[HTML][HTML] Nucleo-cytoplasmic transport as a therapeutic target of cancer

GL Gravina, W Senapedis, D McCauley… - Journal of hematology & …, 2014 - Springer
Shuttling of specific proteins out of the nucleus is essential for the regulation of the cell cycle
and proliferation of both normal and malignant tissues. Dysregulation of this fundamental …

Nuclear export of proteins and drug resistance in cancer

JG Turner, J Dawson, DM Sullivan - Biochemical pharmacology, 2012 - Elsevier
The intracellular location of a protein is crucial to its normal functioning in a cell. Cancer cells
utilize the normal processes of nuclear-cytoplasmic transport through the nuclear pore …

Selective inhibitors of nuclear export show that CRM1/XPO1 is a target in chronic lymphocytic leukemia

R Lapalombella, Q Sun, K Williams… - Blood, The Journal …, 2012 - ashpublications.org
The nuclear export protein XPO1 is overexpressed in cancer, leading to the cytoplasmic
mislocalization of multiple tumor suppressor proteins. Existing XPO1-targeting agents lack …

First-in-class, first-in-human phase I study of selinexor, a selective inhibitor of nuclear export, in patients with advanced solid tumors

AR Abdul Razak, M Mau-Soerensen… - Journal of Clinical …, 2016 - ascopubs.org
Purpose This trial evaluated the safety, pharmacokinetics, pharmacodynamics, and efficacy
of selinexor (KPT-330), a novel, oral small-molecule inhibitor of exportin 1 (XPO1/CRM1) …

CRM1 inhibition induces tumor cell cytotoxicity and impairs osteoclastogenesis in multiple myeloma: molecular mechanisms and therapeutic implications

YT Tai, Y Landesman, C Acharya, Y Calle, MY Zhong… - Leukemia, 2014 - nature.com
The key nuclear export protein CRM1/XPO1 may represent a promising novel therapeutic
target in human multiple myeloma (MM). Here we showed that chromosome region …

p53-based cancer therapy

DP Lane, CF Cheok, S Lain - Cold Spring Harbor …, 2010 - cshperspectives.cshlp.org
Inactivation of p53 functions is an almost universal feature of human cancer cells. This has
spurred a tremendous effort to develop p53 based cancer therapies. Gene therapy using …

KPT‐330 inhibitor of CRM 1 (XPO 1)‐mediated nuclear export has selective anti‐leukaemic activity in preclinical models of T‐cell acute lymphoblastic leukaemia and …

J Etchin, T Sanda, MR Mansour… - British journal of …, 2013 - Wiley Online Library
This study explored the anti‐leukaemic efficacy of novel irreversible inhibitors of the major
nuclear export receptor, chromosome region maintenance 1 (CRM 1, also termed XPO 1) …

[HTML][HTML] Antileukemic activity of nuclear export inhibitors that spare normal hematopoietic cells

J Etchin, Q Sun, A Kentsis, A Farmer, ZC Zhang… - Leukemia, 2013 - nature.com
Drugs that target the chief mediator of nuclear export, chromosome region maintenance 1
protein (CRM1) have potential as therapeutics for leukemia, but existing CRM1 inhibitors …

Importins and exportins as therapeutic targets in cancer

A Mahipal, M Malafa - Pharmacology & therapeutics, 2016 - Elsevier
The nuclear transport proteins, importins and exportins (karyopherin-β proteins), may play
an important role in cancer by transporting key mediators of oncogenesis across the nuclear …

[HTML][HTML] Clinical implications of targeting XPO1-mediated nuclear export in multiple myeloma

UH Gandhi, W Senapedis, E Baloglu, TJ Unger… - … Myeloma and Leukemia, 2018 - Elsevier
Multiple myeloma (MM) is a malignancy of plasma cells that is typically chronic, and relapse
is common. Current therapeutic strategies include combination and sequential treatments …