Article
Pharmacology & Pharmacy
Jing-Quan Wang, Bo Wang, Qiu-Xu Teng, Zi-Ning Lei, Yi-Dong Li, Zhi Shi, Li-Ying Ma, Hong-Min Liu, Zhijun Liu, Zhe-Sheng Chen
Summary: The synthesized compound CMP25 was found to reverse MDR mediated by MRP7 by increasing intracellular accumulation of anticancer drugs and decreasing drug efflux. This suggests that CMP25 could be a useful prototype for designing drugs to combine with conventional anticancer drugs.
BIOCHEMICAL PHARMACOLOGY
(2021)
Article
Cell Biology
Karolina Gronkowska, Sylwia Michlewska, Agnieszka Robaszkiewicz
Summary: The study provides evidence for the role of ABCC subfamily members in the lysosomal sequestration of drugs in paclitaxel-resistant cancer cells.
CELLULAR PHYSIOLOGY AND BIOCHEMISTRY
(2023)
Article
Chemistry, Analytical
Yanyan Ma, Zhanchen Guo, Chuanwen Fan, Jingran Chen, Shuxin Xu, Zhen Liu
Summary: This study developed aptamers that can target ABCG2 and reverse multidrug resistance, showing great potential in cancer diagnosis and treatment. The aptamers can specifically bind to human colorectal cancer stem cells and effectively reverse drug resistance in liver cancer cells.
ANALYTICAL CHEMISTRY
(2022)
Review
Biochemistry & Molecular Biology
Javier Torres-Jimenez, Victor Albarran-Fernandez, Javier Pozas, Maria San Roman-Gil, Jorge Esteban-Villarrubia, Alfredo Carrato, Adriana Rosero, Enrique Grande, Teresa Alonso-Gordoa, Javier Molina-Cerrillo
Summary: Urothelial carcinoma, one of the most prevalent types of cancer worldwide, is experiencing a paradigm shift in its therapeutic landscape with the development of different therapies. Increased knowledge of the pathogenesis and genetic alterations in urothelial carcinoma is also contributing to this transformation.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Oncology
Jing-Quan Wang, Bo Wang, Li-Ying Ma, Zhi Shi, Hong-Min Liu, Zhijun Liu, Zhe-Sheng Chen
Summary: The study found that CP55 efficiently reversed multidrug resistance mediated by ABCC10, increasing the efficacy of ABCC10-substrate anticancer drugs and reducing drug efflux. The potential interactions between CP55 and ABCC10 were predicted through docking analysis, indicating CP55 as a promising therapeutic agent for chemo-resistant cancer related to ABCC10.
EXPERIMENTAL CELL RESEARCH
(2021)
Article
Oncology
Robin Guo, Michael Offin, A. Rose Brannon, Jason Chang, Andrew Chow, Lukas Delasos, Jeffrey Girshman, Olivia Wilkins, Caroline G. McCarthy, Alex Makhnin, Christina Falcon, Kerry Scott, Yuan Tian, Fabiola Cecchi, Todd Hembrough, Deepu Alex, Ronglai Shen, Ryma Benayed, Bob T. Li, Charles M. Rudin, Mark G. Kris, Maria E. Arcila, Natasha Rekhtman, Paul Paik, Ahmet Zehir, Alexander Drilon
Summary: In MET exon 14-altered lung cancers treated with a MET TKI, the genomic mechanisms of primary resistance remain unknown, while MET expression is correlated with treatment benefit.
CLINICAL CANCER RESEARCH
(2021)
Review
Pharmacology & Pharmacy
Noor E. Verhagen, Jan B. Koenderink, Nicole M. A. Blijlevens, Jeroen J. W. M. Janssen, Frans G. M. Russel
Summary: Chronic myeloid leukemia (CML) is a type of blood cancer. Targeted therapy has improved the life expectancy of CML patients, but some patients develop resistance to treatment, possibly due to reduced drug concentrations in cells. This review focuses on drug-transporting proteins involved in the distribution of CML treatment drugs.
