Charles Eigenbrot
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Explore the profile of Charles Eigenbrot including associated specialties, affiliations and a list of published articles.
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106
Citations
4692
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Recent Articles
1.
Hanan E, Braun M, Heald R, MacLeod C, Chan C, