Journal: Frontiers in Pharmacology

Article Title: LSD1 inhibitors for cancer treatment: Focus on multi-target agents and compounds in clinical trials

doi: 10.3389/fphar.2023.1120911

Figure Lengend Snippet: General catalytic mechanism of histone demethylation by LSD1.

Article Snippet: , Salarius Pharmaceuticals, LLC , A Rollover Protocol to Allow for Continued Access to the LSD1 Inhibitor Seclidemstat (SP-2577) , Ewing Sarcoma, Myxoid Liposarcoma, Desmoplastic Small Round Cell Tumor, Extraskeletal Myxoid Chondrosarcoma, Angiomatoid Fibrous Histiocytoma, Clear Cell Sarcoma, Myoepithelial Tumor, Low Grade Fibromyxoid Sarcoma, Sclerosing Epithelioid Fibrosarcoma , Phase 1/2, Enrolling by invitation NCT05266196.

Techniques:

Journal: Frontiers in Pharmacology

Article Title: LSD1 inhibitors for cancer treatment: Focus on multi-target agents and compounds in clinical trials

doi: 10.3389/fphar.2023.1120911

Figure Lengend Snippet: (A) Structural organization of LSD1 with the N -flexible region (grey) and the domains SWIRM (green), AOL (two parts, orange), and Tower (light blue). (B) X-ray structure of the LSD1/CoREST complex, with the domains SWIRM (green), AOL (orange) and Tower (light blue). The CoREST portion is depicted in pink. The FAD cofactor (blue) is located inside of the AOL domain (PDB ID: 3ABT).

Article Snippet: , Salarius Pharmaceuticals, LLC , A Rollover Protocol to Allow for Continued Access to the LSD1 Inhibitor Seclidemstat (SP-2577) , Ewing Sarcoma, Myxoid Liposarcoma, Desmoplastic Small Round Cell Tumor, Extraskeletal Myxoid Chondrosarcoma, Angiomatoid Fibrous Histiocytoma, Clear Cell Sarcoma, Myoepithelial Tumor, Low Grade Fibromyxoid Sarcoma, Sclerosing Epithelioid Fibrosarcoma , Phase 1/2, Enrolling by invitation NCT05266196.

Techniques:

Journal: Frontiers in Pharmacology

Article Title: LSD1 inhibitors for cancer treatment: Focus on multi-target agents and compounds in clinical trials

doi: 10.3389/fphar.2023.1120911

Figure Lengend Snippet: Overview of LSD1 inhibitors currently in clinical investigations for cancer treatment.

Article Snippet: , Salarius Pharmaceuticals, LLC , A Rollover Protocol to Allow for Continued Access to the LSD1 Inhibitor Seclidemstat (SP-2577) , Ewing Sarcoma, Myxoid Liposarcoma, Desmoplastic Small Round Cell Tumor, Extraskeletal Myxoid Chondrosarcoma, Angiomatoid Fibrous Histiocytoma, Clear Cell Sarcoma, Myoepithelial Tumor, Low Grade Fibromyxoid Sarcoma, Sclerosing Epithelioid Fibrosarcoma , Phase 1/2, Enrolling by invitation NCT05266196.

Techniques: Mutagenesis, Activity Assay, Drug discovery

Journal: Frontiers in Pharmacology

Article Title: LSD1 inhibitors for cancer treatment: Focus on multi-target agents and compounds in clinical trials

doi: 10.3389/fphar.2023.1120911

Figure Lengend Snippet: Covalent, TCP-based LSD1 inhibitors substituted on the phenyl ring.

Article Snippet: , Salarius Pharmaceuticals, LLC , A Rollover Protocol to Allow for Continued Access to the LSD1 Inhibitor Seclidemstat (SP-2577) , Ewing Sarcoma, Myxoid Liposarcoma, Desmoplastic Small Round Cell Tumor, Extraskeletal Myxoid Chondrosarcoma, Angiomatoid Fibrous Histiocytoma, Clear Cell Sarcoma, Myoepithelial Tumor, Low Grade Fibromyxoid Sarcoma, Sclerosing Epithelioid Fibrosarcoma , Phase 1/2, Enrolling by invitation NCT05266196.

Techniques:

Journal: Frontiers in Pharmacology

Article Title: LSD1 inhibitors for cancer treatment: Focus on multi-target agents and compounds in clinical trials

doi: 10.3389/fphar.2023.1120911

Figure Lengend Snippet: Hybrid compounds inhibitors of LSD1 and JmjC.

