Article
Chemistry, Medicinal
Sergey A. Dyshlovoy, Dmitry N. Pelageev, Lea S. Jakob, Ksenia L. Borisova, Jessica Hauschild, Tobias Busenbender, Moritz Kaune, Ekaterina A. Khmelevskaya, Markus Graefen, Carsten Bokemeyer, Victor Ph Anufriev, Gunhild von Amsberg
Summary: Synthesized (2-chloroethylthio)-1,4-naphthoquinone derivatives exhibit promising anticancer properties in vitro, suggesting their further development as potential therapeutics for the treatment of castration-resistant prostate cancer.
Article
Endocrinology & Metabolism
Haopeng Xu, Yi Xia, Juan Qin, Jie Xu, Chongyan Li, Yan Wang
Summary: The study demonstrated that LIPUS can improve POF induced by VCD by promoting follicular development, increasing sex hormone secretion, inhibiting excessive follicular atresia, and GCs apoptosis, possibly through increasing Bcl-2 protein expression and decreasing Bax expression in the ovaries.
REPRODUCTIVE BIOLOGY AND ENDOCRINOLOGY
(2021)
Article
Parasitology
Shanming Hu, Yanan Wang, Zhengmao Xu, Yongzhi Zhou, Jie Cao, Houshuang Zhang, Jinlin Zhou
Summary: The study found that the transcription levels of the RhBax gene in ticks increase significantly at all developmental stages, while the transcription levels of both RhBcl-2 and RhBax increase more significantly in the female salivary glands. Inhibiting RhBcl-2 expression significantly inhibited tick feeding, while interference with RhBax had no effect on tick feeding.
PARASITES & VECTORS
(2021)
Article
Biochemistry & Molecular Biology
Qinghan Ren, Guoquan Zhang, Ruiting Yan, Dezheng Zhou, Li Huang, Qianwen Zhang, Wen Li, Guowei Huang, Zhenshu Li, Jing Yan
Summary: Research has shown that folate deficiency in either parents can affect the biological functions of neural cells in offspring. This deficiency can impair the methionine cycle and lead to damage to the central nervous system. The study found that parental folate deficiency caused apoptosis of neural cells in neonatal rats, with the greatest effect seen when both parents were deficient.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Biochemistry & Molecular Biology
Hua-Yuan Tan, Feng-Ming Liang, Wen-Jing Zhang, Yi Zhang, Jun-Hao Cui, Yu-Yu Dai, Xue-Mei Qiu, Wen-Hang Wang, Yue Zhou, Dan-Ping Chen, Cheng-Peng Li
Summary: A series of 1,4-naphthoquinone derivatives were synthesized and their crystal structure was confirmed. One of the derivatives, compound 5i, showed significant cytotoxicity on the A549 cell line. Further experiments revealed that compound 5i induced autophagy and activated the EGFR signal pathway in A549 cells. Molecular docking study identified the potential binding pattern between compound 5i and EGFR tyrosine kinase. This research opens up possibilities for further studies and development of anti-cancer drugs.
Article
Food Science & Technology
Bin Xue, Bei Zhao, Shuangyan Luo, Gang Wu, Xiaodan Hui
Summary: In this study, oat bran was enriched with blackcurrant and blueberry powder to form paste extracts, which were found to significantly inhibit the growth and invasion of hepatocellular carcinoma cells. Mechanistic studies suggested that these extracts induced cell apoptosis through cell cycle arrest and regulation of apoptotic-related protein expressions. The extracts also increased reactive oxygen species levels in the cancer cells via the Nrf2/HO1 signaling pathway. These findings highlight the therapeutic potential of blueberry and blackcurrant-enriched oat bran paste for patients with liver cancer.
JOURNAL OF FUNCTIONAL FOODS
(2022)
Article
Agriculture, Dairy & Animal Science
Reshma S. Raj, D. N. Das, S. Mondal, M. Ashokan, Lakshmi Narasimha Thota, T. Karuthadurai, Nikhil Kumar J. Tej, Kerekoppa P. Ramesha
Summary: This study aimed to analyze the expression of pro-apoptotic BAX and anti-apoptotic BCL-2 genes on lactation performance in Bos indicus and HF crossbred cows during early lactation. The results showed that BCL-2 gene promotes milk production while BAX gene opposes milk production. Bos indicus cows are more sensitive to apoptosis compared to HF crossbreds.
