Review
Chemistry, Medicinal
Bharat Goel, Shivani Jaiswal, Shreyans K. K. Jain
Summary: Microtubules are important intracellular targets for anticancer activity. Various drugs, such as paclitaxel and vinblastine, act by altering the dynamics of microtubules. In this study, the potential of indole derivatives as colchicine-binding site inhibitors is reviewed. These derivatives have shown the ability to inhibit cancer cell proliferation, induce apoptosis, and disrupt microtubule formation. Understanding the structure-activity relationship of these compounds could lead to the development of novel and effective cancer therapies.
ARCHIV DER PHARMAZIE
(2023)
Article
Chemistry, Medicinal
Gang Li, Jia-Qiang Wu, Xiaojia Cai, Wen Guan, Zhijun Zeng, Yanghui Ou, Xiaoyun Wu, Jiayu Li, Xiangxiang Fang, Jinling Liu, Yali Zhang, Huamin Wang, Canqiang Yin, Hongliang Yao
Summary: A series of diaryl heterocyclic analogues were synthesized as tubulin polymerization inhibitors. Compound 6y exhibited the highest antiproliferative activity against HCT-116 colon cancer cells and effectively inhibited tubulin polymerization in vitro. It also showed high metabolic stability on human liver microsomes and suppressed tumor growth in a HCT-116 mouse colon model without toxicity. These results suggest that 6y represents a new class of tubulin inhibitors worthy of further investigation.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Yu Hong, Yuan-Yuan Zhu, Qiuqin He, Shuang-Xi Gu
Summary: This review summarizes the recent progress in the development of indole derivatives as tubulin polymerization inhibitors from 2010 to present. It provides useful clues and inspirations for the further design of outstanding inhibitors.
BIOORGANIC & MEDICINAL CHEMISTRY
(2022)
Article
Oncology
Zahra Rezaei, Mehdi Asadi, Mohammad Nazari Montazer, Elnaz Rezaeiamiri, Saeed Bahadorikhalili, Mohsen Amini, Massoud Amanlou
Summary: This study developed a pharmacophore model and used molecular docking to synthesize and evaluate a series of new tubulin inhibitors, finding that compounds with certain structural features exhibited the highest activity.
ANTI-CANCER AGENTS IN MEDICINAL CHEMISTRY
(2022)
Article
Chemistry, Physical
Ashish Ranjan Dwivedi, Vijay Kumar, Ravi Prakash Yadav, Naveen Kumar, Kailash Jangid, Piyush Anand, Deepak Kumar Sharma, Somesh Barnawal, Vinod Kumar
Summary: A series of 4-Phenyl-1,2,3-triazole substituted pyrimidine derivatives were synthesized and evaluated for their anti-proliferative and anti-tubulin activities. AV-6 and AV-14 exhibited activity against three cancer cell lines, with IC50 values ranging from 1.2μM to 5.5μM for AV-6 and from 4.7μM to 1.4μM for AV-14. These compounds showed non-toxicity to normal cells and induced mitochondria-mediated apoptosis. AV-6 displayed significant tubulin polymerization inhibition potential.
JOURNAL OF MOLECULAR STRUCTURE
(2022)
Article
Biochemistry & Molecular Biology
Yichang Ren, Yong Ruan, Binbin Cheng, Ling Li, Jin Liu, Yuyu Fang, Jianjun Chen
Summary: Compound 3b, designed as a tubulin inhibitor targeting the colchicine binding site, showed high antiproliferative activity against HepG-2 cells, with the ability to suppress microtubule polymerization, disrupt dynamics, inhibit cancer cell migration, induce cell cycle arrest and apoptosis. Docking studies indicated its potential as a novel tubulin inhibitor deserving further investigation.
BIOORGANIC & MEDICINAL CHEMISTRY
(2021)
Review
Pharmacology & Pharmacy
Jiaxing Wang, Duane D. Miller, Wei Li
Summary: This review summarizes the crystal structures of tubulin in complexes with various CBSIs, aiming to facilitate the discovery of new generations of tubulin inhibitors.
