Article
Chemistry, Medicinal
Carine M. Abdelmalek, Zexi Hu, Thales Kronenberger, Jenni Kublbeck, Franziska J. M. Kinnen, Salma S. Hesse, Afsin Malik, Mark Kudolo, Raimund Niess, Matthias Gehringer, Lars Zender, Paula A. Witt-Enderby, Darius P. Zlotos, Stefan A. Laufer
Summary: Anticancer drug conjugates that simultaneously target two receptors may overcome the limitations of current cancer treatments. A series of compounds connecting tamoxifen or endoxifen with the EGFR-inhibitor gefitinib exhibit potent anticancer activity in breast cancer cells.
JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Biochemical Research Methods
Basveshwar Gawali, Aishwarya Jala, Jagadeesh Kumar Gangasani, Eswara Rao Puppala, Roshan M. Borkar, V. G. M. Naidu
Summary: This study developed a bioanalytical method for quantification of IITZ-01 and evaluated its pharmacokinetics and metabolic stability in mice. The method showed good accuracy and precision, making it suitable for pre-clinical investigation.
ANALYTICAL BIOCHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Kazuki Miura, Sayaka Kawano, Takahiro Suto, Takaaki Sato, Noritaka Chida, Siro Simizu
Summary: The study found that madangamine A has strong anti-proliferative activity against human cancer cell lines by inhibiting lysosome function.
BIOORGANIC & MEDICINAL CHEMISTRY
(2021)
Article
Engineering, Biomedical
Huifang Wang, Haoyu Bai, Jiafeng Wang, Xuefei Zhou, Hongda Chen, Liying Wang, Huiming Ren, Zimo Liu, Wei Zhuo, Zhuxian Zhou, Jianbin Tang, Zhijie Li, Jigang Wang, Youqing Shen, Tianhua Zhou, Xiangrui Liu
Summary: Effective combination therapies are urgently needed for the treatment of triple-negative breast cancer (TNBC). In this study, researchers found that the autophagy inhibitor hydroxychloroquine (HCQ) and the topoisomerase I inhibitor 7-ethyl-10-hydroxycamptothecin (SN38) exhibit synergistic effects when combined at a specific molar ratio. They further developed a glutathione-responsive self-assembled combination nanoparticle (Combo NP) that integrates the two drugs at the optimized ratio. In TNBC cells, the Combo NP significantly enhanced the cytotoxic effects of SN38 by blocking autophagy, leading to improved therapeutic benefit in metastatic TNBC models.
Article
Pharmacology & Pharmacy
Jiahao Qiu, Xinfa Bai, Wenjing Zhang, Mingxu Ma, Wenyan Wang, Ye Liang, Hongbo Wang, Jingwei Tian, Pengfei Yu
Summary: This study developed a CDK4/6 degrader against TNBC using hydrophobic tagging technology and demonstrated its efficacy and safety through in vitro and in vivo experiments. This suggests the potential of using hydrophobic tags as a strategy to treat TNBC.
FRONTIERS IN PHARMACOLOGY
(2022)
Review
Pharmacology & Pharmacy
Yomna S. Abd El-Aziz, Josef Gillson, Patric J. Jansson, Sumit Sahni
Summary: This review discusses the critical role of autophagy in the progression of triple negative breast cancer (TNBC) and introduces recent therapeutic approaches that target autophagy.
PHARMACOLOGICAL RESEARCH
(2022)
Article
Oncology
Hui Lyu, Defu Hou, Hao Liu, Sanbao Ruan, Congcong Tan, Jiande Wu, Chindo Hicks, Bolin Liu
Summary: This study aims to determine the mechanisms of action of the histone deacetylase inhibitor panobinostat in TNBC and provide a rationale for effective drug combinations against this aggressive disease.
NPJ PRECISION ONCOLOGY
(2023)
Article
Chemistry, Medicinal
Si-Min Liang, Gui-Bin Liang, Hui-Ling Wang, Hong Jiang, Xian-Li Ma, Jian-Hua Wei, Ri-Zhen Huang, Ye Zhang
Summary: A series of novel multi-target antitumor agents were designed, synthesized, and evaluated. Some compounds exhibited significant antitumor activity and one compound showed excellent efficacy, limited toxicity, and low resistance. Further mechanism studies revealed that the compound exerted antitumor effects through multiple pathways.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Biochemistry & Molecular Biology
Shanshan Lin, Xiao Zhang, Zelei Yu, Xiuwang Huang, Jianhua Xu, Yang Liu, Lixian Wu
Summary: This research focused on exploring new PARP inhibitors that are more potent in killing triple negative breast cancer cells and effectively inhibit the overexpression of receptor protein tyrosine kinase.
