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vhl-based protacs  (Amgen)

 
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    Amgen vhl-based protacs
    Vhl Based Protacs, supplied by Amgen, used in various techniques. Bioz Stars score: 90/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
    https://www.bioz.com/product/vhl-based+protacs/vhl+based+protacs/pm35295813-2-11-35
    Average 90 stars, based on 1 article reviews
    vhl-based protacs - by Bioz Stars, 2026-09
    90/100 stars

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    Related Articles

    Activity Assay:

    Article Title: Profiling of diverse tumor types establishes the broad utility of VHL-based ProTaCs and triages candidate ubiquitin ligases.
    Article Snippet: Profiling of diverse tumor types establishes the broad utility of VHL-based ProTaCs and triages candidate ubiquitin ligases Xin Luo,2 Ivonne Archibeque,1 Ken Dellamaggiore,1 Kate Smither,1 Oliver Homann,2 James Russell Lipford,1 and Dane Mohl1,3,* 1AMGEN Research, Amgen Inc, Thousand Oaks, CA 91320, USA 2AMGEN Research, Amgen Inc, South San Francisco, CA 94080, USA 3Lead contact *Correspondence: dmohl@amgen.com https://doi.org/10.1016/j.isci.

    Article Title: Profiling of diverse tumor types establishes the broad utility of VHL-based ProTaCs and triages candidate ubiquitin ligases.
    Article Snippet: Profiling of diverse tumor types establishes the broad utility of VHL-based ProTaCs and triages candidate ubiquitin ligases Xin Luo, Ivonne Archibeque, Ken Dellamaggiore, Kate Smither, Oliver Homann, James Russell Lipford, Dane Mohl dmohl@amgen.com Highlights Profiling of diverse tumor types establishes the broad utility of VHL-based PROTACs CRBN-dependent dBET1 activity is frequently suppressed in cancer cell lines Copy loss and mRNA expression predict the activity of VHL and CRBNdependent PROTACs Luo et al., iScience 25, 103985 March 18, 2022 a 2022 The Author(s). https://doi.org/10.1016/ j.isci.2022.103985 ll OPEN ACCESS iScience

    Expressing:

    Article Title: Profiling of diverse tumor types establishes the broad utility of VHL-based ProTaCs and triages candidate ubiquitin ligases.
    Article Snippet: Profiling of diverse tumor types establishes the broad utility of VHL-based ProTaCs and triages candidate ubiquitin ligases Xin Luo,2 Ivonne Archibeque,1 Ken Dellamaggiore,1 Kate Smither,1 Oliver Homann,2 James Russell Lipford,1 and Dane Mohl1,3,* 1AMGEN Research, Amgen Inc, Thousand Oaks, CA 91320, USA 2AMGEN Research, Amgen Inc, South San Francisco, CA 94080, USA 3Lead contact *Correspondence: dmohl@amgen.com https://doi.org/10.1016/j.isci.

    Article Title: Profiling of diverse tumor types establishes the broad utility of VHL-based ProTaCs and triages candidate ubiquitin ligases.
    Article Snippet: Profiling of diverse tumor types establishes the broad utility of VHL-based ProTaCs and triages candidate ubiquitin ligases Xin Luo, Ivonne Archibeque, Ken Dellamaggiore, Kate Smither, Oliver Homann, James Russell Lipford, Dane Mohl dmohl@amgen.com Highlights Profiling of diverse tumor types establishes the broad utility of VHL-based PROTACs CRBN-dependent dBET1 activity is frequently suppressed in cancer cell lines Copy loss and mRNA expression predict the activity of VHL and CRBNdependent PROTACs Luo et al., iScience 25, 103985 March 18, 2022 a 2022 The Author(s). https://doi.org/10.1016/ j.isci.2022.103985 ll OPEN ACCESS iScience



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    Image Search Results


    The first disclosed VHL ligand-containing PROTACs. (a) BRD4 targeting PROTAC MZ-1 . (b) ER PROTAC 4 .