Article
Biochemistry & Molecular Biology
Sergei Boichuk, Pavel Dunaev, Ilshat Mustafin, Shinjit Mani, Kirill Syuzov, Elena Valeeva, Firuza Bikinieva, Aigul Galembikova
Summary: This study reports that BGJ398 can restore the sensitivity of ABCB1-overexpressing cancer cells to certain chemotherapeutic agents, improving drug resistance. By inhibiting the function of ABC transporter protein ABCB1, BGJ398 impairs the efflux of chemotherapeutic drugs from cancer cells, leading to increased cell apoptosis.
Review
Biochemistry & Molecular Biology
Manali Tilak, Jennifer Holborn, Laura A. New, Jasmin Lalonde, Nina Jones
Summary: Glioblastoma multiforme (GBM) is a deadly cancer with limited response to existing therapies. Subtypes of GBM with distinct genetic signatures show aberrant activation of signal transduction pathways. Current research focuses on understanding these molecular alterations to develop more efficient targeted therapies.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Toxicology
Alicja Zajdel, Joanna Nycz, Adam Wilczok
Summary: Lapatinib can reverse chemoresistance of breast cancer cells to paclitaxel, enhancing its anticancer activity, and thus may have potential benefits in the treatment of HER2-negative breast cancer.
TOXICOLOGY IN VITRO
(2021)
Article
Oncology
Minoru Horiuchi, Takehiro Uemura, Tetsuya Oguri, Sanae Toda, Sayaka Yamamoto, Yuto Suzuki, Yusuke Kagawa, Kazuki Sone, Satoshi Fukuda, Yuta Mori, Kensuke Fukumitsu, Yoshihiro Kanemitsu, Tomoko Tajiri, Hirotsugu Ohkubo, Masaya Takemura, Yutaka Ito, Ken Maeno, Akio Niimi
Summary: This study found that the ABCC10 rs2125739 variant is associated with the sensitivity of lung cancer cells to paclitaxel and the side effects of nanoparticle albumin-bound paclitaxel treatment.
INVESTIGATIONAL NEW DRUGS
(2022)
Article
Medicine, Research & Experimental
Hui Hua, Jiajia Zeng, Haixin Xing, Yuxin He, Linyu Han, Nasha Zhang, Ming Yang
Summary: This study systematically evaluated the role of genetic variants in A-to-I editing genes on the prognosis of NSCLC patients receiving EGFR-TKIs therapy. The researchers identified several SNPs in the ADAR gene that were significantly associated with patient prognosis and found that silencing ADAR enhanced the sensitivity of NSCLC cells to gefitinib. These findings highlight the importance of A-to-I RNA editing in drug resistance and suggest ADAR as a potential therapeutic target for unresectable NSCLC.
Review
Oncology
Paula Aldaz, Imanol Arozarena
Summary: Glioblastoma (GBM) is the most common and lethal form of malignant brain tumor, and patients typically undergo surgery followed by radiotherapy and chemotherapy. Despite promising preclinical evidence, clinical trials testing the therapeutic potential of tyrosine kinase inhibitors (TKIs) targeting EGFR, PDGF receptors, and other tyrosine kinases have not led to significant breakthroughs in treating GBM over the past two decades. This article critically analyzes the reasons for the failure of TKIs in GBM treatment and proposes alternative approaches for the evaluation of TKIs in GBM patients.
Article
Multidisciplinary Sciences
Diogo Henrique Kita, Nathalie Guragossian, Ingrid Fatima Zattoni, Vivian Rotuno Moure, Fabiane Gomes de Moraes Rego, Sabrina Lusvarghi, Thomas Moulenat, Billel Belhani, Geraldo Picheth, Sofiane Bouacida, Zouhair Bouaziz, Christelle Marminon, Malika Berredjem, Joachim Jose, Marcos Brown Goncalves, Suresh V. Ambudkar, Glaucio Valdameri, Marc Le Borgne
Summary: A new generation of indeno[1,2-b]indole compounds were synthesized and tested as ABCG2 inhibitors, showing potent inhibition activity and ability to fully chemosensitize cancer cells. These compounds exert their effects by stimulating ABCG2 ATPase activity and stabilizing the protein structure.
