Capsaicin: A "hot" KDM1A/LSD1 inhibitor from peppers.
Sign Up to like & getrecommendations! Published in 2020 at "Bioorganic chemistry"
DOI: 10.1016/j.bioorg.2020.104161
Abstract: Capsaicinoids are plant secondary metabolites, and capsaicin is the main principal that responsible to the pungency of chili peppers, with widely application as food additive. In our study, capsaicin was characterized as lysine specific demethylase… read more here.
Keywords: capsaicin hot; inhibitor; lsd1 inhibitor; kdm1a ... See more keywords
Design, Synthesis, and Evaluation of the Selective and Orally Active LSD1 Inhibitor with the Potential of Treating Heart Failure.
Sign Up to like & getrecommendations! Published in 2024 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.4c01303
Abstract: LSD1 has become an appealing target for the development of new pharmacologic agents to treat cardiovascular diseases, including heart failure. Herein, we reported the design, synthesis, and structure-activity relationship of a series of TCP-based derivatives… read more here.
Keywords: heart; inhibitor potential; design synthesis; lsd1 inhibitor ... See more keywords
Abstract 4871: Antitumor activity of novel reversible LSD1 inhibitor, HM97211 in preclinical models of SCLC
Sign Up to like & getrecommendations! Published in 2018 at "Cancer Research"
DOI: 10.1158/1538-7445.am2018-4871
Abstract: Introduction: Global changes in the epigenetic landscape are known as the hallmark in cancer and the histone demethylase Lysine-specific demethylase 1 (LSD1) is one of the novel target for the therapy of various malignant diseases… read more here.
Keywords: inhibitor hm97211; lsd1 inhibitor; reversible lsd1; novel reversible ... See more keywords
The LSD1 Inhibitor Iadademstat Is Active in Acute Myeloid Leukemia.
Sign Up to like & getrecommendations! Published in 2020 at "Cancer discovery"
DOI: 10.1158/2159-8290.cd-rw2020-155
Abstract: In a phase I trial, iadademstat induced blast differentiation and reduced bone marrow blast burden. read more here.
Keywords: inhibitor iadademstat; acute myeloid; myeloid leukemia; lsd1 inhibitor ... See more keywords
Preliminary safety and efficacy results of A phase ib investigation of the LSD1 inhibitor iadademstat (ORY-1001) in combination with azacitidine and venetoclax in newly-diagnosed AML
Sign Up to like & getrecommendations! Published in 2025 at "Blood"
DOI: 10.1182/blood-2025-1649
Abstract: Background: Azacitidine combined with venetoclax (AZA+VEN) is the standard of care treatment for older and/or unfit patients (pts) with newly diagnosed acute myeloid leukemia (ND-AML), yet most pts ultimately relapse. For pts without targetable mutations,… read more here.
Keywords: newly diagnosed; aza ven; iadademstat; response ... See more keywords
An Overview on Screening Methods for Lysine Specific Demethylase 1 (LSD1) Inhibitors.
Sign Up to like & getrecommendations! Published in 2017 at "Current medicinal chemistry"
DOI: 10.2174/0929867324666170509114321
Abstract: BACKGROUND In the past few years, great of attention has been paid to the identification and characterization of selective and potent inhibitors of the first identified histone demethylase LSD1, which may erase mono- and di-methylated… read more here.
Keywords: lsd1 inhibitor; lsd1 inhibitors; chemistry; demethylase lsd1 ... See more keywords
Carrier-free supramolecular nanoassemblies of pure LSD1 inhibitor for effective anti-tumor therapy
Sign Up to like & getrecommendations! Published in 2022 at "Frontiers in Chemistry"
DOI: 10.3389/fchem.2022.1012882
Abstract: The LSD1 protein is an oxidase that regulates protein methylation, which regulates gene expression and triggers tumors. Previously, inhibiting LSD1 has been found to be an effective treatment strategy for opposing tumors caused by overexpression… read more here.
Keywords: lsd1 inhibitor; anti tumor; free supramolecular; carrier free ... See more keywords