Výsledky vyhledávání - "David Cocozziello"

A Method for Determining the Kinetics of Small-Molecule-Induced Ubiquitination

Autor: Stewart L. Fisher, Marta Isasa, Stephen Archer, Heng Li, Mark E. Fitzgerald, Lydia Emerson, Christopher G. Nasveschuk, Linda Lee, Roman V. Agafonov, Richard W. Deibler, Jeffrey R Simard, Ryan E. Michael, Ellen F. Vieux, Brendon Ladd, David A. Proia, Gunther Kern, Eunice S. Park, Andrew J. K. Phillips, David Cocozziello

Publikováno v: SLAS Discovery. 26:547-559

Recent advances in targeted protein degradation have enabled chemical hijacking of the ubiquitin-proteasome system to treat disease. The catalytic rate of cereblon (CRBN)-dependent bifunctional degradation activating compounds (BiDAC), which recruit

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9b95d7f93321f5de660b39ea7553ea25
https://doi.org/10.1177/24725552211000673

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Abstract 3425: The discovery and characterization of CFT1946: A potent, selective, and orally bioavailable degrader of mutant BRAF for the treatment of BRAF-driven cancers

Publikováno v: Cancer Research. 83:3425-3425

The BRAF kinase plays a critical role in the MAPK signaling pathway and is mutated in ~8% of all human cancers including melanoma (~60%), thyroid (~60%), and lung adenocarcinoma (~10%). The most common mutation in BRAF is V600E (Class I), which is fo

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::4eb2b150c4dde824e5ce0d7e8249985a
https://doi.org/10.1158/1538-7445.am2023-3425

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Abstract ND09: The discovery and characterization of CFT8634: A potent and selective degrader of BRD9 for the treatment of SMARCB1-perturbed cancers

Publikováno v: Cancer Research. 82:ND09-ND09

Introduction: The chromatin factor BRD9 is a genetic dependency in some cancers, often referred to as SMARCB1-perturbed cancers. Two types of genetic alterations result in SMARCB1 perturbation: SS18-SSX gene fusion and SMARCB1 loss-of-function mutati

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::96b44ef5d9fa5dc56a4a294008bf6985
https://doi.org/10.1158/1538-7445.am2022-nd09

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Abstract 2158: Preclinical evaluation of CFT1946 as a selective degrader of mutant BRAF for the treatment of BRAF driven cancers

Publikováno v: Cancer Research. 82:2158-2158

The BRAF kinase is a critical node in the MAPK signaling pathway and is mutated in approximately 8% of human cancers including melanoma (~60%), thyroid (~60%), and lung adenocarcinoma (~10%). The most common mutation in BRAF is V600E (Class I), occur

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::f785dda79bcc9822c5d07c44e6bcdb69
https://doi.org/10.1158/1538-7445.am2022-2158

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Abstract ND13: The discovery and characterization of CFT7455: A potent and selective degrader of IKZF1/3 for the treatment of relapsed/refractory multiple myeloma

Publikováno v: Cancer Research. 82:ND13-ND13

Introduction: Ikaros family zinc finger protein 1 and 3 (IKZF1/3) are essential transcription factors (TF) for terminal differentiation of B and T cells. Depletion of IKZF1/3 inhibits the growth of multiple myeloma (MM) cells, confirming their depend

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::42186bfdcb13c3303d47d3055f7346ca
https://doi.org/10.1158/1538-7445.am2022-nd13

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High-throughput dynamic BH3 profiling may quickly and accurately predict effective therapies in solid tumors

Autor: Kimmie Ng, Alaba Sotayo, Patrick Bhola, Elizaveta Lavrova, Kelley E. McQueeney, Otari Chipashvili, Ewa Sicinska, Timothy Hagan, Jennifer L. Guerriero, Eman Ahmed, Andrew J. Aguirre, Jeremy Ryan, David Cocozziello, Emily Su, Jean J. Zhao, Anthony Letai, James M. Cleary, Marissa S. Pioso, Jing Ni

Publikováno v: Sci Signal

Despite decades of effort, the sensitivity of patient tumors to individual drugs is often not predictable on the basis of molecular markers alone. Therefore, unbiased, high-throughput approaches to match patient tumors to effective drugs, without req

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4ea82a99c0f34d2e58b6c27bb9705799
https://pubmed.ncbi.nlm.nih.gov/32546544

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Abstract LB007: CFT7455: A novel, IKZF1/3 degrader that demonstrates potent tumor regression in IMiD-resistant multiple myeloma (MM) xenograft models

Publikováno v: Cancer Research. 81:LB007-LB007

Introduction Ikaros family zinc finger protein 1 and 3 (IKZF1/3) are essential transcription factors (TF) for terminal differentiation of B and T cells. Depletion of IKZF1/3 in MM cells inhibits growth, confirming their dependency on IKZF1/3. IMiDs (

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::1aa2374fa57ec020d2e2ec7fb38e670b
https://doi.org/10.1158/1538-7445.am2021-lb007

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Abstract 1949: In vivo profiling of BET degraders establishes optimal pharmacological properties that showcase distinct biological differences from BET inhibitors

Autor: Marta Issa, Ellen F. Vieux, Roman V. Agafonov, Mark E. Fitzgerald, Eun Sun Park, Brendon Ladd, Ryan E. Michael, David A. Proia, Linda Lee, Christopher G. Nasveschuk, David Cocozziello, Jacob Feala

Publikováno v: Cancer Research. 80:1949-1949

Targeted protein degradation (TPD) with heterobifunctional small molecules is emerging as a promising new therapeutic modality in oncology. We sought to understand how TPD compares versus targeted protein inhibition. We used BRD4 as a surrogate targe

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::1dc5b98b7ee28bdfeaa052d90e8c706c
https://doi.org/10.1158/1538-7445.am2020-1949

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