Article Snippet: , Salarius Pharmaceuticals, LLC , A Rollover Protocol to Allow for Continued Access to the LSD1 Inhibitor Seclidemstat (SP-2577) , Ewing Sarcoma, Myxoid Liposarcoma, Desmoplastic Small Round Cell Tumor, Extraskeletal Myxoid Chondrosarcoma, Angiomatoid Fibrous Histiocytoma, Clear Cell Sarcoma, Myoepithelial Tumor, Low Grade Fibromyxoid Sarcoma, Sclerosing Epithelioid Fibrosarcoma , Phase 1/2, Enrolling by invitation NCT05266196.

Techniques:

Journal: Frontiers in Pharmacology

Article Title: LSD1 inhibitors for cancer treatment: Focus on multi-target agents and compounds in clinical trials

doi: 10.3389/fphar.2023.1120911

Figure Lengend Snippet: Covalent TCP-based LSD1 inhibitors substituted on the amino group.

Article Snippet: , Salarius Pharmaceuticals, LLC , A Rollover Protocol to Allow for Continued Access to the LSD1 Inhibitor Seclidemstat (SP-2577) , Ewing Sarcoma, Myxoid Liposarcoma, Desmoplastic Small Round Cell Tumor, Extraskeletal Myxoid Chondrosarcoma, Angiomatoid Fibrous Histiocytoma, Clear Cell Sarcoma, Myoepithelial Tumor, Low Grade Fibromyxoid Sarcoma, Sclerosing Epithelioid Fibrosarcoma , Phase 1/2, Enrolling by invitation NCT05266196.

Techniques:

Journal: Frontiers in Pharmacology

Article Title: LSD1 inhibitors for cancer treatment: Focus on multi-target agents and compounds in clinical trials

doi: 10.3389/fphar.2023.1120911

Figure Lengend Snippet: Irreversible LSD1 inhibitors in clinical trials for cancer treatment.

Article Snippet: , Salarius Pharmaceuticals, LLC , A Rollover Protocol to Allow for Continued Access to the LSD1 Inhibitor Seclidemstat (SP-2577) , Ewing Sarcoma, Myxoid Liposarcoma, Desmoplastic Small Round Cell Tumor, Extraskeletal Myxoid Chondrosarcoma, Angiomatoid Fibrous Histiocytoma, Clear Cell Sarcoma, Myoepithelial Tumor, Low Grade Fibromyxoid Sarcoma, Sclerosing Epithelioid Fibrosarcoma , Phase 1/2, Enrolling by invitation NCT05266196.

Techniques: Clinical Proteomics

Journal: Frontiers in Pharmacology

Article Title: LSD1 inhibitors for cancer treatment: Focus on multi-target agents and compounds in clinical trials

doi: 10.3389/fphar.2023.1120911

Figure Lengend Snippet: Reversible LSD1 inhibitors.

Article Snippet: , Salarius Pharmaceuticals, LLC , A Rollover Protocol to Allow for Continued Access to the LSD1 Inhibitor Seclidemstat (SP-2577) , Ewing Sarcoma, Myxoid Liposarcoma, Desmoplastic Small Round Cell Tumor, Extraskeletal Myxoid Chondrosarcoma, Angiomatoid Fibrous Histiocytoma, Clear Cell Sarcoma, Myoepithelial Tumor, Low Grade Fibromyxoid Sarcoma, Sclerosing Epithelioid Fibrosarcoma , Phase 1/2, Enrolling by invitation NCT05266196.

Techniques:

Journal: Frontiers in Pharmacology

Article Title: LSD1 inhibitors for cancer treatment: Focus on multi-target agents and compounds in clinical trials

doi: 10.3389/fphar.2023.1120911

Figure Lengend Snippet: Reversible multi-targeting LSD1 inhibitors.

Article Snippet: , Salarius Pharmaceuticals, LLC , A Rollover Protocol to Allow for Continued Access to the LSD1 Inhibitor Seclidemstat (SP-2577) , Ewing Sarcoma, Myxoid Liposarcoma, Desmoplastic Small Round Cell Tumor, Extraskeletal Myxoid Chondrosarcoma, Angiomatoid Fibrous Histiocytoma, Clear Cell Sarcoma, Myoepithelial Tumor, Low Grade Fibromyxoid Sarcoma, Sclerosing Epithelioid Fibrosarcoma , Phase 1/2, Enrolling by invitation NCT05266196.

Techniques:

Journal: Frontiers in Pharmacology

Article Title: LSD1 inhibitors for cancer treatment: Focus on multi-target agents and compounds in clinical trials

doi: 10.3389/fphar.2023.1120911

Figure Lengend Snippet: Reversible LSD1 inhibitors in clinical trials.

