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   Articles with "degrader" as a keyword



Development of selective mono or dual PROTAC degrader probe of CDK isoforms.

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recommendations! Published in 2019 at "European journal of medicinal chemistry"

DOI: 10.1016/j.ejmech.2019.111952

Abstract: Cyclin-dependent kinase (CDK) family members are promising molecular targets in discovering potent inhibitors in disease settings, they function differentially. CDK2, CDK4 and CDK6, directly regulate the cell cycle, while CDK9 primarily modulates the transcription regulation.… read more here.

Keywords: degrader; development selective; protac; selective mono ... See more keywords
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Potent and Selective Mitogen-Activated Protein Kinase Kinase 1/2 (MEK1/2) Heterobifunctional Small-molecule Degraders.

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recommendations! Published in 2020 at "Journal of medicinal chemistry"

DOI: 10.1021/acs.jmedchem.0c01609

Abstract: Previously, we reported a first-in-class von Hippel-Lindau (VHL)-recruiting mitogen-activated protein kinase kinases 1 and 2 (MEK1/2) degrader, MS432. To date, only two MEK1/2 degrader papers have been published and very limited structure-activity relationships (SAR) have… read more here.

Keywords: degrader; kinase; activated protein; mek1 degrader ... See more keywords

Development of Human Carbonic Anhydrase II Heterobifunctional Degraders

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recommendations! Published in 2023 at "Journal of Medicinal Chemistry"

DOI: 10.1021/acs.jmedchem.2c01843

Abstract: Human carbonic anhydrase II (hCAII) is a metalloenzyme essential to critical physiological processes in the body. hCA inhibitors are used clinically for the treatment of indications ranging from glaucoma to epilepsy. Targeted protein degraders have… read more here.

Keywords: human carbonic; development human; carbonic anhydrase; heterobifunctional degraders ... See more keywords

Discovery of LL-K8-22: A Selective, Durable, and Small-Molecule Degrader of the CDK8-Cyclin C Complex.

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recommendations! Published in 2023 at "Journal of medicinal chemistry"

DOI: 10.1021/acs.jmedchem.2c02045

Abstract: The CDK8-cyclin C complex is an important anti-tumor target, but unlike CDK8, cyclin C remains undruggable. Modulators regulating cyclin C activity directly are still under development. Here, a series of hydrophobic tagging-based degraders of the… read more here.

Keywords: cdk8 cyclin; molecule; degrader; cyclin complex ... See more keywords

Discovery of LLC0424 as a Potent and Selective in Vivo NSD2 PROTAC Degrader

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recommendations! Published in 2024 at "Journal of Medicinal Chemistry"

DOI: 10.1021/acs.jmedchem.3c01765

Abstract: Nuclear receptor-binding SET domain-containing 2 (NSD2), a methyltransferase that primarily installs the dimethyl mark on lysine 36 of histone 3 (H3K36me2), has been recognized as a promising therapeutic target against cancer. However, existing NSD2 inhibitors… read more here.

Keywords: potent selective; llc0424 potent; llc0424; degrader ... See more keywords

Discovery and Characterization of a Novel Cereblon-Recruiting PRC1 Bridged PROTAC Degrader.

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recommendations! Published in 2024 at "Journal of medicinal chemistry"

DOI: 10.1021/acs.jmedchem.4c00538

Abstract: Bridged PROTAC is a novel protein complex degrader strategy that exploits the target protein's binding partner to degrade undruggable proteins by inducing proximity to an E3 ubiquitin ligase. In this study, we discovered for the… read more here.

Keywords: discovery characterization; characterization novel; novel cereblon; bridged protac ... See more keywords

Discovery of a Highly Potent and Selective HDAC8 Degrader: Advancing the Functional Understanding and Therapeutic Potential of HDAC8.

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recommendations! Published in 2024 at "Journal of medicinal chemistry"

DOI: 10.1021/acs.jmedchem.4c00761

Abstract: HDAC8 plays crucial roles in biological processes, from gene regulation to cell motility, making it a highly desirable target for therapeutic intervention. HDAC8 also has deacetylase-independent activity which cannot be blocked by a conventional inhibitor.… read more here.

Keywords: hdac8 degrader; potent selective; highly potent; degrader ... See more keywords

Discovery of a Highly Potent, Selective and Efficacious USP7 Degrader for the Treatment of Acute Lymphoblastic Leukemia.

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recommendations! Published in 2024 at "Journal of medicinal chemistry"

DOI: 10.1021/acs.jmedchem.4c01134

Abstract: USP7 is an attractive therapeutic target for cancers, especially for acute lymphoblastic leukemia (ALL) with wild-type p53. Herein, we report the discovery of XM-U-14 as a highly potent, selective and efficacious USP7 proteolysis-targeting chimera degrader.… read more here.

Keywords: potent selective; acute lymphoblastic; lymphoblastic leukemia; highly potent ... See more keywords

Discovery of the First Clinical Protein Degrader for the Treatment of Autoimmune Indications: Orally Bioavailable and Selective IRAK4 Degrader KT-474.

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recommendations! Published in 2024 at "Journal of medicinal chemistry"

DOI: 10.1021/acs.jmedchem.4c02264

Abstract: IRAK4 inhibitors have been sought for the treatment of a host of diseases, however, recent evidence suggests a protein degradation approach might have advantages over an inhibitor. This viewpoint summarizes the discovery of KT-474─a selective… read more here.

Keywords: treatment; orally bioavailable; discovery first; autoimmune indications ... See more keywords

Structure-Guided Design of ISOX-DUAL-Based Degraders Targeting BRD4 and CBP/EP300: A Case of Degrader Collapse

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recommendations! Published in 2025 at "Journal of Medicinal Chemistry"

DOI: 10.1021/acs.jmedchem.5c00395

Abstract: Degraders with dual activity against BRD4 and CBP/EP300 were designed. A structure-guided design approach was taken to assess and test potential exit vectors on the dual BRD4 and CBP/EP300 inhibitor, ISOX-DUAL. Candidate degrader panels revealed… read more here.

Keywords: isox dual; degrader; cbp ep300; brd4 ... See more keywords

Discovery of the First Potent PI3K/mTOR Dual-Targeting PROTAC Degrader for Efficient Modulation of the PI3K/AKT/mTOR Pathway.

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recommendations! Published in 2025 at "Journal of medicinal chemistry"

DOI: 10.1021/acs.jmedchem.5c02244

Abstract: The phosphoinositide 3-kinase (PI3K)/protein kinase B (AKT)/mammalian target of rapamycin (mTOR) pathway is a critical regulator of cell growth and metabolism, and its dysregulation is implicated in various cancers. In this study, a series of… read more here.

Keywords: degrader; pi3k mtor; mtor; mtor pathway ... See more keywords