Article
Biochemistry & Molecular Biology
Ji Su Yang, Naeun Yoon, Mingyu Kong, Byung Hwa Jung, Hyunbeom Lee, Jinyoung Park
Summary: While attempts were made to inhibit cancer cell growth by combining FASN and USP14 inhibitors, there were no synergistic effects on cancer cell death compared to FASN inhibitor alone. Surprisingly, the USP14 inhibitor IU1 did not significantly affect FASN levels in cancer cells, and metabolite changes in IU1-treated cells differed significantly from those in cells treated with the FASN inhibitor Fasnall.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Food Science & Technology
Wenyuan Huang, Xing Guo, Chunyan Wang, Amantay Alzhan, Zhengan Liu, Xiaofeng Ma, Qingyan Shu
Summary: This study found that alpha-linolenic acid (ALA) inhibits the fatty acid synthesis pathway in breast cancer cells, inducing cell apoptosis and inhibiting invasion, metastasis, and cell cycle progression.
JOURNAL OF FUNCTIONAL FOODS
(2022)
Article
Pharmacology & Pharmacy
Ziwen Lu, Zhixin Wang, Zhigang Tu, Hanqing Liu
Summary: The study suggests that the combination of HSP90 inhibitor ganetespib with BTK inhibitor ibrutinib may be an ideal approach for MCL treatment, as it enhances the effects of ibrutinib on MCL cells by promoting cell cycle arrest, inducing cell apoptosis, increasing DNA damage, and inhibiting tumor growth.
FRONTIERS IN PHARMACOLOGY
(2022)
Article
Biochemistry & Molecular Biology
Zoe Day, Alyce J. Mayfosh, Marie-Claire Giel, Yuning Hong, Scott A. Williams, Jascinta P. Santavanond, Thomas F. Rau, Ivan K. Poon, Mark D. Hulett
Summary: This study presents a novel platform for solubilizing fatty acids using amino acids and investigates the tumoricidal activity and mechanism of undecylenic acid. The results demonstrate that the GS-1 formulation, a combination of undecylenic acid and L-Arginine, induces concentration-dependent tumor cell death through a pro-apoptotic mechanism. GS-1 localizes to lipid droplets intracellularly and is taken up by cells via Fatty Acid Transport Protein 2 (FATP2). These findings contribute to the emerging field of fatty acids as potential anti-cancer therapeutics.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Oncology
Yingtong Chen, Ping Yang, Jing Wang, Shuang Gao, Shiyu Xiao, Weilong Zhang, Mingxia Zhu, Yanfang Wang, Xiaoyan Ke, Hongmei Jing
Summary: This study reveals the role of CDC20 in MCL tumorigenesis and the regulatory relationship between p53 and CDC20. It provides a new insight for MCL therapeutics through dual-targeting p53 and CDC20.
EXPERIMENTAL HEMATOLOGY & ONCOLOGY
(2023)
Article
Dermatology
Jennifer R. Landes, Brooke R. Bartley, Stephen A. Moore, Qin He, Rebecca Simonette, Peter L. Rady, Hung Q. Doan, Stephen K. Tyring
Summary: This study demonstrates that Selinexor may provide clinical benefit for patients with metastatic MCC refractory to immune checkpoint inhibitors through inhibition of the lipogenesis pathway. The findings further elucidate Selinexor's mechanism against MCC growth and metastasis.
CLINICAL AND EXPERIMENTAL DERMATOLOGY
(2023)
Article
Pharmacology & Pharmacy
Amineh Ghaderi, Wen Zhong, Mohammad Ali Okhovat, Johanna Aschan, Ann Svensson, Birgitta Sander, Johan Schultz, Thomas Olin, Anders Osterborg, Mohammad Hojjat-Farsangi, Hakan Mellstedt
Summary: The study evaluated the apoptotic effects of a small molecule inhibitor of ROR1 called KAN0441571C in human MCL cells, and found that KAN0441571C alone could induce apoptosis in MCL cells and showed synergistic effects when combined with other anti-tumor drugs. These results suggest that targeting ROR1 with KAN0441571C could be a potential therapeutic approach for MCL.
Article
Biochemistry & Molecular Biology
Fansheng Ran, Yang Liu, Xin Chen, Huijun Zhuo, Changqing Xu, Yuxia Li, Xiaoming Duan, Guisen Zhao
Summary: Ibrutinib and its derivative compound 15c exhibit potent BTK inhibitory activity and antiproliferative effects, with 15c showing higher selectivity and potentially safer treatment for MCL compared to ibrutinib.
BIOORGANIC CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Jingshan Tong, Xiao Tan, Denise Risnik, Man Gao, Xiangping Song, Kaylee Ermine, Liangfang Shen, Shaomeng Wang, Jian Yu, Lin Zhang
Summary: The study shows that inducing BET protein degradation through PROTAC approach can effectively suppress the growth of colorectal cancer by activating DR5-mediated immunogenic cell death. Additionally, DR5 is crucial for the potent antitumor effect of combining BET degradation and anti-PD-1 antibody.