DRUG DISCOVERY TODAY
(2022)
Article
Pharmacology & Pharmacy
Celina de Jesus Guimaraes, Teiliane Rodrigues Carneiro, Marisa Jadna Silva Frederico, Guilherme G. C. de Carvalho, Matthew Little, Valder N. Freire, Victor L. B. Franca, Daniel Nascimento do Amaral, Jessica de Siqueira Guedes, Eliezer J. Barreiro, Lidia Moreira Lima, Francisco W. A. Barros-Nepomuceno, Claudia Pessoa
Summary: LASSBio-1920 was synthesized to overcome the poor solubility of its natural precursor, CA4. The compound exhibited cytotoxic potential against human colorectal cancer cells and non-small cell lung cancer cells. It induced apoptosis and had enzyme-substrate interactions similar to other tyrosine kinase inhibitors. LASSBio-1920 showed good absorption and high CNS permeability, and accumulated in various organs. The obtained pharmacokinetic parameters will guide further in vivo studies on its antitumor potential.
Article
Biochemistry & Molecular Biology
Magdalena Peruzynska, Aleksandra Borzyszkowska-Ledwig, Jacek G. Sosnicki, Lukasz Struk, Tomasz J. Idzik, Gabriela Maciejewska, Lukasz Skalski, Katarzyna Piotrowska, Pawel Lukasik, Marek Drozdzik, Mateusz Kurzawski
Summary: This study successfully obtained a mitotic-specific inhibitor with high antiproliferative activity and selectivity through structural modifications. By inhibiting tubulin polymerization in a dose-dependent manner, aberrant mitotic spindle formation was induced, leading to cell cycle arrest and apoptosis.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Biochemistry & Molecular Biology
XiaoYang Li, HuanXian Wu, Kai-Wen Feng, JiaHuan Xu, Shaoyu Wu, Zhong-Zhen Zhou, Xiao-Fang Li
Summary: In this study, nineteen TH03 analogues were designed and synthesized as tubulin colchicine-binding site inhibitors with potent antiproliferative activities. Among these analogues, 3,5-dimethoxyphenylpyridines 8j with a 4-methoxybenzyl aniline side-chain and trimethoxyphenylpyridine 8o with a 4-methyl-N-methyl aniline side-chain showed the best antiproliferative activities against glioma, colon carcinoma, and lung cancer. These compounds exhibited lower cytotoxicity towards normal cells and higher antiproliferative activities against specific cancer cell lines. Further investigations revealed that 8o exhibited higher tubulin polymerization inhibitory activity and induced cell cycle arrest and cellular apoptosis by disrupting the microtubule network.
BIOORGANIC & MEDICINAL CHEMISTRY
(2022)
Article
Chemistry, Multidisciplinary
Mayank, Ashutosh Singh, Kumar Udit Saumya, Mayank Joshi, Navneet Kaur, Neha Garg, Narinder Singh
Summary: 4H-Chromene derivatives are potential anticancer compounds that bind to the colchicine binding site of tubulin protein. The 2-amino-4-phenyl-4H-benzo[h]chromene-3-carbonitrile-based 4H-chromenes scaffold has a significant impact on tubulin proteins. Understanding the interaction pattern of these compounds against various tubulin isoforms is important for selective targeting of cancer cells. Structural modification can potentially enhance the selective targeting ability of these molecules.