    Journal: Expert Opinion on Therapeutic Patents

    Article Title: A patent review of von Hippel-Lindau (VHL)-recruiting chemical matter: E3 ligase ligands for PROTACs and targeted protein degradation (2019–present)

    doi: 10.1080/13543776.2024.2446232

    Figure Lengend Snippet: The first disclosed VHL ligand-containing PROTACs. (a) BRD4 targeting PROTAC MZ-1 . (b) ER PROTAC 4 .

    Article Snippet: Work in 2019 by Arvinas disclosed a range of VHL-based PROTACs that degrade SMARCA2/4 proteins which included a range of different heterocycles ( ) [ ].

    Techniques:

    Early PROTACs exemplifying the various exit vectors on the VHL ligand. (a) The five primary exit vector positions within the VH032 ligand. (b) Cocrystal structure of VH032 bound to VCB (PDB 4W9H). (c, d) BRD2/3/4 targeting PROTACs ARV-771 , AT1 and AT7 . (e) BRD7/9 targeting PROTAC VZ185 . (f) AR targeting PROTAC ARD-69 .

    Journal: Expert Opinion on Therapeutic Patents

    Article Title: A patent review of von Hippel-Lindau (VHL)-recruiting chemical matter: E3 ligase ligands for PROTACs and targeted protein degradation (2019–present)

    doi: 10.1080/13543776.2024.2446232

    Figure Lengend Snippet: Early PROTACs exemplifying the various exit vectors on the VHL ligand. (a) The five primary exit vector positions within the VH032 ligand. (b) Cocrystal structure of VH032 bound to VCB (PDB 4W9H). (c, d) BRD2/3/4 targeting PROTACs ARV-771 , AT1 and AT7 . (e) BRD7/9 targeting PROTAC VZ185 . (f) AR targeting PROTAC ARD-69 .

    Article Snippet: Work in 2019 by Arvinas disclosed a range of VHL-based PROTACs that degrade SMARCA2/4 proteins which included a range of different heterocycles ( ) [ ].

    Techniques: Plasmid Preparation

    VHL-based PROTACs patented by the University of Michigan in 2024. SMARCA2 degradation reported from HiBiT assay.

    Journal: Expert Opinion on Therapeutic Patents

    Article Title: A patent review of von Hippel-Lindau (VHL)-recruiting chemical matter: E3 ligase ligands for PROTACs and targeted protein degradation (2019–present)

    doi: 10.1080/13543776.2024.2446232

    Figure Lengend Snippet: VHL-based PROTACs patented by the University of Michigan in 2024. SMARCA2 degradation reported from HiBiT assay.

    Article Snippet: Work in 2019 by Arvinas disclosed a range of VHL-based PROTACs that degrade SMARCA2/4 proteins which included a range of different heterocycles ( ) [ ].

    Techniques:

    Indazole modifications introduced in PROTACs by Kymera in 2023. Degradation at 6 h in MOLT-4 in ELISA assay.

    Journal: Expert Opinion on Therapeutic Patents

    Article Title: A patent review of von Hippel-Lindau (VHL)-recruiting chemical matter: E3 ligase ligands for PROTACs and targeted protein degradation (2019–present)

    doi: 10.1080/13543776.2024.2446232

    Figure Lengend Snippet: Indazole modifications introduced in PROTACs by Kymera in 2023. Degradation at 6 h in MOLT-4 in ELISA assay.

    Article Snippet: Work in 2019 by Arvinas disclosed a range of VHL-based PROTACs that degrade SMARCA2/4 proteins which included a range of different heterocycles ( ) [ ].

    Techniques: Enzyme-linked Immunosorbent Assay

    SMARCA degrading PROTACs patented by Arvinas bearing modification to the RHS thiazole.

    Journal: Expert Opinion on Therapeutic Patents

    Article Title: A patent review of von Hippel-Lindau (VHL)-recruiting chemical matter: E3 ligase ligands for PROTACs and targeted protein degradation (2019–present)

    doi: 10.1080/13543776.2024.2446232

    Figure Lengend Snippet: SMARCA degrading PROTACs patented by Arvinas bearing modification to the RHS thiazole.

    Article Snippet: Work in 2019 by Arvinas disclosed a range of VHL-based PROTACs that degrade SMARCA2/4 proteins which included a range of different heterocycles ( ) [ ].

    Techniques: Modification

    BRAF PROTACs patented by Arvinas containing several changes to the methyl thiazole region.