SCIENTIFIC REPORTS
(2021)
Article
Biochemistry & Molecular Biology
Jianyi Li, Yuntong Lv, Kunpeng Yan, Fengting Yang, Xuewei Chen, Xiwu Gao, Shuyuan Wen, Hongfei Xu, Yiou Pan, Qingli Shang
Summary: The study revealed that ATP-binding cassette transporters (ABCs) play important roles in cyantraniliprole resistance. Inhibition of ABCs increased the toxicity of cyantraniliprole, while overexpression of ABCs in fruit flies enhanced their tolerance to cyantraniliprole. Suppression of specific ABC transporters increased the sensitivity of cyantraniliprole-resistant strains. These findings provide valuable insights for resistance management strategies.
PESTICIDE BIOCHEMISTRY AND PHYSIOLOGY
(2022)
Article
Oncology
Xing-Guo Tang, Ke Lin, Shun-Wen Guo, Yi Rong, Dan Chen, Zhe-Sheng Chen, Feng-Feng Ping, Jin-Quan Wang
Summary: This study confirmed that the increment-Ru1/Dox combination had a synergistic effect in inhibiting tumor growth in a mouse xenograft model. It was found that this combination treatment promoted tumor cell apoptosis and reduced cardiac fibrosis and iron accumulation caused by doxorubicin. Further investigation revealed that doxorubicin regulated iron accumulation via the ferroptosis pathway and the expression of lipid peroxidation-related proteins. Therefore, the increment-Ru1/Dox combination therapy shows promise in reducing the toxic side effects of doxorubicin, especially cardiac injury.
RECENT PATENTS ON ANTI-CANCER DRUG DISCOVERY
(2023)
Review
Pharmacology & Pharmacy
Siyuan Qin, Zhe Zhang, Zhao Huang, Yinheng Luo, Ningna Weng, Bowen Li, Yongquan Tang, Li Zhou, Jingwen Jiang, Yi Lu, Jichun Shao, Na Xie, Edouard C. Nice, Zhe-Sheng Chen, Jian Zhang, Canhua Huang
Summary: Although the clinical benefit from blocking the P-glycoprotein (P-gp/ABCB1) pathway in multidrug resistance (MDR) in cancers remains inconclusive, our study demonstrates that the combined use of chemotherapy and CCT251545 (CCT) displays a robust synergistic effect against MDR cancer cells and suppresses tumor growth and metastasis in vivo. The synergistic activity of CCT is mainly attributed to enhanced uptake of chemotherapeutic agents and cell phenotype changes. Mechanistically, CCT exerts its chemosensitizing effect through Rac1-dependent macropinocytosis.
DRUG RESISTANCE UPDATES
(2023)
Review
Pharmacology & Pharmacy
Jingyi Fan, Kenneth Kin Wah To, Zhe-Sheng Chen, Liwu Fu
Summary: Multidrug resistance (MDR) is when cancer cells become resistant to a wide range of unrelated drugs. This hinders cancer treatment and is a major cause of chemotherapy failure. ABC transporters are frequently overexpressed in MDR cancer cells, promoting drug efflux and reducing drug accumulation. Recent evidence suggests that ABC transporters also regulate the tumor immune microenvironment (TIME) by transporting cytokines, influencing anti-tumor immunity and drug sensitivity. Inhibition of ABC transporter expression or function can enhance the efficacy of immune checkpoint inhibitors by promoting an anticancer immune microenvironment. This review provides an update on current research progress in this field.