ANIMAL BIOTECHNOLOGY
(2023)
Article
Biotechnology & Applied Microbiology
Yanwu Hu, Haitao Li, Ruili Li, Yue Tian, Zijing Wu
Summary: Schisandrin B, extracted from Schisandra chinensis, demonstrates hepatoprotective effects by preventing D-GalN-induced oxidative damage and apoptosis in L02 cells. This protective mechanism may be achieved through regulating the expression of Bax and Bcl-2.
Article
Cell Biology
Wenwen Cheng, Cifeng Cai, Yifan Xu, Xueqi Xiao, Tiantian Shi, Yueling Liao, Xiaoyi Wang, Shasha Chen, Meiliang Zhou, Zhiyong Liao
Summary: This study identified a signaling pathway associated with hyperglycemia-induced apoptosis and proposed tartary buckwheat flavonoids as a potential treatment.
CELL DEATH & DISEASE
(2023)
Review
Biochemistry & Molecular Biology
Kaiming Li, Mark F. van Delft, Grant Dewson
Summary: Apoptotic cell death plays important roles in physiological and pathological processes, especially in cancer therapy and neurodegenerative diseases. Inhibitors of apoptosis have emerged as a potential strategy to combat pathological cell loss, serving as important research tools due to their mechanisms of action, advantages, and limitations.
Article
Biochemistry & Molecular Biology
Te-Chun Hsia, Shu-Fen Peng, Fu-Shin Chueh, Kung-Wen Lu, Jiun-Long Yang, An-Cheng Huang, Fei-Ting Hsu, Rick Sai-Chuen Wu
Summary: This study demonstrates that BDMC possesses potent anticancer activity on human glioblastoma cells, inhibiting tumor cell proliferation and inducing apoptosis. In a mouse model, BDMC treatment significantly suppresses tumor growth without inducing systemic toxicity.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Biochemistry & Molecular Biology
Adrhyann Jullyanne de Sousa Portilho, Emerson Lucena da Silva, Emanuel Cintra Austregesilo Bezerra, Carinne Borges de Souza Moraes Rego Gomes, Vitor Ferreira, Maria Elisabete Amaral de Moraes, David Rodrigues da Rocha, Rommel Mario Rodriguez Burbano, Caroline Aquino Moreira-Nunes, Raquel Carvalho Montenegro
Summary: The study found that CNN1 can induce cell death and genotoxic effects in leukemia cell lines, showing potential anti-cancer properties.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Chemistry, Organic
Bei Wang, Hong Xu, Fu-Yu Li, Ji-Yu Wang
Summary: A divergent transformation of 2-amino-1,4-quinones was developed for the synthesis of pyrroquinone derivatives and 2-halo-3-amino-1,4-quinones. The mechanism study revealed that both the tandem cyclization and halogenation involved Cu(I)-catalyzed oxidative radical processes. This protocol not only fabricated novel pyrroquinone derivatives with high atom economy but also provided a new method for halogenation through directed C(sp(2))-H functionalization, using CuX (X = I, Br, Cl) as the X source.
JOURNAL OF ORGANIC CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Shuai Zhao, Yichi Zhang, Xiuqin Lu, Han Ding, Bing Han, Xiaoling Song, Huijie Miao, Xuya Cui, Shiyin Wei, Wangrui Liu, Shuxian Chen, Jian Wang
Summary: This study found that CDC20 is highly expressed in HCC and is involved in radio resistance of HCC cells by affecting P53 mutation Bcl-2/Bax signaling pathway, enhancing the sensitivity of HCC to radiation therapy.
INTERNATIONAL JOURNAL OF BIOLOGICAL SCIENCES
(2021)
Article
Biochemistry & Molecular Biology
Akande Rouchidane Eyitayo, Axel Boudier-Lemosquet, Stephane Chaignepain, Muriel Priault, Stephen Manon
Summary: The antiapoptotic protein Bcl-xL plays a crucial role in regulating cell death and survival, but many aspects of its functions are still unclear. Using a model system of cell-free protein synthesis and nanodisc insertion, we found that newly synthesized Bcl-xL could spontaneously insert into nanodiscs. The deletion of the C-terminal α-helix of Bcl-xL prevented its insertion into nanodiscs. We also observed that nanodisc insertion protected Bcl-xL from proteolysis and enhanced the insertion of Bax into nanodiscs, similar to what happens in mitochondria. This cell-free synthesis system with nanodiscs provides a suitable platform to study the molecular interactions between Bcl-xL and Bax during their membrane insertion.
