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Home » Topics » Drugs » Degradation inducer

Degradation inducer
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Microscopic image of acute myeloid leukemia (AML) cells.
Cancer

Oral KAT2A/B degrader gets go-ahead for acute myeloid leukemia

Feb. 5, 2025
Auron Therapeutics Inc. has received FDA clearance of its IND application for its oral KAT2A/B degrader AUTX-703 in hematological malignancies. A phase I proof-of-concept trial in acute myeloid leukemia (AML) will open enrollment this quarter, supported by a recently completed $27 million series B financing.
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Art concept for molecular glue degradation
Cancer

Seed’s RBM39 degrader awarded US orphan drug, rare pediatric disease designations

Jan. 29, 2025
Seed Therapeutics Inc.’s ST-01156 has been awarded orphan drug designation for the treatment of Ewing sarcoma as well as rare pediatric disease designation by the FDA.
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Cancer

SIAIS-562055, a SOS1 PROTAC with activity in models of KRAS-mutant tumors and BCR-ABL-positive leukemia

Jan. 21, 2025
Son of sevenless homolog 1 (SOS1) is an essential guanine nucleotide exchange factor (GEF) in KRAS-driven tumors, and it also functions as a downstream node protein of BCR-ABL, suggesting its critical role in the pathogenesis of chronic myeloid leukemia (CML). Investigators at Shanghaitech University have reported the discovery and preclinical characterization of a novel potent SOS1 proteolysis targeting chimera (PROTAC) – SIAIS-562055 – being developed as an anticancer agent.
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Liver illustration
Gastrointestinal

HDAC6 degrader protects from acute liver injury

Jan. 20, 2025
In the preclinical setting, inhibitors of histone deacetylase 6 (HDAC6) have proven effective at reducing liver inflammation through modulation of the immune response.
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Art concept for drug research
Cancer

Novel PD-L1 degrader described in China

Jan. 8, 2025
Immune checkpoint blockade is one of the major advances in cancer treatment in recent years. However, the majority of immune checkpoints are embedded in the cell membrane and this fact represents a limitation for targeted degradation using proteolysis-targeting chimeras (PROTACs).
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Doctor points at molecular structure
Cancer

New class of selective estrogen receptor degraders reported

Jan. 7, 2025
Aromatase inhibitors (AI) are among the most widely used therapies in the treatment of breast tumors expressing estrogen receptor α (ERα). Alone or in combination with other agents, they are the standard of care for hormone receptor-positive tumors.
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Illustration of chronic lymphocytic leukemia cells
Cancer

New MALT1 degrader shows potent activity in preclinical lymphoma models

Dec. 30, 2024
The protease mucosa-associated lymphoid tissue lymphoma translocation 1 (MALT1) is a signaling protein with both molecular scaffolding and protease activity involved in lymphocyte activation. MALT1 is considered a therapeutic target for chronic lymphocytic leukemia (CLL) in patients who develop resistance to Bruton tyrosine kinase (BTK) inhibitors.
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Prostate cancer cells
Cancer

ATC-324 targets prostate cancer AR mutants and splice variants

Dec. 10, 2024
Researchers from AUTOTAC Bio Inc. and affiliated organizations presented preclinical data for ATC-324, a novel autophagy-targeting chimera (AUTOTAC) designed to induce androgen receptor (AR) degradation.
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Joint pain
Musculoskeletal

Gilead’s GS-6791 ameliorates arthritis symptoms in mice

Nov. 21, 2024
Interleukin-1 receptor-associated kinase 4 is critical in the modulation of inflammatory responses through Toll-like receptor and IL-1R signaling.
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Cancer

MBT-C101, a selective and potent HSP90 chaperone-mediated degrader of PI3Kα

Nov. 18, 2024
MBT-C101 is a selective, potentially first-in-class potent HSP90 chaperone-mediated degrader of PI3Kα, for the treatment of breast cancer. It was developed by Magicbullet Therapeutics Inc. using the company’s Chaperone-mediated Degrader (CM-Degrader) platform.
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