Selinexor, selective inhibitor of nuclear export: Unselective bullet for blood cancers

K Benkova, J Mihalyova, R Hajek, T Jelinek - Blood Reviews, 2021 - Elsevier
Abstract Exportin 1 (XPO1), also known as chromosome maintenance 1 protein (CRM1), is
the main transporter for hundreds of proteins like tumor suppressors, growth regulatory …

Selinexor for advanced hematologic malignancies

JS Walker, R Garzon, R Lapalombella - Leukemia & Lymphoma, 2020 - Taylor & Francis
Recent measures to classify novel molecular targets with therapeutic potential across
multiple hematologic tumors have identified the eukaryotic nuclear exporter, exportin 1 …

[HTML][HTML] The past, present, and future of CRM1/XPO1 inhibitors

AY Wang, H Liu - Stem cell investigation, 2019 - ncbi.nlm.nih.gov
Therapies targeted at inhibiting nucleo-cytoplasmic transport have found broad applications
in the field of oncology. Chromosome region maintenance 1 (CRM1), better known as …

[HTML][HTML] Eltanexor (KPT-8602), a second-generation selective inhibitor of nuclear export (SINE) compound, in patients with refractory multiple myeloma

RF Cornell, AC Rossi, R Baz, CC Hofmeister, C Shustik… - Blood, 2017 - Elsevier
Introduction-Elevated expression of XPO1 (Exportin 1) increases the nuclear
export/inactivation of tumor suppressor proteins (eg p53, IkB, p21, FOXO) and promotes the …

Pharmacokinetics of selinexor: the first-in-class selective inhibitor of nuclear export

JC Bader, AR Abdul Razak, S Shacham, H Xu - Clinical Pharmacokinetics, 2021 - Springer
The functionality of many tumor suppressor proteins (TSPs) and oncoprotein transcript RNAs
largely depend on their location within the cell. The exportin 1 complex (XPO1) transports …

Next-generation XPO1 inhibitor shows improved efficacy and in vivo tolerability in hematological malignancies

ZA Hing, HYJ Fung, P Ranganathan, S Mitchell… - Leukemia, 2016 - nature.com
The nuclear export receptor, Exportin 1 (XPO1), mediates transport of growth-regulatory
proteins, including tumor suppressors, and is overactive in many cancers, including chronic …

[HTML][HTML] Preliminary evidence of anti tumor activity of selinexor (KPT-330) in a phase I trial ofa first-in-class oral selective inhibitor of nuclear export (SINE) in patients …

J Kuruvilla, M Gutierrez, BD Shah, NY Gabrail… - Blood, 2013 - Elsevier
Abstract Background Exportin 1 (CRM1/XPO1) is the exclusive transporter of the majority of
Tumor Suppressor Proteins (TSP) out of the nucleus, rendering these TSPs non-functional …

Selective inhibitors of nuclear export (SINE) in hematological malignancies

A Das, G Wei, K Parikh, D Liu - Experimental hematology & oncology, 2015 - Springer
Regulated nucleo-cytoplasmic transport plays a major role in maintaining cellular
homeostasis. CRM1 (chromosome region maintenance 1 or exportin 1 or XPO 1) is …

SINE (selective inhibitor of nuclear export)–translational science in a new class of anti-cancer agents

J Gerecitano - Journal of hematology & oncology, 2014 - Springer
Regulation of protein trafficking between the nucleus and cytoplasm represents a novel
control point for antineoplastic intervention. Several proteins involved with cellular growth …

Selective inhibitors of nuclear export (SINE)–a novel class of anti-cancer agents

K Parikh, S Cang, A Sekhri, D Liu - Journal of hematology & oncology, 2014 - Springer
Dysregulation of the nucleo-cytoplasmic transport of proteins plays an important role in
carcinogenesis. The nuclear export of proteins depends on the activity of transport proteins …