DRUG RESISTANCE UPDATES
(2023)
Review
Pharmacology & Pharmacy
Kun Pang, Zhen-Duo Shi, Liu-Ya Wei, Yang Dong, Yu-Yang Ma, Wei Wang, Guang-Yue Wang, Ming-Yang Cao, Jia-Jun Dong, Yu-Ang Chen, Peng Zhang, Lin Hao, Hao Xu, Deng Pan, Zhe-Sheng Chen, Cong-Hui Han
Summary: The PD-1/PD-L1 immune checkpoint plays a crucial role in tumor immune escape, but the main challenges of this therapy are low response rate and acquired resistance, thus further research is needed to improve the treatment outcome.
DRUG RESISTANCE UPDATES
(2023)
Article
Physics, Multidisciplinary
Jiuxiang Zhang, Zhesheng Chen, Jonathan Caillaux, Yannick Klein, Andrea Gauzzi, Azzedine Bendounan, Amina Taleb-Ibrahimi, Luca Perfetti, Evangelos Papalazarou, Marino Marsi
Summary: Time-resolved ARPES provides a method to investigate the band structure and dynamics of excited electronic states in solids. Understanding the orbital character of bands near the Fermi level is crucial for explaining exotic phenomena in quantum materials. By conducting polarization-dependent time-and angle-resolved photoemission spectroscopy and analyzing the photoelectron yield for different crystal orientations, we determine the orbital character of bands above and below the chemical potential in the Dirac semimetal BaNiS2. Our results demonstrate the significance of controlling and understanding matrix elements' effects in time-resolved photoemission spectroscopy for the study of quantum materials.
EUROPEAN PHYSICAL JOURNAL-SPECIAL TOPICS
(2023)
Article
Chemistry, Multidisciplinary
Jiuxiang Zhang, Thibault Daniel Pierre Sohier, Michele Casula, Zhesheng Chen, Jonathan Caillaux, Evangelos Papalazarou, Luca Perfetti, Luca Petaccia, Azzedine Bendounan, Amina Taleb-Ibrahimi, David Santos-Cottin, Yannick Klein, Andrea Gauzzi, Marino Marsi
Summary: In the Dirac semimetal BaNiS2, the Dirac nodes can be moved along the Gamma-M symmetry line in reciprocal space by varying the concentration of adsorbed K atoms. This peculiar feature offers a promising tool for engineering Dirac states at surfaces, interfaces, and heterostructures, as demonstrated by first-principles calculations considering the effect of charge transfer gap.
Article
Biochemistry & Molecular Biology
Gao-Jie Ye, Chao-Yun Cai, Zhuo-Xun Wu, Qiu-Xu Teng, Jing-Quan Wang, Zhe-Sheng Chen, Bo Wang
Summary: Three series of phenylurea indole derivatives were synthesized with potent inhibitory activities on ABCG2. Four phenylurea indole derivatives with extended 7C system showed the most potent ABCG2 inhibition and no inhibition on ABCB1. Further investigation on two compounds revealed that they increased the accumulation of mitoxantrone in ABCG2-overexpressing cells and stimulated the ATP hydrolysis of ABCG2 transporter.
BIOORGANIC CHEMISTRY
(2023)
Article
Oncology
Ruikun Lin, Lei Zhang, Biwei Ye, Yanan Wang, Yi-Dong Li, Hsu Jason, Wenzhen Liu, Ping Hu, Jincan Chen, Zhe-Sheng Chen, Zhuo Chen
Summary: Our study demonstrates a novel approach to treat multidrug resistance in cancer by targeting and inhibition of P-gp using a nanoparticle system. In vitro and in vivo experiments showed that this nanoparticle system significantly enhanced the efficacy of chemotherapy, reversed drug resistance, inhibited cell proliferation, induced apoptosis, and prevented cancer cell metastasis, with no apparent toxicity.