Article
Chemistry, Medicinal
Cesar Augusto Roque-Borda, Mauro de Mesquita Souza Saraiva, Daniel F. M. Monte, Lucas Bocchini Rodrigues Alves, Adriana Maria de Almeida, Taisa Santiago Ferreira, Tulio Spina de Lima, Valdinete Pereira Benevides, Julia Memrava Cabrera, Sunil Claire, Andreia Bagliotti Meneguin, Marlus Chorilli, Fernando Rogerio Pavan, Angelo Berchieri Junior, Eduardo Festozo Vicente
Summary: This study evaluated the effect of microcapsules containing a specific antimicrobial peptide on the colonization and systemic infection of poultry infected with S. Enteritidis. The results showed that the microcapsules significantly reduced the bacterial load of S. Enteritidis in the liver, spleen, and cecum, and also decreased bacterial excretion in feces.
ACS INFECTIOUS DISEASES
(2022)
Article
Engineering, Biomedical
Cesar Augusto Roque-Borda, Mauro de Mesquita Souza Saraiva, Wagner Dias Macedo Junior, Jose Carlos Estanislao Marquez Montesinos, Andreia Bagliotti Meneguin, Anna Beatriz Toledo Borges, Edson Crusca Junior, Saulo Santesso Garrido, Adriana Maria de Almeida, Reinaldo Marchetto, Marlus Chorilli, Angelo Berchieri Junior, Silvio Rainho Teixeira, Fernando Rogerio Pavan, Eduardo Festozo Vicente
Summary: The incorrect use of conventional drugs for intestinal infections has led to the spread of bacterial resistance. Antimicrobial peptide Ctx(Ile21)-Ha has shown effective antimicrobial activity against multidrug-resistant bacteria. However, direct oral application is not feasible due to gastrointestinal degradation. In this study, alginate microparticles loaded with Ctx(Ile21)-Ha peptide were designed to protect it and release it in the intestine, providing a potential solution for combating intestinal pathogens.
Article
Chemistry, Medicinal
Carolina Girotto Pressete, Flavia Pereira Dias Viegas, Thamara Gaspar Campos, Ester Siqueira Caixeta, Joao Adolfo Costa Hanemann, Guilherme Alvaro Ferreira-Silva, Bruno Zavan, Alexandre Ferro Aissa, Marta Miyazawa, Claudio Viegas-Jr, Marisa Ionta
Summary: Melanoma, the most aggressive form of skin cancer, remains highly metastatic and deadly despite advances in immunotherapy and targeted therapies. In this study, we designed hybrid compounds combining pharmacophores from piperine and chlorogenic acid to explore potential antitumoral properties. Among the compounds tested, PQM-277 (3a) showed the highest cytotoxicity on melanoma cells, inhibiting mitosis progression and altering gene expression related to G2/M transition and mitosis onset. Furthermore, compound 3a interacted with the CUL1-RBX1 complex and induced apoptosis by increasing the BAX/BCL2 ratio. These findings suggest that compound 3a has promising potential as an antitumor candidate for melanoma treatment, especially in refractory cases.
Article
Chemistry, Physical
Rafael R. Domeneguetti, Vanessa Y. Sakai, Gustavo F. Perotti, Isabel C. Silva, Agnieszka Tercjak, Hernane S. Barud, Fernando Pavan, Vera R. L. Constantino, Sidney J. Ribeiro
Summary: The effect of different concentrations of Laponite on the structure and properties of bacterial cellulose (BC) membranes was investigated. It was found that an appropriate amount of Laponite can improve the transparency and properties of BC membranes. This opens up new possibilities for the application of nanocomposites in the fields of medical, pharmaceutical, and cosmetics.
