Related Experiment Video

Updated: Jan 26, 2026

Using Generative Art to Convey Past and Future Climate Transitions
06:10

Using Generative Art to Convey Past and Future Climate Transitions

Published on: March 31, 2023

1.4K

The past, present, and future of CRM1/XPO1 inhibitors

Amy Y Wang1, Hongtao Liu1

  • 1Department of Medicine, Section of Hematology/Oncology, University of Chicago Medicine, Chicago, IL, USA.

Stem Cell Investigation
|April 13, 2019
PubMed

Insights

Selective inhibitors of nuclear transport (SINE) target exportin 1 (XPO1), a protein crucial for tumor suppressor transport. This review explores XPO1 dysregulation in cancer and the therapeutic potential of SINE compounds like selinexor.

Area of Science:

  • Oncology
  • Molecular Biology
  • Pharmacology

Background:

  • Nucleo-cytoplasmic transport is vital for cellular regulation.
  • Exportin 1 (XPO1) mediates the transport of tumor suppressors and growth factors.
  • XPO1 dysregulation is implicated in numerous cancers, correlating with poor prognosis.

Purpose of the Study:

  • To review the role of XPO1 dysregulation in promoting tumorigenesis.
  • To discuss the historical development of selective inhibitors of nuclear transport (SINE) compounds.
  • To examine the current clinical applications of SINE compounds in cancer therapy.

Main Methods:

  • Literature review of studies on XPO1 function, cancer biology, and SINE compounds.
  • Analysis of clinical trial data for SINE agents, particularly selinexor.
  • Synthesis of information on the mechanism of action and therapeutic efficacy.

Main Results:

  • XPO1 inhibition represents a promising therapeutic strategy in oncology.
  • SINE compounds, such as selinexor, have demonstrated activity in various solid tumors and hematologic malignancies.
  • Clinical trials indicate the potential of SINEs in treating cancers with XPO1 upregulation.

Conclusions:

  • Targeting XPO1 offers a novel approach to cancer treatment.
  • SINE compounds are emerging as a significant class of anti-cancer agents.
  • Further research and clinical evaluation are ongoing to optimize SINE-based therapies.
Keywords:
Selinexorchromosome region maintenance 1/exportin 1 inhibitors (XPO1/CRM1 inhibitors)

More Related Videos

Y-90 Radioembolization and PD-1 Inhibitor as Neoadjuvant Treatment in Hepatocellular Carcinoma09:11

Y-90 Radioembolization and PD-1 Inhibitor as Neoadjuvant Treatment in Hepatocellular Carcinoma

Published on: May 24, 2024

1.1K
Assays for Validating Histone Acetyltransferase Inhibitors09:11

Assays for Validating Histone Acetyltransferase Inhibitors

Published on: August 6, 2020

7.0K

Related Concept Videos

Eukaryotic Transcription Inhibitors01:52

Eukaryotic Transcription Inhibitors

Certain biochemical processes, such as embryonic development and cell growth regulation, depend on the repression of specific genes. DNA binding proteins known as eukaryotic transcription inhibitors regulate the repression of gene expression in eukaryotes. The presence of these inhibitors at the required location and time in the cell is triggered by the presence of hormones and additional signals from other cells.
Eukaryotic transcription inhibitors usually contain two distinct domains, a...
10.9K
Dipeptidyl Peptidase 4 Inhibitors01:23

Dipeptidyl Peptidase 4 Inhibitors

Dipeptidyl peptidase 4 (DPP-4) is a serine protease widely distributed in the body. It's involved in the inactivation of GLP-1 and GIP hormones, which are crucial for insulin regulation. DPP-4 inhibitors, such as sitagliptin (Januvia), saxagliptin (Onglyza), linagliptin (Tradjenta), alogliptin (Nesina), and vildagliptin (Galvus), help increase the proportion of active GLP-1, enhancing insulin secretion. These inhibitors work by competitively binding to DPP-4. This binding causes a...
626
Antihypertensive Drugs: Direct Renin Inhibitors01:25

Antihypertensive Drugs: Direct Renin Inhibitors

The renin-angiotensin-aldosterone system (RAAS) is an intricate physiological pathway involving numerous enzymes and hormones, including renin, angiotensin-converting enzyme (ACE), angiotensin I and II, and aldosterone. Imbalances within this system increase the production of angiotensin II and aldosterone. Increased angiotensin II levels promote vasoconstriction and blood pressure elevation. Concurrently, higher aldosterone levels stimulate sodium and water reabsorption in the kidneys,...
1.4K
Antihypertensive Drugs: Angiotensin-Converting Enzyme Inhibitors01:30

Antihypertensive Drugs: Angiotensin-Converting Enzyme Inhibitors

Angiotensin-converting enzyme (ACE), a vital component of the renin-angiotensin-aldosterone system, is abundant in lung endothelial cells. ACE converts the inactive decapeptide, angiotensin I, into the active octapeptide, angiotensin II. This potent vasoconstrictor narrows blood vessels, increasing resistance to blood flow and elevating blood pressure. Angiotensin II also stimulates aldosterone production, encouraging kidney cells to reabsorb more sodium and water from urine, thereby increasing...
2.4K
Treatment for Pulmonary Arterial Hypertension: Phosphodiesterase Inhibitors01:28

Treatment for Pulmonary Arterial Hypertension: Phosphodiesterase Inhibitors

Phosphodiesterase 5 (PDE5) inhibitors are potent enzymes that function to hydrolyze cyclic nucleotides to their corresponding 5' monophosphates. Their unique biochemical properties have been applied in treating Pulmonary Arterial Hypertension (PAH).
Among the PDE5 inhibitors, sildenafil (Revatio) stands out as a competitive and selective inhibitor. It operates by elevating cellular levels of cGMP and augmenting signaling through the cGMP-PKG pathway, promoting vasodilation. Upon oral...
587
Oral Hypoglycemic Agents: α-Glucosidase Inhibitors01:19

Oral Hypoglycemic Agents: α-Glucosidase Inhibitors

α-glucosidase inhibitors, including acarbose (Precose), miglitol (Glyset), and voglibose (Voglib) (primarily available in Asia), are drugs that control blood sugar levels by delaying the digestion of starch and disaccharides. They achieve this by inhibiting α-glucosidase enzymes in the intestine, which slow the absorption of carbohydrates in the intestine, which in turn leads to a prolonged release of the glucoregulatory hormone GLP-1 from intestinal L-cells.
Acarbose and miglitol are...
555