NEW JOURNAL OF CHEMISTRY
(2023)
Article
Chemistry, Medicinal
Ya-Xin Sun, Jian Song, Li-Jun Kong, Bei-Bei Sha, Xin-Yi Tian, Xiu-Juan Liu, Tao Hu, Ping Chen, Sai-Yang Zhang
Summary: This study designed a series of novel bis-substituted aromatic amide dithiocarbamate derivatives as tubulin inhibitors with potential anticancer activities. Among them, compound 20q exhibited the most potent antiproliferative activity and was identified as a tubulin inhibitor targeting the colchicine binding site.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Chemistry, Medicinal
Xiang-Yu Yan, Jia-Fu Leng, Ting-Ting Chen, Yong-Jun Zhao, Ling-Yi Kong, Yong Yin
Summary: A series of novel diphenylamine derivatives were synthesized and evaluated for their anti-proliferative activities against human cancer cell lines. Among them, compound 5f exhibited promising anti-proliferative activity against HT29 cells and showed inhibitory effects on cancer cell migration, colony formation, and angiogenesis. Further studies revealed that compound 5f inhibited tubulin polymerization, arrested HT29 cell cycle, induced cell apoptosis, and inhibited tumor growth in animal models. The compound also demonstrated good pharmacokinetic properties. These findings suggest that compound 5f has potential as an antitumor candidate and warrants further investigation.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Chemistry, Medicinal
Yingying Kang, Yuanyuan Pei, Jinling Qin, Yixin Zhang, Yongtao Duan, Hua Yang, Yongfang Yao, Moran Sun
Summary: A library of new pyrimidine analogs was synthesized and compound K10 showed the most potent activity against four cancer cell lines, inhibiting microtubule polymerization and inducing apoptosis in HepG2 cells. It also inhibited the migration and invasion of HepG2 cells. Overall, this study suggests that the tubulin polymerization inhibitor incorporating pyrimidine and the 3,4,5-trimethoxyphenyl ring may be a promising candidate for cancer therapy.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2023)
Review
Chemistry, Medicinal
Fatima Naaz, Kumari Neha, Md Rafi Haider, Syed Shafi
Summary: Indole-based tubulin inhibitors are compounds that disrupt the dynamic equilibrium of microtubule polymerization and depolymerization. Indole moiety is significant for developing new drug candidates for cancer therapy. Synthetic indole derivatives with antitubulin activity have been identified and reported in the past decade, showcasing diverse structure-activity relationships and biological activities.
FUTURE MEDICINAL CHEMISTRY
(2021)
Article
Oncology
Ashish Ranjan Dwivedi, Suraj Singh Rawat, Vijay Kumar, Naveen Kumar, Vinay Kumar, Ravi Prakash Yadav, Somesh Baranwal, Amit Prashad, Vinod Kumar
Summary: The study focuses on developing anticancer agents targeting tubulin protein by synthesizing and screening benzotriazole-substituted 2-phenyl quinazolines. The compounds ARV-2 and ARV-3 demonstrate potent antiproliferative activities and induce mitochondria-mediated apoptosis.
CURRENT CANCER DRUG TARGETS
(2023)
Article
Chemistry, Physical
Pavneet Kaur, Priyanka Sharma, Vinod Kumar, Dinkar Sahal, Rakesh Kumar
Summary: An operationally simple three-component coupling reaction of THIQ, aldehydes, and indoles or indole-3-carboxylic acids was successfully achieved using chitosan-ionic liquid supported FeCl3 (chitIL@FeCl3) as a recyclable catalyst. The waste-free approach provided rapid access to biologically important THIQ-indole hybrids without the need for any additive or ligand. The synthesized hybrids showed potent antiplasmodial activity against Plasmodium falciparum strains and demonstrated potential as new antimalarial agents with a novel mechanism of action.
JOURNAL OF MOLECULAR STRUCTURE
(2023)
Article
Biochemical Research Methods
Ramkaran Ramkaran, Ravindra K. K. Rawal, Praveen K. K. Gupta, Bhupinder Kumar, Rohit Bhatia
Summary: The severity and prevalence of cancer in modern time are a huge global health burden. Continuous efforts are being made toward the development of newer therapeutic candidates to treat and manage this ailment. In this study, a series of sixteen dihydropyrimidinone derivatives were synthesized and evaluated for their cytotoxic activity against breast cancer, lung cancer, and colon cancer cell lines. Compounds 5D and 5P showed the most potent cytotoxic activity and better inhibition of tubulin polymerization compared to the standard drug colchicine. Molecular docking analysis revealed significant interactions between compounds 5D and 5P and tubulin, suggesting their potential as leads in drug development against cancer.