APPLIED CLAY SCIENCE
(2023)
Article
Chemistry, Medicinal
Guilherme F. S. Fernandes, Karyn F. Manieri, Andressa F. Bonjorno, Debora L. Campos, Camila M. Ribeiro, Fernanda M. Demarqui, Daniel A. G. Ruiz, Nailton M. Nascimento-Junior, William A. Denny, Andrew M. Thompson, Fernando R. Pavan, Jean L. Dos Santos
Summary: New carbamate derivatives showed potent antimicrobial activity against multidrug-resistant strains of M. tuberculosis with minimal toxicity to host cells and other microorganisms. Molecular docking studies indicated that these compounds may interact with the nitroreductase in a similar manner to pretomanid. These findings highlight the potential of imidazo[2,1-b][1,3]oxazine derivatives in treating multidrug-resistant tuberculosis.
Article
Biochemistry & Molecular Biology
Renan C. F. Leitao, Francisco Silva, Gabriel H. Ribeiro, Isabel C. Santos, Joana F. Guerreiro, Filipa Mendes, Alzir A. Batista, Fernando R. Pavan, Pedro Ivo da S. Maia, Antonio Paulo, Victor M. Deflon
Summary: Gallium and indium octahedral complexes with isoniazid derivative ligands were successfully synthesized. The complexes showed moderate affinity with human serum albumin through hydrophobic interactions. The complexes with H2L2 exhibited higher cytotoxicity against MCF-7 cells, as well as stronger accumulation in MCF-7 and PC-3 cells compared to the non-halogenated complexes. The ligands and metal complexes also demonstrated potent growth inhibitory effects against Mycobacterium tuberculosis.
JOURNAL OF INORGANIC BIOCHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Wilton R. Lustri, Silmara C. Lazarini, Nayara Ap Simei Aquaroni, Flavia A. Resende, Nadia A. Aleixo, Douglas H. Pereira, Bruna Cardinali Lustri, Cristiano Gallina Moreira, Camila M. Ribeiro, Fernando R. Pavan, Douglas H. Nakahata, Adriano M. Goncalves, Nailton M. Nascimento-Junior, Pedro P. Corbi
Summary: This article describes the in vitro antibacterial activity and beta-lactamase inhibition of a novel silver(I) complex with the sulfonamide probenecid (Ag-PROB). The Ag-PROB complex showed significant growth inhibitory activity against various bacteria, including multi-drug resistant uropathogenic E. coli and ESBL-producing bacteria. Molecular docking results suggested the potential molecular mechanism of ESBL inhibition by Ag-PROB. These findings highlight the potential of Ag-PROB as a promising antibacterial agent.
JOURNAL OF INORGANIC BIOCHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Raphael Tristao Cruvinel Silva, Micaela Guidotti-Takeuchi, Jessica Laura Miranda Peixoto, Fernanda Manaia Demarqui, Ananda Paula Mori, Carolyne Ferreira Dumont, Gabriella Rayane Aparecida Ferreira, Gabriele de Menezes Pereira, Daise Aparecida Rossi, Pedro Paulo Corbi, Fernando Rogerio Pavan, Celso de Oliveira Rezende Junior, Roberta Torres de Melo, Wendell Guerra
Summary: This work presents the synthesis, characterization, and antimicrobial activity of four palladium(II) complexes. The complexes showed high antimicrobial activity against Mycobacterium tuberculosis H37Rv strain and Campylobacter jejuni. Complex 2 exhibited the highest activity with a minimum inhibitory concentration (MIC) of 3.28 mu g/mL against M. tuberculosis. Complex 1 significantly reduced the bacterial population and biomass intensity of C. jejuni.
Review
Microbiology
Giulia Polinario, Laura Maria Duran Gleriani Primo, Maiara Alane Baraldi Cerquetani Rosa, Freddy Humberto Marin Dett, Paula Aboud Barbugli, Cesar Augusto Roque-Borda, Fernando Rogerio Pavan
Summary: Tuberculosis and lung cancer are closely related diseases with similar symptoms. Patients with active pulmonary tuberculosis are more likely to develop lung cancer. Therefore, it is crucial to monitor patients after recovery and explore combined therapies to treat both diseases, as well as address the issue of drug resistance.
