecular modeling simulations supported the biological evaluation results.
Article
Engineering, Multidisciplinary
Ahmed Emam, Khaled R. A. Abdellatif, Noha H. Amin, Khaled M. Elokely
Summary: HCV, an RNA virus with no available vaccine, poses challenges for developing effective medications due to genetic differences and mutations leading to drug resistance. Important amino acids affecting ligand recognition have been identified, with mutations potentially impacting ligand affinity, as demonstrated through molecular dynamics simulation studies.
INTERNATIONAL JOURNAL OF MODELLING AND SIMULATION
(2022)
Article
Immunology
Hany H. Arab, Sarah A. Abd El-Aal, Ahmed H. Eid, El-Shaimaa A. Arafa, Ayman M. Mahmoud, Ahmed M. Ashour
Summary: Troxerutin attenuates MTX-induced renal injury by inhibiting inflammation and apoptosis and activating autophagy.
INTERNATIONAL IMMUNOPHARMACOLOGY
(2022)
Review
Multidisciplinary Sciences
El-Shaimaa A. Arafa, Mohamed S. Refaey, Omnia A. M. Abd El-Ghafar, Emad H. M. Hassanein, Ahmed M. Sayed
Summary: Research has shown that certain ginsenosides have therapeutic potential in downregulating p38 MAPK signaling, leading to their pharmacological benefits in various ailments. Studies on individual ginsenosides have focused on their specific molecular mechanisms of action, rather than the effects of whole-plant extracts.
Article
Chemistry, Medicinal
Hany H. Arab, Alzahraa A. Elhemiely, Azza A. K. El-Sheikh, Hana J. Al Khabbaz, El-Shaimaa A. Arafa, Ahmed M. Ashour, Ahmed M. Kabel, Ahmed H. Eid
Summary: The study investigated the potential effects of linagliptin on cadmium-induced testicular impairment. Linagliptin showed positive effects by improving histopathological lesions, sperm count/motility, and serum testosterone levels. These effects were mediated by reducing testicular inflammation, suppressing apoptosis, and enhancing autophagy.
Article
Chemistry, Medicinal
Mohamed A. Abdelgawad, Syed N. A. Bukhari, Arafa Musa, Mohammed Elmowafy, Mohammed H. Elkomy, AbdElAziz A. Nayl, Ahmed H. El-Ghorab, Ibrahim Hotan Alsohaimi, Mohamed Sadek Abdel-Bakky, Ibrahim O. Althobaiti, Hamud A. Altaleb, Hany A. Omar, Ahmed H. Abdelazeem, Mohamed A. Zaki, Mohamed E. Shaker, Heba A. H. Elshemy
Summary: This study designed and synthesized new sulphamethoxazole derivatives and evaluated their inhibitory activities against human carbonic anhydrase IX and XII, revealing that compound S15 may serve as a potential lead for emerging selective cytotoxic compounds targeting hCAs IX and XII.
Article
Chemistry, Medicinal
Hany H. Arab, Hayat A. Abd El Aal, Shuruq E. Alsufyani, Azza A. K. El-Sheikh, El-Shaimaa A. Arafa, Ahmed M. Ashour, Ahmed M. Kabel, Ahmed H. Eid
Summary: In this study, the effect of topiramate on cadmium-induced testicular impairment was investigated. The results showed that topiramate administration improved serum testosterone levels, sperm count/abnormalities, relative testicular weight, and histopathological changes in cadmium-intoxicated rats. The protective effect of topiramate was achieved by suppressing the NLRP3/caspase-1/IL-1 beta cascade, reducing apoptosis, and activating autophagy in the testes.
Article
Immunology
Emad H. M. Hassanein, Wafaa R. Mohamed, Rasha M. Hussein, El-Shaimaa A. Arafa
Summary: Edaravone (ED) was found to have protective effects against methotrexate (MTX)-induced testicular damage by reducing oxidative stress, inflammation, and apoptosis. It also regulated the Akt/p53 signaling pathway and improved steroidogenesis. These findings highlight the potential of ED as a treatment for MTX-induced testicular damage.
INTERNATIONAL IMMUNOPHARMACOLOGY
(2023)
Article
Chemistry, Multidisciplinary
Mohamed A. S. Badawy, Eman K. A. Abdelall, EL-Shaymaa EL-Nahass, Khaled R. A. Abdellatif, Hamdy M. Abdel-Rahman
Summary: In this study, a novel series of benzimidazole derivatives were designed and synthesized, with some compounds showing selective inhibition to COX-2 isozyme. Among them, compound 11b exhibited the strongest inhibitory activity against COX-2 with good anti-inflammatory activity and lower ulcerogenic liability. Molecular docking studies were consistent with the in vitro COX-2 inhibitory activities.
Review
Pharmacology & Pharmacy
El-Shaimaa A. Arafa, Noura T. Shurrab, Manal A. Buabeid
Summary: Chemotherapeutics can cause various toxic effects in the body, but the natural compound tangeretin found in citrus fruits has shown promising antioxidant and anti-inflammatory properties, along with selective toxicity to cancer cells. Tangeretin works through multiple mechanisms to mitigate inflammation and enhance the efficiency of chemotherapy drugs, potentially improving the overall health outcomes for cancer patients.
ADVANCES IN PHARMACOLOGICAL AND PHARMACEUTICAL SCIENCES
(2021)
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)