Article Snippet: , Salarius Pharmaceuticals, LLC , A Rollover Protocol to Allow for Continued Access to the LSD1 Inhibitor Seclidemstat (SP-2577) , Ewing Sarcoma, Myxoid Liposarcoma, Desmoplastic Small Round Cell Tumor, Extraskeletal Myxoid Chondrosarcoma, Angiomatoid Fibrous Histiocytoma, Clear Cell Sarcoma, Myoepithelial Tumor, Low Grade Fibromyxoid Sarcoma, Sclerosing Epithelioid Fibrosarcoma , Phase 1/2, Enrolling by invitation NCT05266196.

Techniques: Clinical Proteomics

Journal: PLoS ONE

Article Title: LSD1 mediated changes in the local redox environment during the DNA damage response

doi: 10.1371/journal.pone.0201907

Figure Lengend Snippet: A. U2OS cells were irradiated with 800 nm laser light, fixed at different time points post irradiation then immunostained for LSD1. Quantification of LSD1 was determined by dividing pixel intensity of fluorescence along laser by background (uncut region). B. U2OS cells were treated with ROS sensing dye and irradiated with 800 nm light from a femtosecond near infrared (NIR) laser and either mock treated or treated with 3.4 μM of the LSD1 inhibitor GSK2879552. The pixel intensity along the laser track was quantified and divided by the background nuclear signal. The 95% confidence interval are shown above and below the best fit line for each data set. C. U2OS stained with antibody against LSD1 in either control siRNA treated cells or siLSD1 treated cells 36 hours post transfection. LSD1 expression as determined by IF was reduced approximately 39% in siLSD1 treated cells. D. Accumulation of ROS as sensed by ROS sensing dye in sicontrol treated cells vs siLSD1 treated cells. Pixel intensity of dye fluorescence (higher intensity indicates presence of ROS) along laser track divided by background was calculated to determine the kinetics of dye reaction following laser irradiation.

Article Snippet: Cells treated with LSD1 inhibitor GSK2879552 (Chemietek, Indianapolis, IN) were incubated in HBSS containing 3.4μM GSK inhibitor for 1 hour at 37°C prior to irradiation.

Techniques: Irradiation, Fluorescence, Staining, Control, Transfection, Expressing

Journal: PLoS ONE

Article Title: LSD1 mediated changes in the local redox environment during the DNA damage response

doi: 10.1371/journal.pone.0201907

Figure Lengend Snippet: LSD1 is recruited to double strand breaks. Its histone demethylase activity results in H 2 O 2 as a byproduct. H 2 O 2 reduces DNA end binding activity of Ku80 favoring Nbs1 and HR.

Article Snippet: Cells treated with LSD1 inhibitor GSK2879552 (Chemietek, Indianapolis, IN) were incubated in HBSS containing 3.4μM GSK inhibitor for 1 hour at 37°C prior to irradiation.

Techniques: Activity Assay, Binding Assay

Journal: Journal of Enzyme Inhibition and Medicinal Chemistry

Article Title: Palladium-catalysed synthesis of small-molecule epigenetic inhibitors as anticancer therapeutics

doi: 10.1080/14756366.2026.2621477

Figure Lengend Snippet: Design Strategy & Synthetic Route of Novel Benzofuran Derivatives as Potent LSD1 Inhibitors (the figure was drawn by the authors using chemdraw software).

Article Snippet: Duan et al. designed 5-cyano-3-phenylindole-based LSD1/HDAC dual inhibitors for colorectal cancer, inspired by the Novartis LSD1 inhibitor ( 350 ).

Techniques: Software

Journal: Journal of Enzyme Inhibition and Medicinal Chemistry

Article Title: Palladium-catalysed synthesis of small-molecule epigenetic inhibitors as anticancer therapeutics

doi: 10.1080/14756366.2026.2621477

Figure Lengend Snippet: Design Strategy & Synthetic Route of Novel Indole Derivatives as LSD1 Inhibitors (the figure was drawn by the authors using chemdraw software).

Article Snippet: Duan et al. designed 5-cyano-3-phenylindole-based LSD1/HDAC dual inhibitors for colorectal cancer, inspired by the Novartis LSD1 inhibitor ( 350 ).

Techniques: Software

Journal: Journal of Enzyme Inhibition and Medicinal Chemistry

Article Title: Palladium-catalysed synthesis of small-molecule epigenetic inhibitors as anticancer therapeutics

doi: 10.1080/14756366.2026.2621477

Figure Lengend Snippet: Design Strategy & Synthetic Route of Dual EZH2 & LSD1 Inhibitor (the figure was drawn by the authors using chemdraw software).

Article Snippet: Duan et al. designed 5-cyano-3-phenylindole-based LSD1/HDAC dual inhibitors for colorectal cancer, inspired by the Novartis LSD1 inhibitor ( 350 ).

