Results 1 to 10 of about 7,047 (156)

Preclinical characterization of a reversible XPO1 inhibitor for cancer therapy [PDF]

Nature Communications
Exportin 1 (XPO1/CRM1) is a clinically validated anticancer target whose inhibition blocks nuclear export and promotes cancer cell apoptosis. Current XPO1 inhibitors rely on covalent Michael addition to Cys528 in the nuclear export signal binding groove ...
Janne Van Hauwenhuyse, Felien Reniers, Leentje Persoons, Sam Noppen, Casey E. Wing, Ashley B. Niesman, Ho Yee Joyce Fung, Els Vanstreels, Maarten Jacquemyn, Eline Boel, Ann Vankerckhoven, Yani Berckmans, Bert Kwanten, An Coosemans, Guy Van den Mooter, Yuh Min Chook, Wim Dehaen, Dirk Daelemans   +17 more
doaj   +2 more sources

XPO1-mediated TRIM21 nuclear export reprograms TREM2+ macrophage polarization by targeting IRF3 to augment anti-PD-1 efficacy in small cell lung cancer [PDF]

Nature Communications
Small cell lung cancer (SCLC) is an aggressive malignancy that responds poorly to immune checkpoint inhibitor (ICI) therapy, due to its immunosuppressive tumor microenvironment.
Qingwu Du, Tingting Qin, Jingya Wang, Yantao Jiang, Qi Xu, Xueyang Li, Huiyan Liu, Junjie Yu, Yi Lu, Luyao Tong, Tao Sun, Peng Chen, Richeng Jiang, Dingzhi Huang   +13 more
doaj   +2 more sources

USP34 Haploinsufficiency as a Cause of Neurodevelopmental Phenotypes. [PDF]

Clin Genet
Heterozygous loss‐of‐function variants in USP34 cause a novel neurodevelopmental disorder characterized by global developmental delay, speech impairment, autism, hypotonia, craniofacial dysmorphism, and distal limb anomalies. Disrupted Wnt/β‐catenin signaling via reduced Axin stabilization refines gene‐specific contributions within 2p15p16.1 ...
Wigoda H, Khan A, Mendelsohn BA, Miyake N, Okamoto N, Matsumoto N, Knijnenburg PJC, van Hagen JM, van de Kamp J, Waisfisz Q, Webb BD.   +10 more
europepmc   +2 more sources

Targeting nuclear export and Janus Kinase/Signal Transducer and Activator of Transcription (JAK/STAT) signalling in myelofibrosis: A novel combinatorial strategy that impacts intrinsic and microenvironment-related pathways. [PDF]

Br J Haematol
Selinexor targets molecular pathways critical to myelofibrosis (MF) progenitor cell fitness and demonstrates complementary activity with ruxolitinib, supporting its potential as a novel disease‐modifying therapeutic strategy for MF. Summary Myelofibrosis (MF) is a chronic myeloproliferative neoplasm (MPN) characterized by splenomegaly, constitutional ...
Kashyap T, Ellero AA, Walker CJ, Maloof ME, Lu M, Xia L, Hoffman R, Taverna P.   +7 more
europepmc   +2 more sources

Anticancer effects of an XPO1 inhibitor (selinexor) with sotorasib following omeprazole preconditioning in KRAS G12C-mutant non-small cell lung cancer cells in vitro and in a mouse tumor xenograft [PDF]

Neoplasia: An International Journal for Oncology Research
Background: KRAS G12C-mutant advanced non-small cell lung cancer (NSCLC) is currently treated with KRAS G12C covalent inhibitors, such as sotorasib, or RAS (ON) G12-selective inhibitors; however, response rates and progression-free survival remain ...
Jèssica González, Xueting Cai, Wenjing Diao, Gaël Roué, Kevin València-Clua, Daniel Olmo-González, María González-Cao, Anisha Jain, Eloisa Jantus-Lewintre, Ana Giménez-Capitán, Miguel Angel Molina-Vila, Jordi Codony-Servat, Peng Cao, Rafael Rosell   +13 more
doaj   +2 more sources

Targeting the nuclear export receptor exportin‐1 in acute myeloid leukaemia: From biology to clinical translation [PDF]

Clinical and Translational Medicine
Background Exportin‐1 (XPO1), a key regulator of nucleocytoplasmic transport, is frequently dysregulated in acute myeloid leukemia (AML) and contributes to leukemogenesis, disease progression and therapeutic resistance.
Yifan Liu, Xiaoya Yun, Weidong Ding, Suxiao Li, Hui Liu   +4 more
doaj   +2 more sources

XPO1 serves as a prognostic marker involving AKT/MAPK/TGFBR1 pathway in OSCC

Cancer Medicine
Background Exportin 1 (XPO1) is a nuclear export protein that facilitates the transportation of various substances. XPO1 promotes tumor development as a poor prognostic factor in a variety of tumors and is a therapeutic target for screening inhibitors ...
Tong Su, Kun Xia, Haofeng Xiong
exaly   +2 more sources

XPO1-dependent nuclear export regulates NS3 localization and promotes DENV-2 replication through mitochondrial remodeling and interferon suppression [PDF]

Nucleus
Nucleocytoplasmic transport is essential for cellular homeostasis and is frequently exploited by viruses during infection. Although dengue virus (DENV) non-structural protein 3 (NS3) undergoes nuclear trafficking, the role of nuclear export pathways in ...
Selvin Noé Palacios-Rápalo, Jonathan Hernández-Castillo, Luis Adrián De Jesús-González, Daniel Talamas-Lara, Carlos Daniel Cordero-Rivera, Bulmaro Cisneros-Vega, Jose Manuel Reyes-Ruiz, Rosa María del Ángel   +7 more
doaj   +2 more sources

NRF2 activators and the inhibitor of nuclear export, selinexor, restrict coronaviruses by targeting a network involving ACE2, TMPRSS2, and XPO1 through an NRF2-independent mechanism [PDF]

Communications Biology
Nuclear factor erythroid 2–related factor 2 (NRF2) plays important roles in antiviral host cell defenses. We assessed the potential of the NRF2 activators 4-octyl itaconate (4OI), bardoxolone (BARD), and sulforaphane (SFN), and the exportin-1 (XPO1 ...
Fakhar H. Waqas, Leandro Silva da Costa, Francisco J. Zapatero-Belinchón, Madalina E. Carter-Timofte, Lisa Lasswitz, Demi van der Horst, Rebecca Möller, Julia Dahlmann, Ruth Olmer, Robert Geffers, Gisa Gerold, David Olagnier, Frank Pessler   +12 more
doaj   +2 more sources

CCT3-mediated regulation of XPO1/RB1 axis stability promotes cellular senescence and tumor progression in clear cell renal carcinoma [PDF]

iScience
Summary: Cellular senescence’s role in clear cell renal carcinoma (ccRCC) remains unclear. We identify CCT3 as a driver of ccRCC progression by enhancing XPO1 stability via correct folding, confirmed by Co-IP and GST pull-down.
Yilong Cao, Chao Xu, Yuepeng Liu, Bei Shi, Xiaoling Li, Jiehan Li, Bowei Zhang, Zeyuan Zhang, Shengtao Dai, Qingyun Sun, Junfei Gu   +10 more
doaj   +2 more sources