Article
Chemistry, Medicinal
Linling Gan, Zongjie Gan, Yanrong Dan, Yaowei Li, Peiming Zhang, Shanwen Chen, Zaijun Ye, Tao Pan, Chunmei Wan, Xuelian Hu, Yu Yu
Summary: A series of novel TNBG analogues were developed, among which compound 14g exhibited strong inhibitory effects on HepG2 and A549 cells, possibly through the activation of PPARγ expression. In an in vivo xenograft model, 14g effectively reduced tumor growth and demonstrated excellent water solubility.
JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Cell Biology
Kai Xue, Ji-Chuan Wu, Xi-Ya Li, Ran Li, Qun-ling Zhang, Jin-Jia Chang, Yi-Zhen Liu, Chun-Hui Xu, Jia-Ying Zhang, Xiao-Jian Sun, Juan J. Gu, Wei-Jian Guo, Lan Wang
Summary: The study demonstrated that chidamide showed therapeutic effects in rituximab/chemotherapy resistant B-cell lymphoma by inhibiting cell growth, inducing cell death, and activating autophagy pathway. Chidamide targeted BTG1 and FOXO1 genes, regulating autophagy and cell cycle, and enhanced the efficacy when combined with cisplatin in a synergistic manner. These findings provide a theoretical and mechanistic basis for further evaluation of chidamide-based treatment in relapsed and refractory B-cell lymphoma patients.
CELL DEATH & DISEASE
(2021)
Article
Food Science & Technology
Huijin Fan, Yong Guo, Yaonan Zhang, Ning Ding, Meiling Liu, Xiaofeng Ma, Jianhong Yang
Summary: It was found that α-mangostin inhibits the proliferation and migration of osteosarcoma cells by blocking FASN expression, which may serve as a potential target for osteosarcoma treatment.
JOURNAL OF FUNCTIONAL FOODS
(2022)
Article
Oncology
Thomas W. Grunt, Lisa Lemberger, Ramon Colomer, Maria Luz Lopez-Rodriguez, Renate Wagner
Summary: Ovarian cancer cells are highly dependent on lipids and sensitive to FASN inhibitors, with an inability to resist FASN inhibition by increasing uptake of exogenous lipids. Instead, growth arrest is mainly caused by a reduction in the uptake of external fats and low-density lipoproteins.
FRONTIERS IN ONCOLOGY
(2021)
Article
Oncology
Xin-Xin Zeng, Wan-Wei Guo, Jue Shen, Yu-Ying Jiang, Shuang Liu, Xu-Hui Zhang
Summary: REG gamma regulates p-STAT3 expression and downregulates the NF-KB signaling pathway to promote MCL cell apoptosis by negatively regulating STAT3-mediated PSMB5 expression and subsequently upregulating IKB expression.
TRANSLATIONAL CANCER RESEARCH
(2023)
Article
Oncology
Yuheng Hong, Tianyuan Ren, Xiaoxuan Wang, Xia Liu, Yue Fei, Shen Meng, Xu Han, Cong Sun, Hongru Shen, Lanfang Li, Lihua Qiu, Zhengzi Qian, Shiyong Zhou, Huilai Zhang, Xianhuo Wang
Summary: TP53 mutations are associated with poor prognosis in DLBCL, particularly in GCB and UNC subtypes. APR-246 shows anti-tumor effects by restoring binding of mutant p53 to target genes. Mutations in exons 5, 6, and 7 of TP53 are predictors of progression and survival in DLBCL.
Article
Biochemistry & Molecular Biology
Pascal Gelebart, Mihaela Popa, Emmet McCormack
CURRENT PHARMACEUTICAL BIOTECHNOLOGY
(2015)
Article
Multidisciplinary Sciences
Marcus J. G. W. Ladds, Ingeborg M. M. van Leeuwen, Catherine J. Drummond, Su Chu, Alan R. Healy, Gergana Popova, Andres Pastor Fernandez, Tanzina Mollick, Suhas Darekar, Saikiran K. Sedimbi, Marta Nekulova, Marijke C. C. Sachweh, Johanna Campbell, Maureen Higgins, Chloe Tuck, Mihaela Popa, Mireia Mayoral Safont, Pascal Gelebart, Zinayida Fandalyuk, Alastair M. Thompson, Richard Svensson, Anna-Lena Gustavsson, Lars Johansson, Katarina Farnegardh, Ulrika Yngve, Aljona Saleh, Martin Haraldsson, Agathe C. A. D'Hollander, Marcela Franco, Yan Zhao, Maria Hakansson, Bjorn Walse, Karin Larsson, Emma M. Peat, Vicent Pelechano, John Lunec, Borivoj Vojtesek, Mar Carmena, William C. Earnshaw, Anna R. McCarthy, Nicholas J. Westwood, Marie Arsenian-Henriksson, David P. Lane, Ravi Bhatia, Emmet McCormack, Sonia Lain
NATURE COMMUNICATIONS
(2018)
Correction
Multidisciplinary Sciences
