Relevant bibliographies by topics / Molecular glue degrader

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Academic literature on the topic 'Molecular glue degrader'

Author: Grafiati
Published: 4 June 2025
Last updated: 1 August 2025

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Journal articles on the topic "Molecular glue degrader"

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Zhang, Yujia, Jessica Bates, Benoit Gourdet, et al. "Abstract 3429: Beyond cereblon IMIDs - biophysics-based discovery of novel molecular glue chemotypes." Cancer Research 83, no. 7_Supplement (2023): 3429. http://dx.doi.org/10.1158/1538-7445.am2023-3429.

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Abstract Molecular glue degraders are compact, low molecular weight molecules that can efficiently induce specific and potent degradation of a target protein. This class of degraders function by inducing interactions between a target of interest and a ubiquitin-ligase, either by stabilization of weak pre-existing interactions, or by generation of entirely novel interactions. These molecules offer significant opportunity beyond heterobifunctional degraders such as PROTACs, not least in terms of improved molecular properties. However, beyond the IMID molecular glues, typified by thalidomide, pom
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Jordan, Allan M., Kuhulika Bhalla, Helen Burston, et al. "Abstract 1660: Seeking new glues - Toward an E3 ligase-agnostic molecular glue degrader identification platform." Cancer Research 85, no. 8_Supplement_1 (2025): 1660. https://doi.org/10.1158/1538-7445.am2025-1660.

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Abstract Targeted Protein Degradation (TPD) is a rapidly growing modality in oncology and is broadly driven by development of bifunctional (PROTAC-type) or monovalent degraders. Whilst the latter group largely consists of molecular glue degraders (MGDs), it also encompasses compounds that act as degraders via allosteric or other mechanisms. Screening for compounds with MGD properties can be undertaken via biophysical methods, where proximity of an effector and target protein is measured, limiting the effect of the compound to a known, selected effector, such as a particular ubiquitin-ligase of
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Liu, Yuan, Mads Larsen, Bo Lin, et al. "Abstract 6070: Identification of a molecular glue degrader that engages a cancer-specific E3 ligase." Cancer Research 84, no. 6_Supplement (2024): 6070. http://dx.doi.org/10.1158/1538-7445.am2024-6070.

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Abstract To date, most successful molecular glues have leveraged ubiquitously expressed E3 ligases, most notably Cereblon in the case of the thalidomide derivatives. However, a number of specific E3 ligases are highly over-expressed in certain tumors. Compounds that engage such tumor-specific E3 ligases might provide a unique opportunity to develop molecular glues with higher therapeutic indexes. One such tumor-specific E3 ligase is FBXO5, a member of the F-box family of E3 ligases. Expression analysis suggests this E3 ligase is highly expressed in a wide array of tumor tissues when compared t
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Kang, Incheol, Seungoh Seo, and Seong Hyeok Cho. "Abstract 384: IPS-06061, a novel TPD molecular glue degrader targeting KRAS G12D." Cancer Research 85, no. 8_Supplement_1 (2025): 384. https://doi.org/10.1158/1538-7445.am2025-384.

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Abstract We have discovered a novel KRAS G12D-degrading Molecular Glue using IPS's cutting-edge ProGlu AI-based drug discovery platform and PPIExplorer, an IPS-Chip based Proteomics technology. ProGlu accurately predicts PPI between E3 ligase and KRAS G12D through MD simulation, enabling de novo design of MG degraders. One such degrader, namely IPS-06061, was successfully synthesized and confirmed a strong anti-tumor efficacy using a xenograft animal model. These data demonstrate that KRAS MG will be a promising new therapeutic modality for the treatment of PDA, CRC, and NSCLC. Citation Format
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Bouvier, Corentin, Rachel Lawrence, Francesca Cavallo, et al. "Breaking Bad Proteins—Discovery Approaches and the Road to Clinic for Degraders." Cells 13, no. 7 (2024): 578. http://dx.doi.org/10.3390/cells13070578.

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Proteolysis-targeting chimeras (PROTACs) describe compounds that bind to and induce degradation of a target by simultaneously binding to a ubiquitin ligase. More generally referred to as bifunctional degraders, PROTACs have led the way in the field of targeted protein degradation (TPD), with several compounds currently undergoing clinical testing. Alongside bifunctional degraders, single-moiety compounds, or molecular glue degraders (MGDs), are increasingly being considered as a viable approach for development of therapeutics, driven by advances in rational discovery approaches. This review fo
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Martin, Leenus, Nasrin Rastgoo, Jean-Francois Brazeau, et al. "Abstract 6375: Discovery and characterization of novel, potent and selective CDK2 molecular glue degrader against CCNE1-amplified tumors." Cancer Research 85, no. 8_Supplement_1 (2025): 6375. https://doi.org/10.1158/1538-7445.am2025-6375.