Techniques: Software

Journal: Journal of Enzyme Inhibition and Medicinal Chemistry

Article Title: Palladium-catalysed synthesis of small-molecule epigenetic inhibitors as anticancer therapeutics

doi: 10.1080/14756366.2026.2621477

Figure Lengend Snippet: Design Strategy & Synthetic Route of 2‑Aryl-4-aminoquinazolin-Based LSD1 Inhibitors (the figure was drawn by the authors using chemdraw software).

Article Snippet: Duan et al. designed 5-cyano-3-phenylindole-based LSD1/HDAC dual inhibitors for colorectal cancer, inspired by the Novartis LSD1 inhibitor ( 350 ).

Techniques: Software

Journal: Journal of Enzyme Inhibition and Medicinal Chemistry

Article Title: Palladium-catalysed synthesis of small-molecule epigenetic inhibitors as anticancer therapeutics

doi: 10.1080/14756366.2026.2621477

Figure Lengend Snippet: Design Strategy & Synthetic Route of Novel 1H‑Pyrrolo[2,3‑c]pyridin Derivatives Based Lysine Specific Demethylase 1 Inhibitors (the figure was drawn by the authors using chemdraw software).

Article Snippet: Duan et al. designed 5-cyano-3-phenylindole-based LSD1/HDAC dual inhibitors for colorectal cancer, inspired by the Novartis LSD1 inhibitor ( 350 ).

Techniques: Software

Journal: Journal of Enzyme Inhibition and Medicinal Chemistry

Article Title: Palladium-catalysed synthesis of small-molecule epigenetic inhibitors as anticancer therapeutics

doi: 10.1080/14756366.2026.2621477

Figure Lengend Snippet: Design Strategy & Synthetic Route of Dual LSD1 and HDAC Inhibitor (the figure was drawn by the authors using chemdraw software).

Article Snippet: Duan et al. designed 5-cyano-3-phenylindole-based LSD1/HDAC dual inhibitors for colorectal cancer, inspired by the Novartis LSD1 inhibitor ( 350 ).

Techniques: Software

Journal: Journal of Enzyme Inhibition and Medicinal Chemistry

Article Title: Palladium-catalysed synthesis of small-molecule epigenetic inhibitors as anticancer therapeutics

doi: 10.1080/14756366.2026.2621477

Figure Lengend Snippet: Design Strategy & Synthetic Route of Novel acridine-based LSD1 inhibitors (the figure was drawn by the authors using chemdraw software).

Article Snippet: Duan et al. designed 5-cyano-3-phenylindole-based LSD1/HDAC dual inhibitors for colorectal cancer, inspired by the Novartis LSD1 inhibitor ( 350 ).

Techniques: Software

Journal: Journal of Enzyme Inhibition and Medicinal Chemistry

Article Title: Palladium-catalysed synthesis of small-molecule epigenetic inhibitors as anticancer therapeutics

doi: 10.1080/14756366.2026.2621477

Figure Lengend Snippet: Design Strategy & Synthetic Route of Dual LSD1 & HDAC Inhibitor (the figure was drawn by the authors using chemdraw software).

Article Snippet: Duan et al. designed 5-cyano-3-phenylindole-based LSD1/HDAC dual inhibitors for colorectal cancer, inspired by the Novartis LSD1 inhibitor ( 350 ).

Techniques: Software

Journal: Journal of Enzyme Inhibition and Medicinal Chemistry

Article Title: Palladium-catalysed synthesis of small-molecule epigenetic inhibitors as anticancer therapeutics

doi: 10.1080/14756366.2026.2621477

Figure Lengend Snippet: Design Strategy & Synthetic Route of Novel 5‑Cyano-3-phenylindole-Based LSD1/HDAC Dual Inhibitors (the figure was drawn by the authors using chemdraw software).

Article Snippet: Duan et al. designed 5-cyano-3-phenylindole-based LSD1/HDAC dual inhibitors for colorectal cancer, inspired by the Novartis LSD1 inhibitor ( 350 ).

Techniques: Software

Journal: Journal of Enzyme Inhibition and Medicinal Chemistry

Article Title: Palladium-catalysed synthesis of small-molecule epigenetic inhibitors as anticancer therapeutics

doi: 10.1080/14756366.2026.2621477

Figure Lengend Snippet: Design Strategy & Synthetic Route of CC-90011 (328): A Lysine Specific Demethylase 1 Inhibitors (the figure was drawn by the authors using chemdraw software).

Article Snippet: Duan et al. designed 5-cyano-3-phenylindole-based LSD1/HDAC dual inhibitors for colorectal cancer, inspired by the Novartis LSD1 inhibitor ( 350 ).

Techniques: Software