Article
Pharmacology & Pharmacy
Saeed Alqahtani, Jamilah Alnahdi, Razan Almofada, Asma'a bin Hazza, Abdullah Alsultan, Farjah Alqahtani
Summary: This study aimed to investigate the pharmacokinetics of rivaroxaban in real-world patients and determine the factors that may cause differences in its pharmacokinetics. The study found that liver enzymes, body mass index, and albumin concentrations influenced the clearance of rivaroxaban. These results can guide clinicians in the initiation and adjustment of therapeutic regimens.
JOURNAL OF CLINICAL PHARMACOLOGY
(2023)
Article
Oncology
Ruixiang Guo, Huiru Dai, Fuweijian Liu, Minling Liu, Xueying Li, Tingwei Li, Jiehao Liao, Zhe-Sheng Chen, Yuchen Liu, Shuo Fang
Summary: LEF1 has been found to be significantly associated with high histological grade in hepatocellular carcinoma (HCC) and its overexpression is correlated with poor prognosis. LEF1 may regulate the cell cycle, WNT signaling pathway, and NOTCH signaling pathway in HCC. It could serve as a potential drug target for HCC.
RECENT PATENTS ON ANTI-CANCER DRUG DISCOVERY
(2023)
Article
Pharmacology & Pharmacy
Congying Gao, Lei Zhang, Yun Xu, Xiangyu Ma, Peilei Chen, Zhe-Sheng Chen, Liuya Wei
Summary: In this study, the potent histone deacetylase inhibitor I13 was assessed for its effect on chronic myeloid leukemia (CML) cells harboring T315I-mutated and wild-type BCR-ABL. I13 showed strong activity against both types of cells, inducing cell differentiation and suppressing proliferation by causing cell cycle G0/G1-phase accumulation. It was found that I13 blocked the CML signaling pathway by depleting BCR-ABL, resulting in cell differentiation. These findings highlight I13 as a BCR-ABL modulator for overcoming drug resistance caused by T315I-mutated BCR-ABL and have implications for CML therapy development.
FRONTIERS IN PHARMACOLOGY
(2023)
Article
Fisheries
Peng Xu, Kuopeng Cui, Liming Chen, Shaoshu Chen, Zheng Wang
Summary: This study evaluated the potential of Bifidobacterium animalis subsp. lactis BLa80 as a probiotic for Japanese seabass aquaculture. The results showed that BLa80 supplementation improved survival, accelerated growth, enhanced antioxidant capacity, reduced apoptosis, and altered the gut microbiota structure of juvenile Japanese seabass.
AQUACULTURE INTERNATIONAL
(2023)
Article
Pharmacology & Pharmacy
Xuan-Yu Chen, Yi-Dong Li, Yuhao Xie, Lu-Qi Cao, Charles R. Ashby, Hongbing Zhao, Zhe-Sheng Chen
Article
Pharmacology & Pharmacy
Zhijian Wang, Yuhao Xie, Jing-Quan Wang, Yuanhui Cheng, Joshua Fleishman, Zhe-Sheng Chen, Yun Chen
Summary: On January 25, 2022, the FDA approved tebentafusp for the treatment of HLA-A*02:01-positive adult patients with unresectable or metastatic uveal melanoma (mUM). Tebentafusp targets a specific HLA-A*02:01/gp100 complex, activating T cells to induce tumor cell death. Clinical trials have shown positive overall survival and response rates, as well as manageable adverse events. The approval of tebentafusp is groundbreaking due to the limited efficacy of current treatments for mUM.
Article
Pharmacology & Pharmacy
Xing Liu, Gao-Chuan Fang, Hao Lu, Zhen-Duo Shi, Zhe-Sheng Chen, Cong-Hui Han
Summary: On March 23, 2022, the FDA approved Pluvicto (lutetium Lu 177 vipivotide tetraxetan) as the first targeted radioligand therapy for PSMA-positive mCRPC patients. This groundbreaking therapy selectively binds to PSMA, leading to DNA damage and cell death in prostate cancer cells. With its promising mechanism of action and high specificity, it represents an exciting advancement in precision medicine for individualized treatments.