Marcus J. G. W. Ladds, Ingeborg M. M. van Leeuwen, Catherine J. Drummond, Su Chu, Alan R. Healy, Gergana Popova, Andres Pastor Fernandez, Tanzina Mollick, Suhas Darekar, Saikiran K. Sedimbi, Marta Nekulova, Marijke C. C. Sachweh, Johanna Campbell, Maureen Higgins, Chloe Tuck, Mihaela Popa, Mireia Mayoral Safont, Pascal Gelebart, Zinayida Fandalyuk, Alastair M. Thompson, Richard Svensson, Anna-Lena Gustavsson, Lars Johansson, Katarina Farnegardh, Ulrika Yngve, Aljona Saleh, Martin Haraldsson, Agathe C. A. D'Hollander, Marcela Franco, Yan Zhao, Maria Hakansson, Bjorn Walse, Karin Larsson, Emma M. Peat, Vicent Pelechano, John Lunec, Borivoj Vojtesek, Mar Carmena, William C. Earnshaw, Anna R. McCarthy, Nicholas J. Westwood, Marie Arsenian-Henriksson, David P. Lane, Ravi Bhatia, Emmet McCormack, Sonia Lain
NATURE COMMUNICATIONS
(2018)
Article
Hematology
Ommoleila Molavi, Peng Wang, Zoulika Zak, Pascal Gelebart, Andrew Belch, Raymond Lai
BRITISH JOURNAL OF HAEMATOLOGY
(2013)
Article
Cell Biology
Peng Wang, Jing Dong Zhang, Fang Wu, Xiaoxia Ye, David Sharon, Mary Hitt, Todd P. McMullen, Samar A. Hegazy, Pascal Gelebart, Jianchang Yang, Yupo Ma, Raymond Lai
CELLULAR SIGNALLING
(2012)
Correction
Cell Biology
Samar A. Hegazy, Abdulraheem Alshareef, Pascal Gelebart, Mona Anand, Hanan Armanious, Robert J. Ingham, Raymond Lai
CELLULAR SIGNALLING
(2013)
Article
Cell Biology
Hanan Armanious, Pascal Gelebart, Mona Anand, Raymond Lai
CELLULAR SIGNALLING
(2013)
Article
Cell Biology
Samar A. Hegazy, Abdulraheem Alshareef, Pascal Gelebart, Mona Anand, Hanan Armanious, Robert J. Ingham, Raymond Lai
CELLULAR SIGNALLING
(2013)
Article
Oncology
Jingdong Zhang, Peng Wang, Mark Dykstra, Pascale Gelebart, David Williams, Robert Ingham, Esther Ekpe Adewuyi, Raymond Lai, Todd McMullen
JOURNAL OF PATHOLOGY
(2012)
Article
Biochemistry & Molecular Biology
Gregory Lazarian, Chloe Friedrich, Anne Quinquenel, Julie Tran, Souhail Ouriemmi, Elisabetta Dondi, Antoine Martin, Imane Mihoub, David Chiron, Celine Bellanger, Carole Fleury, Pascal Gelebart, Emmet McCormack, Dominique Ledoux, Catherine Thieblemont, Jacek Marzec, John G. Gribben, Florence Cymbalista, Nadine Varin-Blank, Laura Gardano, Fanny Baran-Marszak
Review
Biochemistry & Molecular Biology
Bela Papp, Sophie Launay, Pascal Gelebart, Atousa Arbabian, Agnes Enyedi, Jean-Philippe Brouland, Edgardo D. Carosella, Homa Adle-Biassette
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2020)
Article
Biochemistry & Molecular Biology
Abdulraheem Alshareef, Anthea C. Peters, Pascal Gelebart, Will Chen, Raymond Lai
Summary: The constitutive activation of the Wnt canonical pathway (WCP) in mantle cell lymphoma (MCL) is mainly due to gene methylation/silencing of WIF1, which promotes cell growth. Gene transfection of WIF1 into cells significantly reduces cell growth and results in downregulation of various proteins in WCP.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Letter
Hematology
Sahba Shafiee, Pascal Gelebart, Mihaela Popa, Monica Hellesoy, Randi Hovland, Rakel Brendsdal Forthun, Jungwoo Lee, Kaoru Tohyama, Anders Molven, Biju Parekkadan, Bjorn Tore Gjertsen, Astrid Olsnes Kittang, Emmet McCormack
BRITISH JOURNAL OF HAEMATOLOGY
(2021)
Article
Hematology
Pascal Gelebart, May Eriksen Gjerstad, Susanne Benjaminsen, Jianhua Han, Ida Karlsen, Mireia Mayoral Safont, Calum Leitch, Zinayida Fandalyuk, Mihaela Popa, Lars Helgeland, Bela Papp, Fanny Baran-Marszak, Emmet McCormack
Summary: This study reports the identification and expression of a new AXL splice variant, AXL3, in MCL cells, which is constitutively activated and is essential for MCL cell survival. Inhibition of AXL3 leads to apoptosis of MCL cells and significantly reduces the activation of proproliferative and survival pathways. Bemcentinib shows promise as a targeted therapy for MCL, demonstrating higher efficacy than ibrutinib in reducing tumor burden and increasing overall survival in preclinical studies.