BioCentury | Oct 23, 2020
Product Development

What’s next for targeted protein degradation

...compounds that recruit the ligases RNF114, RNF4 and KEAP1.Vividion...
...zinc finger 1 IRAK4 – Interleukin-1 receptor-associated kinase 4 KEAP1...
BioCentury | Mar 14, 2020
Translation in Brief

A peptide fusion blocker for multiple coronaviruses, the cryo-EM structure of SARS-CoV-2 main protease, plus Locus, Excision and Harvard-Dana-Farber

...Described in Nature , they identified in a proof-of-concept experiment two compounds that displaced a KEAP1-binding...
...and 2.7 μM. Targets 3CLpro (NSP5; Mpro) - 3C-like proteinase Cas3 - CRISPR-associated helicase Cas3 KEAP1...
BioCentury | Nov 27, 2017
Distillery Therapeutics

Cancer

...KRAS-mutant lung cancers that also harbor KEAP1 mutations. In a mouse model of KRAS- and KEAP1-mutant...
...inhibitor CB-839 decreased tumor burden compared with vehicle, whereas in a mouse model of KRAS-mutant, KEAP1...
...of lung cancer harboring KRAS and KEAP1 mutations, but not in PDX models of KRAS-mutant, KEAP1...
BioCentury | Mar 29, 2017
Distillery Techniques

Disease models

...TECHNOLOGY: Transgenics and knockouts Double KEAP1 / NFE2L2 -knockout mice could be used to screen therapies...
...could be used to screen therapies for nephrogenic diabetes insipidus. Mice with systemic knockout of KEAP1...
...diabetes insipidus. Next steps could include using the model to screen for therapies. DESCRIPTION: Double kelch-like ECH-associated protein 1 (KEAP1)/nuclear...
BioCentury | Mar 6, 2017
Clinical News

Researchers identify KEAP1 as AD target

...manuscript published in PLoS Genetics , U.K. researchers identified Kelch-like ECH associated protein 1 ( KEAP1...
...Additionally, flies with reduced KEAP1 expression had reduced Aβ42 levels. The authors said that reducing KEAP1...
...KEAP1-NRF2 interaction may be a more effective strategy than targeting other upstream regulators of NRF2. Becky Simon Kelch-like ECH-associated protein 1 (KEAP1) Nuclear...
BioCentury | Oct 8, 2015
Distillery Therapeutics

Therapeutics: Kelch-like ECH-associated protein 1 (KEAP1); nuclear factor (erythroid-derived 2)-like 2 (NFE2L2; NRF2)

...Hematology INDICATION: Sickle cell disease Mouse studies suggest inhibiting KEAP1 or activating NFE2L2 could help treat...
...NFE2L2 could help treat sickle cell disease. In a mouse model of sickle cell disease, KEAP1...
...lung and decreased disease-associated liver necrosis and lung infiltration by inflammatory cells compared with normal KEAP1...
BioCentury | Sep 24, 2015
Distillery Therapeutics

Therapeutics: Kelch-like ECH-associated protein 1 (KEAP1); nuclear factor (erythroid-derived 2)-like 2 (NFE2L2; NRF2)

...inflammation. Disassociation of the KEAP1-NFE2L2 complex activates NFE2L2-mediated antioxidant responses. Chemical synthesis and testing in KEAP1-NFE2L2...
...Next steps could include testing the compound in mouse models of arthritis and lupus. TARGET/MARKER/PATHWAY: Kelch-like ECH-associated protein 1 (KEAP1)...
BioCentury | Oct 28, 2013
Emerging Company Profile

Rescue Therapeutics: Xenobiotic attack

...NRF2 is responsible for triggering antioxidant and anti-inflammatory effects. Rescue believes RTI-79 dissociates NRF2 from Kelch-like ECH-associated protein 1 (KEAP1)...
...which, when bound to NRF2, keeps it in an active state. Once disassociated from KEAP1...
BioCentury | Oct 29, 2012
Product Development

Reata, AIM, backfire

...and other AIMs might have unacceptable toxicities. AIMs target highly reactive cysteine residues in the Kelch-like ECH-associated protein 1 (KEAP1)...
...2 ( NFE2L2 ; NRF2 ) and keeps it in an active state. By modifying KEAP1...
BioCentury | Dec 19, 2011
Strategy

Abbott takes AIM

...the KEAP1 protein, which binds NRF2 and keeps it in an inactive state. By modifying KEAP1...
...KEAP1. That makes it possible to use low doses of bardoxolone that react only with KEAP1...
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