ASSAY AND DRUG DEVELOPMENT TECHNOLOGIES
(2023)
Article
Biochemistry & Molecular Biology
Rohit Pal, Bhupinder Kumar, P. M. Guruubasavaraja Swamy, Pooja A. Chawla
Summary: A series of substituted-N-(5,6-diphenyl-1,2,4-triazin-3-yl) benzamides were designed, synthesized, and evaluated for their antidepressant-like activity. Compound R:5 and R:9 exhibited potent MAO-A inhibition activity and significant antidepressant effects in FST and TST. ADME and docking studies further confirmed their pharmacological characteristics and binding abilities.
BIOORGANIC CHEMISTRY
(2023)
Review
Pharmacology & Pharmacy
Joyson Paul, Karanvir Singh, Sumit Pannu, Rohit Pal, Shah Alam Khan, Bhupinder Kumar, Md Jawaid Akhtar
Summary: According to the WHO's data, the global cancer burden reached 18.1 million new cases in 2018, resulting in 9.6 million deaths. Pharmaceutical spending accounts for around 19% of the annual R&D cost to discover new anticancer drugs. However, drug resistance and side effects remain major issues. This review compiles and discusses analytical and bioanalytical methods for anticancer drugs, covering cytotoxic drugs and targeted-based drugs. The accuracy and precision of UV-HPLC, LC-MS, and fluorometry HPLC are examined, along with advanced methods such as Au/Pd@rGO@p(L-Cys) and endophytic fungi for drug production. This review aims to support researchers in overcoming the challenges in drug development.
CURRENT PHARMACEUTICAL ANALYSIS
(2023)
Review
Chemistry, Medicinal
Chahat, Rohit Bhatia, Bhupinder Kumar
Summary: Cancer is a dangerous disease and p53 is a well-researched tumor suppressor protein that plays a critical role in maintaining genetic stability and controlling various cellular processes. Abnormalities in p53 contribute to genetic instability and carcinogenesis. Enhancing p53 activity in cancer cells is a promising anticancer strategy. This article discusses the current advancements in anti-tumor activities targeting p53-MDM2 and emphasizes the structure-activity relationship characteristics (SAR).
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Cell Biology
Md Jawaid Akhtar, Shah Alam Khan, Bhupinder Kumar, Pooja Chawla, Rohit Bhatia, Karanvir Singh
Summary: This review discusses the structure, function, and regulation of the NaCT transporter, highlighting the role of citrate in diagnosing diseases such as cancer, diabetes, and fatty liver. The therapeutic potential of synthetic inhibitors against NaCT transporters is also summarized.
MOLECULAR AND CELLULAR BIOCHEMISTRY
(2023)
Article
Environmental Sciences
Kazi Jamil, Nasreem Abdulrazack, Saja Fakhraldeen, Vinod Kumar, Sherain Al-Subiai, Tareq Al-Aati, Hebah Kamal, Farhana Husain, Imtiaz Ahmed, Islam Hussein
Summary: Effective surveillance for epidemic-prone viral diseases is crucial for emergency preparedness. Sewage-based epidemiological studies provide a unique way to monitor the population's health. Our study in Kuwait successfully detected multiple pathogenic viruses in urban sewage samples, demonstrating the country's preparedness for viral disease outbreaks and enhancing its capacity to respond in the future.
ENVIRONMENTAL MONITORING AND ASSESSMENT
(2023)
Review
Biochemistry & Molecular Biology
Gurkaran Singh Baweja, Shankar Gupta, Bhupinder Kumar, Preeti Patel, Vivek Asati
Summary: Parkinson's disease is a neurodegenerative disorder characterized by symptoms such as slow movement, tremors, and stiffness, caused by the loss of dopaminergic neurons in the brain's substantia nigra. The disease is associated with a decrease in dopamine concentration in the brain and can be influenced by genetic and environmental factors. The irregular expression of the MAO-B enzyme, which causes the oxidative deamination of biogenic amines like dopamine, is implicated in Parkinson's disease. Current MAO-B inhibitors have adverse effects, and the development of new inhibitors with minimal side effects is urgently needed. Recent studies have identified potential lead compounds for the development of potent MAO-B inhibitors.