    Journal: Expert Opinion on Therapeutic Patents

    Article Title: A patent review of von Hippel-Lindau (VHL)-recruiting chemical matter: E3 ligase ligands for PROTACs and targeted protein degradation (2019–present)

    doi: 10.1080/13543776.2024.2446232

    Figure Lengend Snippet: BRAF PROTACs patented by Arvinas containing several changes to the methyl thiazole region.

    Article Snippet: Work in 2019 by Arvinas disclosed a range of VHL-based PROTACs that degrade SMARCA2/4 proteins which included a range of different heterocycles ( ) [ ].

    Techniques:

    Halo-phenyl containing KRAS PROTACs patented by Erasca.

    Journal: Expert Opinion on Therapeutic Patents

    Article Title: A patent review of von Hippel-Lindau (VHL)-recruiting chemical matter: E3 ligase ligands for PROTACs and targeted protein degradation (2019–present)

    doi: 10.1080/13543776.2024.2446232

    Figure Lengend Snippet: Halo-phenyl containing KRAS PROTACs patented by Erasca.

    Article Snippet: Work in 2019 by Arvinas disclosed a range of VHL-based PROTACs that degrade SMARCA2/4 proteins which included a range of different heterocycles ( ) [ ].

    Techniques:

    Small group replacements of Me-thiazole. (a) SMARCA2 PROTACs from Foghorn therapeutics containing smaller groups in place of the thiazole. (b) BCL-xL degrader 362 by Kymera containing an alkyne moiety.

    Journal: Expert Opinion on Therapeutic Patents

    Article Title: A patent review of von Hippel-Lindau (VHL)-recruiting chemical matter: E3 ligase ligands for PROTACs and targeted protein degradation (2019–present)

    doi: 10.1080/13543776.2024.2446232

    Figure Lengend Snippet: Small group replacements of Me-thiazole. (a) SMARCA2 PROTACs from Foghorn therapeutics containing smaller groups in place of the thiazole. (b) BCL-xL degrader 362 by Kymera containing an alkyne moiety.

    Article Snippet: Work in 2019 by Arvinas disclosed a range of VHL-based PROTACs that degrade SMARCA2/4 proteins which included a range of different heterocycles ( ) [ ].

    Techniques:

    Ester pro-drug masking of hydroxyproline. (a) PROTACs with modified Hyp groups that degrade SMARCA2/4 reported by Aurigene in 2019. D (100 nM) = degradation of SMARCA2 achieved after compound treatment at 100 nM. ‘-’ indicates data not reported. (b) PTK6 targeting PROTAC 373 .

    Journal: Expert Opinion on Therapeutic Patents

    Article Title: A patent review of von Hippel-Lindau (VHL)-recruiting chemical matter: E3 ligase ligands for PROTACs and targeted protein degradation (2019–present)

    doi: 10.1080/13543776.2024.2446232

    Figure Lengend Snippet: Ester pro-drug masking of hydroxyproline. (a) PROTACs with modified Hyp groups that degrade SMARCA2/4 reported by Aurigene in 2019. D (100 nM) = degradation of SMARCA2 achieved after compound treatment at 100 nM. ‘-’ indicates data not reported. (b) PTK6 targeting PROTAC 373 .

    Article Snippet: Work in 2019 by Arvinas disclosed a range of VHL-based PROTACs that degrade SMARCA2/4 proteins which included a range of different heterocycles ( ) [ ].

    Techniques: Modification

    Folate caged PROTACs from BIDMC targeting BRD, MEK and AKT proteins respectively.

    Journal: Expert Opinion on Therapeutic Patents

    Article Title: A patent review of von Hippel-Lindau (VHL)-recruiting chemical matter: E3 ligase ligands for PROTACs and targeted protein degradation (2019–present)

    doi: 10.1080/13543776.2024.2446232

    Figure Lengend Snippet: Folate caged PROTACs from BIDMC targeting BRD, MEK and AKT proteins respectively.

    Article Snippet: Work in 2019 by Arvinas disclosed a range of VHL-based PROTACs that degrade SMARCA2/4 proteins which included a range of different heterocycles ( ) [ ].

    Techniques: