Výsledky vyhledávání

Akademický článek

Affinity and cooperativity modulate ternary complex formation to drive targeted protein degradation

Autor: Ryan P. Wurz, Huan Rui, Ken Dellamaggiore, Sudipa Ghimire-Rijal, Kaylee Choi, Kate Smither, Albert Amegadzie, Ning Chen, Xiaofen Li, Abhisek Banerjee, Qing Chen, Dane Mohl, Amit Vaish

Publikováno v: Nature Communications, Vol 14, Iss 1, Pp 1-16 (2023)

Abstract Targeted protein degradation via “hijacking” of the ubiquitin-proteasome system using proteolysis targeting chimeras (PROTACs) has evolved into a novel therapeutic modality. The design of PROTACs is challenging; multiple steps involved i

Externí odkaz: https://doaj.org/article/de7e722d28104330ab18533bf9830472

Zobrazit plný text záznamu

Data from Loss of NAPRT1 Expression by Tumor-Specific Promoter Methylation Provides a Novel Predictive Biomarker for NAMPT Inhibitors

Autor: Lisa D. Belmont, Hartmut Koeppen, Richard Bourgon, Thomas O'Brien, Robert L. Yauch, Xiaorong Liang, Bianca Liederer, Peter M. Haverty, Thinh Pham, Yang Xiao, Dane Mohl, Pan Du, Thomas Holcomb, Kimberly Walter, Kristi Elkins, David S. Shames

Purpose: We sought to identify predictive biomarkers for a novel nicotinamide phosphoribosyltransferase (NAMPT) inhibitor.Experimental Design: We use a NAMPT inhibitor, GNE-617, to evaluate nicotinic acid rescue status in a panel of more than 400 can

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4e84aa7961f32a2031d250e784a4c317
https://doi.org/10.1158/1078-0432.c.6520628.v1

Zobrazit plný text záznamu

Supplementary Figure 1 from Loss of NAPRT1 Expression by Tumor-Specific Promoter Methylation Provides a Novel Predictive Biomarker for NAMPT Inhibitors

PDF file 122K, A) Chemical structure of GNE-617, B) cellular NAD and ATP levels in H522 cells after exposure to 4nM GNE-617, C) correlation of NAPRT1 mRNA and protein (n=32, spearman r= 0.88, p,0.0001)

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3078920a930d4fcc697360aeedd937c0
https://doi.org/10.1158/1078-0432.22446035

Zobrazit plný text záznamu

Supplementary Methods and Tables from Loss of NAPRT1 Expression by Tumor-Specific Promoter Methylation Provides a Novel Predictive Biomarker for NAMPT Inhibitors

PDF file 141K, Supplementary methods for NAD quantification and the QMSP assay. Table S1 GNE-617 IC50 and mRNA Levels of NAMPT and NAPRT1, Table S2 Cell Lines Not Rescued with 10uM NA, Table S3 Cell Lines with Low NAPRT1 Expression

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2ead523cff3b9f9c55d3f8c544a360c9
https://doi.org/10.1158/1078-0432.22446032.v1

Zobrazit plný text záznamu

Profiling of diverse tumor types establishes the broad utility of VHL-based ProTaCs and triages candidate ubiquitin ligases

Autor: Xin, Luo, Ivonne, Archibeque, Ken, Dellamaggiore, Kate, Smither, Oliver, Homann, James Russell, Lipford, Dane, Mohl

Publikováno v: iScience. 25:103985

The success of small molecule therapeutics that promotes degradation of critical cancer targets has fueled an intense effort to mimic this activity with bispecific molecules called PROTACs (proteolysis targeting chimeras). The simultaneous binding of

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c1dbb0320a876e23b1de3b66460906b3
https://doi.org/10.1016/j.isci.2022.103985

Zobrazit plný text záznamu

A 'Click Chemistry Platform' for the Rapid Synthesis of Bispecific Molecules for Inducing Protein Degradation

Autor: Christine Sastri, Noelle Javier, Ryan Wurz, J. Russell Lipford, Hannah Dou, Mei-Chu Lo, Victor J. Cee, John McCarter, Ken Dellamaggiore, Dane Mohl

Publikováno v: Journal of Medicinal Chemistry. 61:453-461

Proteolysis targeting chimeras (PROTACs) are bispecific molecules containing a target protein binder and an ubiquitin ligase binder connected by a linker. By recruiting an ubiquitin ligase to a target protein, PROTACs promote ubiquitination and prote

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cecc44534d76887770e2aaa9542e5fc1
https://doi.org/10.1021/acs.jmedchem.6b01781

Zobrazit plný text záznamu

Harnessing the Power of Proteolysis for Targeted Protein Inactivation

Autor: Dane Mohl, Rati Verma, Raymond J. Deshaies

Publikováno v: Molecular cell. 77(3)

Two decades into the twenty-first century, a confluence of breakthrough technologies wielded at the molecular level is presenting biologists with unique opportunities to unravel the complexities of the cellular world. CRISPR/Cas9 allows gene knock-ou

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9e215c360f594a70cab6bda3274b27d3
https://pubmed.ncbi.nlm.nih.gov/32004468

Zobrazit plný text záznamu

Loss of NAPRT1 expression by tumor-specific promoter methylation provides a novel predictive biomarker for NAMPT inhibitors

Autor: Peter M. Haverty, David S. Shames, Robert L. Yauch, Dane Mohl, Thinh Pham, Richard Bourgon, Pan Du, Thomas Holcomb, Kimberly Walter, Thomas O'Brien, Bianca M. Liederer, Lisa D. Belmont, Xiaorong Liang, Hartmut Koeppen, Kristi Elkins, Yang Xiao

Publikováno v: Clinical cancer research : an official journal of the American Association for Cancer Research. 19(24)

Purpose: We sought to identify predictive biomarkers for a novel nicotinamide phosphoribosyltransferase (NAMPT) inhibitor. Experimental Design: We use a NAMPT inhibitor, GNE-617, to evaluate nicotinic acid rescue status in a panel of more than 400 ca

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6ca4a802142a020c310a9019da204466
https://pubmed.ncbi.nlm.nih.gov/24097869

Zobrazit plný text záznamu

Vyhledávací nástroje:

Upřesnit hledání