MOLECULAR DIVERSITY
(2023)
Review
Cell & Tissue Engineering
Harsh Vikram Singh, Lakshmana Das, Rhuthuparna Malayil, Tashvinder Singh, Sandeep Singh, Tarun Goyal, Anjana Munshi
Summary: To effectively treat damaged articular chondrocytes, this article reviews the cell culture parameters required for developing an efficient tissue engineering protocol to differentiate autologous MSC in cartilaginous tissue. The development of morphologically and mechanically complex hyaline cartilage at the injury site is crucial for treating osteoarthritic patients. This review aims to shed light on the development of tissue engineering approaches that consider various parameters to regulate chondrogenesis and promote better articular cartilage development for effective osteoarthritis treatment.
REGENERATIVE MEDICINE
(2023)
Article
Neurosciences
Abhilash Ludhiadch, Sandeep Sulena, Sandeep Singh, Sudip Chakraborty, Dixit Sharma, Mahesh Kulharia, Paramdeep Singh, Anjana Munshi
Summary: This study evaluates the association between MPV and PLT count with genetic variation and its impact on the development of ischemic stroke and its subtypes. The results suggest that THPO and ARHGEF3 genes play a significant role in determining MPV values and are associated with platelet activation, aggregation, and cytoskeleton rearrangements. These findings highlight the potential of MPV as a biomarker and therapeutic target for ischemic stroke.
MOLECULAR NEUROBIOLOGY
(2023)
Review
Pharmacology & Pharmacy
Kapil Kumar Goel, Somesh Thapliyal, Rajeev Kharb, Gaurav Joshi, Arvind Negi, Bhupinder Kumar
Summary: This article discusses the structure-activity relationship and development overview of imidazole derivatives as antidepressant drugs, as well as their role in modulating the serotonergic system.
Article
Chemistry, Multidisciplinary
Vijay Kumar, Praval Pratap Singh, Ashish Ranjan Dwivedi, Naveen Kumar, Rakesh Kumar, Subash Chandra Sahoo, Sudip Chakraborty, Vinod Kumar
Summary: A facile methodology without catalysts was developed to selectively functionalize 4,6-diphenylpyrimidin-2(1H)-ones under mild conditions. Cs2CO3 in DMF was used to achieve selectivity towards the O-regioisomer without coupling reagents. A total of 14 regioselective O-alkylated 4,6-diphenylpyrimidines were synthesized in yields of 81-91%. DFT studies showed that the transition state for forming the O-regioisomer is more favorable with Cs2CO3 compared to K2CO3. Furthermore, this method was extended to increase the O/N ratio for alkylation of 2-phenylquinazolin-4(3H)-one derivatives.
Review
Oncology
Rhuthuparna Malayil, Yogita Chhichholiya, Kanika Vasudeva, Harsh Vikram Singh, Tashvinder Singh, Sandeep Singh, Anjana Munshi
Summary: Oncogenic metabolic reprogramming affects the abundance of key metabolites regulating signaling and epigenetics. The Warburg effect demonstrates the metabolic vulnerability of cancer cells. Research on metabolism in breast cancer is focused on. The mechanisms underlying metabolic reprogramming in breast cancer are complex and only partially understood.
Review
Oncology
Yogita Chhichholiya, Harsh Vikram Singh, Sandeep Singh, Anjana Munshi
Summary: MicroRNAs (miRNAs) can negatively regulate gene expression by binding to specific mRNAs, which can lead to mRNA degradation or translational repression. Abnormal expression of various miRNAs has been linked to human cancer, including breast cancer (BC), where oncogenic or tumor-suppressor miRNAs regulate important pathways involved in BC development. Genetic variations in miRNA-encoding genes and their target genes contribute to dysregulated gene expression and the progression of BC. Therapeutic approaches for BC include chemotherapy, radiation therapy, surgery, hormone therapy, and targeted biological therapy. This review examines the genetic variations in tumor-suppressor miRNA-encoding genes and their target genes in relation to BC development and prognosis, as well as discusses potential therapeutic interventions targeting these variants for improved disease outcomes.
CLINICAL & TRANSLATIONAL ONCOLOGY
(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)