BIOORGANIC & MEDICINAL CHEMISTRY
(2022)
Article
Medicine, Research & Experimental
Shan Xu, Xin Sun, Leixuan Luo, Yang Yang, Qiuyan Guo, Sheng Tang, Zhiyan Jiang, Yuzhen Li, Jiaqian Han, Wenhui Gan, Feiyi Yang, Xuan Zhang, Yijun Liu, Chuanchuan Sun, Jie He, Meng Liu, Daiying Zuo, Wufu Zhu, Yingliang Wu
Summary: Breast cancer has become the most commonly diagnosed cancer and there is an urgent need for effective therapeutic drugs. In this study, a novel drug XS-2 was designed and synthesized, showing potent anti-tumor activity against breast cancer cells, particularly triple-negative breast cancer (TNBC). XS-2 exhibited strong inhibitory effects on cancer cells both in vitro and in vivo, with low toxicity. Furthermore, XS-2 was found to inhibit cell invasion and migration. These findings suggest that XS-2 has the potential to be developed as a high-efficiency and low-toxicity therapeutic drug for TNBC.
BIOMEDICINE & PHARMACOTHERAPY
(2022)
Article
Chemistry, Physical
Anwesha Pradhan, Debendra Behera, Soumya Ranjan Jena, Siba Soren, Purnendu Parhi, Luna Samanta
Summary: The use of SrSnO3 nanoparticles as a nanocatalyst for near infrared photo-catalytic production of oxidative holes shows promising results in the treatment of Triple Negative Breast Cancer (TNBC). The nanoparticles were found to have efficient anticancer efficacy when triggered by near infrared irradiation, leading to increased release of reactive oxygen species.
JOURNAL OF MOLECULAR STRUCTURE
(2023)
Article
Biochemistry & Molecular Biology
Yu Dong, Guoyuan Zhu, Sheng-Fang Wang, Kristine A. Keon, John L. Rubinstein, Si-Xin Zeng, Shuang Zhang, Qiu-Ling Chen, Jing Fu, Min Li, Han-Ming Shen, Jin-Jian Lu, Xiu-Ping Chen, Jia-Hong Lu
Summary: In this study, a potent autophagy inhibitor called toosendanin was identified, which effectively blocked autophagosome maturation and caused the accumulation of autophagy substrates in various cancer cells. Additionally, toosendanin directly inhibited V-ATPase activity and enhanced anti-cancer activity by blocking chemotherapy-induced protective autophagy.
INTERNATIONAL JOURNAL OF BIOLOGICAL SCIENCES
(2022)
Article
Chemistry, Medicinal
Jian-Jia Liang, Wu-Lin Yu, Liang Yang, Kong-Ming Qin, Yu-Ping Yin, Dan Li, Yuan-Hao Ni, Jing-Jing Yan, Yin-Xian Zhong, Zi-Xin Deng, Kui Hong
Summary: A series of novel derivatives with modification on C24 of MHO7 were synthesized, and compound 4m showed promising antitumor activity against TNBC. It induced apoptosis through the mitochondria pathway and caused cell cycle arrest. In addition, 4m affected the expression of key proteins and inhibited cell metastasis. These findings suggest that modifying C24 of MHO7 is a potential approach for developing new anti-TNBC agents.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Chemistry, Physical
Pilei Si, Haijun Chen, Jiquan Liu, Enzhao Zhang, Chengzhen Li, Jiaojiao Gu, Ruoyan Wang, Wentao Li
Summary: In this study, a potent BRD4 inhibitor, 10-HCPT, was identified for the treatment of triple-negative breast cancer (TNBC). The results showed that 10-HCPT can inhibit the growth of TNBC cells by binding to BRD4 and inducing apoptosis. The study also provided new insights into the potential use of 10-HCPT as a therapy for TNBC.
JOURNAL OF MOLECULAR STRUCTURE
(2022)
Article
Chemistry, Medicinal
Vojtech Novohradsky, Alicia Marco, Lenka Markova, Natalia Cutillas, Jose Ruiz, Viktor Brabec
Summary: In this study, a series of new octahedral iridium(III) complexes Ir1-Ir9 were reported, which showed potential for inhibiting metastasis in triple-negative breast cancer. The results demonstrated that the structural modifications within the complexes strongly influenced their anti-metastatic properties, with complex Ir1 exhibiting the highest activity. Contrary to the effects of the conventional chemotherapy drug doxorubicin, which promoted metastatic properties of TNBC cells, the results suggested that doxorubicin therapy may increase the risk of breast cancer metastasis.
JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Analytical
Vishal Sharad Chaudhari, Aishwarya Jala, Upadhyayula Suryanarayana Murty, Roshan M. Borkar, Subham Banerjee
Summary: An analytical method using UPLC/ESI/MS/MS was developed and validated for the assessment of the pharmacokinetics of active plant constituents in rat plasma. The method was able to quantify quercetin and piperine, and was successfully applied to the study of nanostructured lipid carriers.
ANALYTICAL METHODS
(2022)
Article
Environmental Sciences
Aishwarya Jala, Bincy Varghese, Ratul Dutta, Ramu Adela, Roshan M. Borkar
Summary: Limited information is available about the levels of exposure of paraben and bisphenols emerging from personal care products use in Indian women and the risk associated with it. Liquid chromatography tandem mass spectrometry (LC-MS/MS) was used to determine the concentrations of these substances in PCPs samples and urine samples of young adult females. The concentrations measured in the samples were used to determine the estimated daily intake. The study found that Indian young adult females were exposed to parabens and bisphenols through the use of personal care products, but there were no significant health concerns associated with this exposure.
Article
Multidisciplinary Sciences
Jagadees Kumar Gangasani, Siwaswarup Yarasi, Vegi Ganga Modi Naidu, Jayathirtha Rao Vaidya
Summary: This chapter focuses on the synthesis, characterization, evaluation of anticancer properties, and the journey of triazine-based derivatives towards potential cancer medicine.
PHYSICAL SCIENCES REVIEWS
(2022)
Article
Chemistry, Medicinal
V. V. S. Prasanna Kumari Rayala, Kashyap Ajaybhai Trivedi, Suryanarayana Murthy Upadhyayula, Srinivasu Gunnam, Roshan M. Borkar, P. Radhakrishnanand
Summary: A novel enantiomeric chromatographic technique has been established to estimate the enantiomeric purity of acalabrutinib. The technique showed excellent separation efficiency and high accuracy.
Article
Biochemical Research Methods
Gangasani Jagadeesh Kumar, Sachin Dattram Pawar, Swati Ramesh Pawar, Abraroddin Mumtajoddin Khatib, Anurag Saini, Pintu Das, Kalyan K. Sethi, Pullapanthula Radhakrishnanand, Upadhyayula Suryanarayana Murty, P. L. Sahu, Sachin Dubey, Kapendra Sahu, Awanish Upadhyay, Rajesh Kumar Kori, Pramod Kumar
Summary: This study developed a novel synthetic procedure for carboxy toremifene and characterized it using advanced analytical techniques. It is recommended to use this synthesized carboxy toremifene as a reference material to strengthen WADA-accredited labs in maintaining a clean sports mission during competitions.
DRUG TESTING AND ANALYSIS
(2022)
Article
Biophysics
Aparajita Ghosh, Bishal Rajdev, Nidhi Parihar, Srikanth Ponneganti, Pintu Das, V. G. M. Naidu, P. Radha Krishnanand, U. S. N. Murty, Jagadeesh Kumar, Deepak B. Pemmaraju
Summary: A new lithocholic acid/IR 780 conjugate (LIC) was designed and synthesized for theranostic applications in triple-negative breast cancer. The conjugate exhibited photothermal cytotoxic effect, and when developed into a polymeric nanosystem (LIPNCs), it showed efficient cellular uptake and remarkable heat generation upon NIR light exposure. The in-vitro studies demonstrated high photothermal efficacy and biocompatibility of LIPNCs, making it a potential candidate for image-guided cancer theranostics.
COLLOIDS AND SURFACES B-BIOINTERFACES
(2023)
Article
Plant Sciences
Eswara Rao Puppala, Sai Sudha Yalamarthi, Sunepjungla L. Aochenlar, Neethu Prasad, N. P. Syamprasad, Meenakshi Singh, Satheesh Kumar Nanjappan, V. Ravichandiran, Dinesh Mani Tripathi, Jagadeesh Kumar Gangasani, V. G. M. Naidu
Summary: Mesua Assamica extract exhibits significant anti-inflammatory and antioxidant properties, showing potential therapeutic effects in a murine model of ulcerative colitis induced by chronic restraint stress and DSS. The extract regulates NF-Kappa B/STAT3 and HO-1/Nrf2/SIRT1 signaling pathways, leading to the amelioration of colonic inflammation.
