Histone lysine specific demethylase 1 inhibitors

被引：19

作者：

Mehndiratta, Samir ^{[1
,2
]}

Liou, Jing-Ping ^{[1
]}

机构：

[1] Taipei Med Univ, Sch Pharm, Coll Pharm, Taipei, Taiwan

[2] Univ Southern Calif, Dept Pharmacol & Pharmaceut Sci, Sch Pharm, Los Angeles, CA 90007 USA

来源：

RSC MEDICINAL CHEMISTRY | 2020年 / 11卷 / 09期

关键词：

CYCLIC PEPTIDE INHIBITORS; BIOLOGICAL-ACTIVITY; TRANYLCYPROMINE DERIVATIVES; REVERSIBLE INHIBITORS; LSD1; INHIBITORS; DUAL INHIBITORS; DESIGN; METHYLATION; POTENT; DISCOVERY;

D O I：

10.1039/d0md00141d

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

LSD1 plays a pivotal role in numerous biological functions. The overexpression of LSD1 is reported to be associated with different malignancies. Over the last decade, LSD1 has emerged as an interesting target for the treatment of acute myeloid leukaemia (AML). Numerous researchers have designed, synthesized, and evaluated various LSD1 inhibitors with diverse chemical architectures. Some of these inhibitors have entered clinical trials and are currently at different phases of clinical evaluation. This comprehensive review enlists recent research developments in LSD1 targeting pharmacophores reported over the last few years.

引用

页码：969 / 981

页数：13

共 102 条

[1] Chemical con artists foil drug discovery [J].

Baell, Jonathan ;

Walters, Michael A. .

NATURE, 2014, 513 (7519) :481-483

[2] Feeling Nature's PAINS: Natural Products, Natural Product Drugs, and Pan Assay Interference Compounds (PAINS) [J].

Baell, Jonathan B. .

JOURNAL OF NATURAL PRODUCTS, 2016, 79 (03) :616-628

[3] Histone methylation: Dynamic or static? [J].

Bannister, AJ ;

Schneider, R ;

Kouzarides, T .

CELL, 2002, 109 (07) :801-806

[4] LSD1 dual function in mediating epigenetic corruption of the vitamin D signaling in prostate cancer [J].

Battaglia, Sebastiano ;

Karasik, Ellen ;

Gillard, Bryan ;

Williams, Jennifer ;

Winchester, Trisha ;

Moser, Michael T. ;

Smiraglia, Dominic J. ;

Foster, Barbara A. .

CLINICAL EPIGENETICS, 2017, 9 :82

[5] Phase I, Open-Label, Dose-Escalation Study of the Safety, Pharmacokinetics, Pharmacodynamics, and Efficacy of GSK2879552 in Relapsed/Refractory SCLC [J].

Bauer, Todd M. ;

Besse, Benjamin ;

Martinez-Marti, Alex ;

Trigo, Jose Manuel ;

Moreno, Victor ;

Garrido, Pilar ;

Ferron-Brady, Geraldine ;

Wu, Yuehui ;

Park, Jennifer ;

Collingwood, Therese ;

Kruger, Ryan G. ;

Mohammad, Helai P. ;

Ballas, Marc S. ;

Dhar, Arindam ;

Govindan, Ramaswamy .

JOURNAL OF THORACIC ONCOLOGY, 2019, 14 (10) :1828-1838

[6] Enantioselective synthesis of tranylcypromine analogues as lysine demethylase (LSD1) inhibitors [J].

Benelkebir, Hanae ;

Hodgkinson, Christopher ;

Duriez, Patrick J. ;

Hayden, Annette L. ;

Bulleid, Rosemary A. ;

Crabb, Simon J. ;

Packham, Graham ;

Ganesan, A. .

BIOORGANIC & MEDICINAL CHEMISTRY, 2011, 19 (12) :3709-3716

[7] DNA methylation patterns and epigenetic memory [J].

Bird, A .

GENES & DEVELOPMENT, 2002, 16 (01) :6-21

[8] Histone Lysine Methylation Dynamics: Establishment, Regulation, and Biological Impact [J].

Black, Joshua C. ;

Van Rechem, Capucine ;

Whetstine, Johnathan R. .

MOLECULAR CELL, 2012, 48 (04) :491-507

[9] Fluorinated tranylcypromine analogues as inhibitors of lysine-specific demethylase 1 (LSD1, KDM1A) [J].

Borrello, Maria Teresa ;

Schinor, Benjamin ;

Bartels, Katharina ;

Benelkebir, Hanae ;

Pereira, Sara ;

Al-Jamal, Wafa T. ;

Douglas, Leon ;

Duriez, Patrick J. ;

Packham, Graham ;

Haufe, Guenter ;

Ganesan, A. .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2017, 27 (10) :2099-2101

[10] Structural insight into substrate recognition by histone demethylase LSD2/KDM1b [J].

Chen, Fei ;

Yang, Huirong ;

Dong, Zhenghong ;

Fang, Jian ;

Wang, Ping ;

Zhu, Tingting ;

Gong, Wei ;

Fang, Rui ;

Shi, Yujiang Geno ;

Li, Ze ;

Xu, Yanhui .

CELL RESEARCH, 2013, 23 (02) :306-309

← 1 2 3 4 5 6 7 8 9 10 →