4.6 Review

Pharmacological Inhibition of LSD1 for Cancer Treatment

Journal

MOLECULES
Volume 23, Issue 12, Pages -

Publisher

MDPI
DOI: 10.3390/molecules23123194

Keywords

LSD1; demethylase; histone; breast cancer; prostate cancer; acute myeloid leukemia; cancer therapy

Funding

  1. Hong Kong Baptist University [FRG2/16-17/007, FRG2/17-18/003]
  2. Health and Medical Research Fund [HMRF/14150561]
  3. National Natural Science Foundation of China [21575121, 21775131, 21628502]
  4. Hong Kong Baptist University Century Club Sponsorship Scheme 2018
  5. Interdisciplinary Research Matching Scheme [RC-IRMS/16-17/03]
  6. Interdisciplinary Research Clusters Matching Scheme [RC-IRCs/17-18/03]
  7. Matching Proof of Concept Fund [MPCF-001-2017/18]
  8. HKBU Strategic Development Fund [SKLP_1718_P04]
  9. Science and Technology Development Fund, Macao SAR [0072/2018/A2]
  10. University of Macau [MYRG2016-00151-ICMS-QRCM, MYRG2018-00187-ICMS]
  11. SKLEBA
  12. [HKBU/12301115]
  13. [ITS/260/16FX]
  14. [C5026-16G]

Ask authors/readers for more resources

Lysine-specific demethylase 1A (LSD1, also named KDM1A) is a demethylase that can remove methyl groups from histones H3K4me1/2 and H3K9me1/2. It is aberrantly expressed in many cancers, where it impedes differentiation and contributes to cancer cell proliferation, cell metastasis and invasiveness, and is associated with inferior prognosis. Pharmacological inhibition of LSD1 has been reported to significantly attenuate tumor progression in vitro and in vivo in a range of solid tumors and acute myeloid leukemia. This review will present the structural aspects of LSD1, its role in carcinogenesis, a comparison of currently available approaches for screening LSD1 inhibitors, a classification of LSD1 inhibitors, and its potential as a drug target in cancer therapy.

Authors

I am an author on this paper
Click your name to claim this paper and add it to your profile.

Reviews

Primary Rating

4.6
Not enough ratings

Secondary Ratings

Novelty
-
Significance
-
Scientific rigor
-
Rate this paper

Recommended

No Data Available
No Data Available