JOURNAL OF ETHNOPHARMACOLOGY
(2023)
Article
Food Science & Technology
Aparajita Ghosh, Bijoyani Ghosh, Nidhi Parihar, Myrthong Ilaweibaphyrnai, Samir R. Panda, Amit Alexander, Naveen Chella, Murty Usn, Naidu Vgm, Jagadeesh Kumar, Deepak B. Pemmaraju
Summary: The novel coronavirus SARS-CoV-2 has presented a significant health challenge worldwide, and there is ongoing exploration of using phytochemicals to combat it. Houttuynia cordata, with its antioxidant, anti-inflammatory, and antiviral properties, has potential as a nutraceutical agent for viruses like HIV, HSV, and influenza.
Article
Environmental Sciences
Aishwarya Jala, Ratul Dutta, Jhansi Venkata Nagamani Josyula, Srinivasa Rao Mutheneni, Roshan M. Borkar
Summary: Urinary biomonitoring is the most accurate method for assessing environmental phenols exposure. This study aimed to investigate the association between environmental phenols exposure and the metabolome of young adult females from India. The study identified seven potential biomarkers and revealed the metabolic pathways altered by environmental phenol exposure. Additionally, an innovative strategy combining urinary metabolomics and machine learning algorithms was proposed for early disease prediction.
Article
Immunology
N. P. Syamprasad, Bishal Rajdev, Siddhi Jain, Samir Ranjan Panda, Eswara Rao Puppala, Pradip Chaudhari, Jayathirtha Rao Vaidya, Gangasani Jagadeesh Kumar, V. G. M. Naidu
Summary: This study finds that AKR1B1 overexpression is linked to inflammation and oxidative stress, contributing to the progression of colitis-associated colon carcinogenesis. Inhibition of AKR1B1 may serve as a promising strategy for preventing colitis-associated colorectal cancer (CA-CRC).
INTERNATIONAL IMMUNOPHARMACOLOGY
(2023)
Article
Pharmacology & Pharmacy
Daya Raju Adye, Sachin B. Jorvekar, Upadhyayula Suryanarayana Murty, Subham Banerjee, Roshan M. Borkar
Summary: Analytical sample preparation techniques are crucial for evaluating chemicals in different biological matrices, and the development of extraction techniques is a contemporary trend in bioanalytical sciences.
Review
Biochemistry & Molecular Biology
Sakshi Arora, Shiva Satija, Aayushi Mittal, Saveena Solanki, Sanjay Kumar Mohanty, Vaibhav Srivastava, Debarka Sengupta, Diptiranjan Rout, Natarajan Arul Murugan, Roshan M. Borkar, Gaurav Ahuja
Summary: The cellular genome encodes genetic information that is dynamically altered due to various insults. The extent of genomic changes is controlled by the balance between DNA repair processes and the genotoxic potential of causative agents. DNA adducts formed by genotoxins can cause significant alterations in cellular processes. Understanding and predicting DNA adducts are important for predicting carcinogenicity. In this review, the use of AI-based modeling in decoding DNA adducts and various computational strategies are discussed.
Article
Biochemistry & Molecular Biology
N. P. Syamprasad, Siddhi Jain, Bishal Rajdev, Samir Ranjan Panda, Jagadeesh Kumar Gangasani, Veerabhadra Swamy Challa, Jayathirtha Rao Vaidya, Gopal C. Kundu, V. G. M. Naidu
Summary: The cardioprotective effect of AKR1B1 inhibitor NARI-29 was evaluated in this study. The results showed that NARI-29 increased the sensitivity of breast cancer cells to Dox, while reducing its toxicity to cardiomyocytes and decreasing the secretion of inflammatory cytokines. Animal experiments also confirmed the protective effect of NARI-29 on Dox-induced cardiac injury.
CHEMICO-BIOLOGICAL INTERACTIONS
(2023)
Article
Food Science & Technology
Aishwarya Jala, Daya Raju Adye, Roshan M. Borkar
Summary: In this study, 108 tea bag samples were collected from the Indian market and analyzed for the presence of 12 perfluoroalkyl substances (PFAS). The results showed that 90% of the samples contained detectable levels of PFAS, with concentrations ranging from...
Article
Biochemical Research Methods
Roshan M. Borkar, Abhinav Kanwal, Bandu Raju, Sai Sharanya Pulimamidi, Agneesh Pratim Das, Subhash Mohan Agarwal, Sanjay K. Banerjee, Ragampeta Srinivas
Summary: Phlorizin (PRZ) is a natural dihydrochalcone that blocks glucose absorption by inhibiting sodium/glucose cotransporters (SGLTs) in the intestine and kidney. It can be used as an adjuvant treatment for type 2 diabetes.
JOURNAL OF MASS SPECTROMETRY
(2023)