Results 161 to 170 of about 22,508 (191)

Small-Molecule Antagonist Targeting Exportin-1 via Rational Structure-Based Discovery

Journal of Medicinal Chemistry, 2020
Exportin-1 (also named as CRM1) plays a prominent role in autoimmune disorders and has emerged as a potential therapeutic target for colitis. Here we report on the rational structure-based discovery of a small-molecule antagonist of exportin-1, LFS-829, with low-range nanomolar activities.
Xibao Tian, Jiali Gao, Meishuo Liu, Yuqin Lei, Fangjun Wang, Jin Chen, Peng Chu, Jiujiao Gao, Feida Long, Minzhi Liang, Xiangyu Long, Huiying Chu, Cuixia Liu, Xueliang Li, Qingxiang Sun, Guohui Li, Yongliang Yang   +16 more
openaire   +2 more sources

EXPORTIN 1 INHIBITION ATTENUATES NUCLEAR FACTOR-κB-DEPENDENT GENE EXPRESSION

Shock, 2008
Activation of nuclear factor (NF)-kappaB is mediated by signal-induced phosphorylation of IkappaBalpha, subsequent IkappaBalpha degradation, and then translocation of unbound NF-kappaB to the nucleus. Termination of gene expression occurs when IkappaBalpha binds NF-kappaB subunits (Rel A) in the nucleus.
Mark D, Walsh, Christine R, Hamiel, Anirban, Banerjee, Aaron M, Cheng, Guillermo, Escobar, Robert C, McIntyre   +5 more
openaire   +2 more sources

Targeting Exportin 1 as treatment for cutaneous squamous cell carcinoma.

Journal of Clinical Oncology, 2023
e21564 Background: Cutaneous squamous cell carcinomas (cSCC) are among the most frequent solid cancers in humans and in the U.S., cSCC cases are increasing. Molecular mechanisms transitioning premalignant lesions to cancer are not well characterized. As a result, targeted therapies need to be identified to treat these lesions.
Ricky Rana, Laura A. Hansen
openaire   +1 more source

Inhibition of Exportin-1 inhibits endothelial cell ICAM expression

Journal of the American College of Surgeons, 2004
Abstract Introduction: Regulation of the export of adaptor proteins that reside in the nucleus may modulate signal transduction. MyD88 is the principal adaptor protein for Toll/IL-1 receptor signaling. We have observed that MyD88 is a predominantly nuclear protein in murine macrophages.
Mark D. Walsh, Anirban Banerjee, Christine Hamiel, Katherine Barsness, Robert McIntyre   +4 more
openaire   +1 more source

Expression of exportin 1 (XPO1/CRM1) in pancreatic adenocarcinoma.

Journal of Clinical Oncology, 2017
327 Background: Exportin 1 (XPO1/CRM1) is a nuclear export chaperone that mediates the nuclear export of several proteins that are essential to growth regulation and tumor suppression. It was found to be overexpressed in several types of human malignancies and overexpression was found to be associated with poor prognosis.
David M Saulino, Pamela S Younes, Jennifer M Biley, Mamoun Younes   +3 more
openaire   +1 more source

Exportin-1 is critical for cell proliferation and survival in adult T cell leukemia

Investigational New Drugs, 2022
Since treatment options for adult T cell leukemia (ATL) associated with human T cell leukemia virus type 1 (HTLV-1) fail to obtain long-term response, novel therapies targeting ATL-dysregulated pathways are necessary. Dysregulated nuclear import and export machinery is common in malignancies. This study aimed to investigate the potential of exportin-1 (
Chie, Ishikawa, Naoki, Mori
openaire   +2 more sources

Exportin-1 is required for the maintenance of the planarian epidermal lineage

International Journal of Biological Macromolecules, 2019
Nucleocytoplasmic transport is essential for normal cellular function that mediates cargo transport from the cytoplasm to the nucleus. However, the mechanisms of nucleocytoplasmic transport that integrate stem cell development remain largely unknown. Since it has a large population of stem cells, the planarian flatworm is an ideal system for the study ...
Qingnan, Tian, Guixia, Zhao, Yujia, Sun, Dandan, Yuan, Qi, Guo, Yizhe, Zhang, Jiaqian, Liu, Shoutao, Zhang   +7 more
openaire   +2 more sources

Exportin-1 (XPO1, CRM1) inhibitors for the management of viral infection

Drugs of the Future, 2021
A therapeutic gap exists between new emerging infectious diseases and effective treatments. Targeting host factors involved in the replication strategies of evolutionarily diverse viruses may bridge this gap. Exportin-1 (XPO1, also termed chromosome region maintenance 1 [CRM1]) is a cellular nuclear export receptor for cellular and viral protein and ...
openaire   +1 more source

Exploring the exportin-1 inhibitors for COVID-19 and anticancer treatment

Journal of Biomolecular Structure and Dynamics
Nuclear export protein 1, also known as XPO1, plays a crucial role in cellular homeostasis and assists in the nucleocytoplasmic transfer of ribonucleic acids (RNAs) and proteins. In addition, this nuclear export receptor is essential for the export of a variety of cargo molecules, such as proteins implicated in the immune response, tumor suppression ...
Tanuj, Sharma, Tanmoy, Mondal, Venu Venkatarame Gowda, Saralamma, Md Imtaiyaz, Hassan, Chang Joong, Kim, Marianela Patzi, Churqui, Kristina, Nyström, Ketan, Thombare, Mohammad Hassan, Baig, Jae-June, Dong   +9 more
openaire   +2 more sources

Identifying novel inhibitors targeting Exportin-1 for the potential treatment of COVID-19

Archives of Microbiology
The nuclear export protein 1 (XPO1) mediates the nucleocytoplasmic transport of proteins and ribonucleic acids (RNAs) and plays a prominent role in maintaining cellular homeostasis. XPO1 has emerged as a promising therapeutic approach to interfere with the lifecycle of many viruses.
Tanuj, Sharma, Tanmoy, Mondal, Sajid, Khan, Marianela Patzi, Churqui, Kristina, Nyström, Ketan, Thombare, Mohammad Hassan, Baig, Jae-June, Dong   +7 more
openaire   +2 more sources