FRONTIERS IN MICROBIOLOGY
(2023)
Article
Microbiology
Bianca T. M. Oliveira, Thales M. H. Dourado, Patrick W. S. Santos, Tamires A. Bitencourt, Carlos R. Tirapelli, Arnaldo L. Colombo, Fausto Almeida
Summary: This study demonstrated that low concentrations of Candida haemulonii EVs are not recognized by the classical pathway of the oxidative burst generated by macrophages, allowing them to transport virulence factors and evade host immune system. However, high concentrations of EVs activated microbicidal actions in macrophages. Therefore, EVs may contribute to the virulence of Candida haemulonii and could be potential therapeutic targets.
Article
Biochemistry & Molecular Biology
Gregory F. Grawe, Katia M. Oliveira, Celisnolia M. Leite, Tamires D. de Oliveira, Analu R. Costa, Carlos A. F. Moraes, Joao Honorato, Marcia R. Cominetti, Eduardo E. Castellano, Rodrigo S. Correa, Sergio P. Machado, Alzir A. Batista
Summary: This study reports on three new ruthenium(II) complexes and their cytotoxicity against lung and breast cancer cell lines. The results show that these complexes have potential as anticancer agents, with better selectivity than cisplatin. The complexes also exhibit interactions with DNA and human serum albumin, indicating their promising therapeutic effects.
JOURNAL OF INORGANIC BIOCHEMISTRY
(2023)
Article
Chemistry, Inorganic & Nuclear
Julia H. V. Rodrigues, Alexandre B. de Carvalho, Valdenizia R. Silva, Luciano de S. Santos, Milena B. P. Soares, Daniel P. Bezerra, Katia M. Oliveira, Rodrigo S. Corre
Summary: We report on the synthesis and characterization of four new heteroleptic Cu(II) complexes with different ligands. These complexes show moderate interaction with DNA and BSA, and exhibit cytotoxicity against human cancer cells. Among them, complexes 2 and 4 show higher cytotoxicity, suggesting the importance of the phen ligand in enhancing the biological effect of the compounds.
Article
Nutrition & Dietetics
Katiuska Tuttis, Ana Rita Thomazela Machado, Patrick Wellington De Silva Santos, Lusania Maria Greggi Antunes
Summary: Prostate cancer is the second most common cancer worldwide, but there is currently no effective treatment for advanced and metastatic cases. Sulforaphane and vitamin D have shown promise as anticancer agents, but their low bioavailability limits their effectiveness in clinical trials. This study investigated whether combining sulforaphane and vitamin D at clinically relevant concentrations could enhance their cytotoxicity against prostate tumor cells. The results showed that the combination decreased cell viability, induced oxidative stress, DNA damage, and autophagy, and regulated the expression of various proteins involved in cell death pathways. These findings suggest that the combination of sulforaphane and vitamin D has potential as a therapy for prostate cancer and can modulate the JNK/MAPK signaling pathway.
Review
Pharmacology & Pharmacy
Christian Shleider Carnero Canales, Jessica Marquez Cazorla, Andre Henrique Furtado Torres, Eloise T. Monteiro Filardi, Leonardo Delello Di Filippo, Paulo Inacio Costa, Cesar Augusto Roque-Borda, Fernando Rogerio Pavan
Summary: This article reviews the latest scientific evidence on new diagnostic approaches and emerging therapeutic treatments for latent tuberculosis infection (LTBI). New diagnostic tests based on molecular diagnostics, pulmonary immunity, epigenetics, metabolomics, and next-generation MTB antigen-based skin test (TBST) show potential for accurately distinguishing between LTBI and active TB. Therapeutic options include anti-LTBI drugs, anti-resistant TB drugs, and innovative candidates in preclinical and clinical stages. However, further research and clinical evidence are needed to validate the effectiveness and safety of these new approaches.
Article
Biochemistry & Molecular Biology
Carolina P. Bernardes, Neife A. G. Santos, Tassia R. Costa, Danilo L. Menaldo, Flavia M. Sisti, Martin K. Amstalden, Diego L. Ribeiro, Lusania M. G. Antunes, Suely V. Sampaio, Antonio C. Santos
Summary: In this study, the snake-venom-based tripeptide BTX-I was chemically modified to enhance its neurotrophic and neuroprotective effects. The ethyl-esterified peptide BTX-II showed significant improvement in promoting neuritogenesis and upregulating proteins and genes associated with cognitive improvements.
INTERNATIONAL JOURNAL OF PEPTIDE RESEARCH AND THERAPEUTICS
(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)