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Abstract Introduction: The Cyclin-Dependent Kinases (CDKs) with their cyclin binding partners are associated with cell cycle progression and transcriptional regulation. Dysregulation of the cell cycle is a hallmark of cancer and targeting CDKs is a key oncology therapeutic strategy. Cyclin E1 (CCNE1) amplification/overexpression and activation of its canonical binding partner CDK2 is a major resistance mechanism in CDK4/6i breast cancer therapy. In addition, elevated CCNE1 expression and complexation with CDK2 promotes aberrant cell cycling which is associated with poor prognosis in ovarian an
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Chan, Chi-Chung, Chun-Sing Li, Lihong Hu, Wenxi Li, Zhenzhen Zhu, and Shuhui Chen. "Abstract 393: Discovery of novel, potent and orally active GSPT1 molecular glue degraders." Cancer Research 85, no. 8_Supplement_1 (2025): 393. https://doi.org/10.1158/1538-7445.am2025-393.

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Abstract Molecular glue degrader (MGD) is an emerging therapeutic strategy offering an exciting alternative to traditional small molecules exploring new target space. These small molecules interact with the ubiquitin-proteasome system (UPS) to promote degradation of protein of interest (POI), especially those considered to be challenging targets (e.g., GSPT1, VAV1, WIZ, BCL6, STAT6, IKZFs). In fact, clinical proof of concept has been obtained with immunomodulatory drugs such as thalidomide, lenalidomide and pomalidomide, which degrade IKZF1/IKZF3. GSPT1 (G1 to S phase transition protein 1) is
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Duncan, Aundrietta D., Daniela Y. Santiesteban, Nadeem Q. Mirza, et al. "Abstract 6253: SP-3164, a novel molecular glue degrader with activity in preclinical models of multiple myeloma." Cancer Research 83, no. 7_Supplement (2023): 6253. http://dx.doi.org/10.1158/1538-7445.am2023-6253.

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Abstract Multiple myeloma (MM) makes up approximately 10% of all hematologic malignancies, with increasing incidence worldwide. Though treatment options for newly diagnosed patients have evolved in recent years, they are not curative, and relapse is common with 2,500-3,000 relapsed or refractory (R/R) MM US patients seeking novel treatments, annually. Cereblon (CRBN)-binding Ikaros and Aiolos (I/A) protein degraders (i.e., lenalidomide (LEN) and pomalidomide (POM)) have had great success in treating MM. However, due to the unstable chiral nature of the CRBN-binding moiety, common to these mole
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Read, Timothy J., Richard Steel, Leah Damon, et al. "Abstract LB007: Discovery of a novel molecular glue degrader of Nrf2." Cancer Research 85, no. 8_Supplement_2 (2025): LB007. https://doi.org/10.1158/1538-7445.am2025-lb007.

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Abstract Nrf2 is an oncogenic transcription factor that is frequently overactive in tumors bearing mutations in the NRF2/KEAP1 pathway, but to date, no direct Nrf2 inhibitors have been tested clinically. Using high-throughput transcriptomic screens in combination with biophysical assays, we discovered ARP-4922 as a potent molecular glue degrader of Nrf2. ARP-4922 degrades Nrf2 in a proteasome- and cullin- dependent manner with exceptional activity, especially in NRF2/KEAP1-mutant backgrounds. Genetic experiments identified the likely E3 ligase driving ARP-4922-mediated degradation of Nrf2, and
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Au, CheukMan Cherie, Michelle Naidoo, Catrina Estrella, et al. "Abstract 1645: Developing first-in-class AR-V7/AR-fl molecular glue degrader to revolutionize prostate cancer therapeutics." Cancer Research 85, no. 8_Supplement_1 (2025): 1645. https://doi.org/10.1158/1538-7445.am2025-1645.

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Abstract Metastatic castration resistance prostate cancer (mCRPC) is a lethal disease due to the resistance of standard-of-care (SoC) treatments, including androgen receptor (AR) pathway inhibitors and taxanes. Treatment resistance occurs partly due to the expression of constitutively active AR splice variants, that hijack AR signaling even after castration. AR-V7 is the most prevalent variant and is expressed in ∼75% of patients with mCRPC, which confers resistance to SoC treatment. Currently, there is no AR-V7 pharmacologic inhibitor, limiting patients’ therapeutic options. Thus, AR-V7 inhib
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Book chapters on the topic "Molecular glue degrader"

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Malone, Marie L., Nicholas A. Sanchez, Stacy L. Hu, and Christopher B. Phelps. "Application of DELs for E3 Ligase Ligand Discovery and Targeted Protein Degradation." In DNA-encoded Library Technology for Drug Discovery. Royal Society of Chemistry, 2025. https://doi.org/10.1039/9781788016032-00134.

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Targeted protein degradation (TPD) provides new therapeutic opportunities beyond traditional inhibitors. TPD relies on the ability to induce proximity between an E3 ligase and the target of interest, harnessing the ubiquitin proteasome system to ubiquitylate and degrade the target. This proximity can be induced by either monofunctional ligands (molecular glues) or bifunctional molecules that tether ligases and target ligands together. DNA encoded libraries (DELs) provide rapid access to diverse chemical space for ligand discovery and, by their design, facilitate the development of both molecul
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Jean, N’Dre, Hamideh Salehi, Marie Maumus, Danièle Noël, Yolande Koffi-Gnagne, and Frédéric Cuisinier. "Characterization of Degraded Cartilage Using Confocal Raman Microscopy." In Cartilage - Recent Findings and Treatment [Working Title]. IntechOpen, 2023. http://dx.doi.org/10.5772/intechopen.107310.

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Osteoarthritis is a degenerative disease with pathological changes at the molecular level. Moreover, the damage to articular cartilage is irreversible. Early detection and the ability to follow the progression of osteoarthritis are essential to anticipate management. To characterize degraded human articular cartilage and to identify cellular changes that are precursors of phenotypic matrix changes in osteoarthritis, normal and degraded articular cartilage explants were harvested from the same patient’s knee after informed consent. The blocks were washed several times (four times) with phosphat
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Conference papers on the topic "Molecular glue degrader"

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Ainscow, Edward K., Adrian Campbell, Michael Cripps, et al. "Abstract P051: Identification of an orally bioavailable dual Cyclin K glue degrader - CDK12/13 inhibitor." In Abstracts: AACR-NCI-EORTC Virtual International Conference on Molecular Targets and Cancer Therapeutics; October 7-10, 2021. American Association for Cancer Research, 2021. http://dx.doi.org/10.1158/1535-7163.targ-21-p051.

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Gavory, Gerald, Bernhard Fasching, Debora Bonenfant, et al. "Abstract LBA004: Identification of GSPT1-directed molecular glue degrader (MGD) for the treatment of Myc-driven breast cancer." In Abstracts: AACR-NCI-EORTC Virtual International Conference on Molecular Targets and Cancer Therapeutics; October 7-10, 2021. American Association for Cancer Research, 2021. http://dx.doi.org/10.1158/1535-7163.targ-21-lba004.

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Thompson, Peggy A., Pengyu Yang, Yujun Huang, et al. "1393 Discovery of PLX-4107, a selective IKZF2 molecular glue degrader, that modulates suppressive regulatory T cells and demonstrates anti-tumor activity." In SITC 38th Annual Meeting (SITC 2023) Abstracts. BMJ Publishing Group Ltd, 2023. http://dx.doi.org/10.1136/jitc-2023-sitc2023.1393.

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Cartwright, A., F. Desai, S. Vora, et al. "POS1200 MRT-6160, A VAV1-DIRECTED MOLECULAR GLUE DEGRADER, REDUCES JOINT INFLAMMATION, CYTOKINE PRODUCTION, AND AUTOANTIBODY LEVELS IN A COLLAGEN-INDUCED ARTHRITIS DISEASE MODEL." In EULAR 2024 European Congress of Rheumatology, 12-15 June. Vienna, Austria. BMJ Publishing Group Ltd and European League Against Rheumatism, 2024. http://dx.doi.org/10.1136/annrheumdis-2024-eular.262.

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Angles-Cano, E., R. Pannell, and V. Gurewich. "FIBRIN-BINDING STUDIES OF PRO-UROKINASE (PRO-UK) USING SOLID PHASE FIBRIN PLATES." In XIth International Congress on Thrombosis and Haemostasis. Schattauer GmbH, 1987. http://dx.doi.org/10.1055/s-0038-1642904.

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Pro-UK is a single chain urokinase-type plasminogen activator (scu-PA) which has fibrin selective thrombolytic properties. However, quantitative data on pro-UK binding to fibrin and on the mechanism of its fibrin enhanced activation of plasminogen have been difficult to obtain. In the present study, a well defined fibrin network constructed on glutaraldehyde-activated PVC plates (Anal. Biochem. 153 : 201-210, 1986) and highly purified pro-UK (99 % scu-PA) were used. Binding was investigated as follows : varying dilutions of pro-UK in the presence of a trace amount of I-labeled pro-UK in buffer
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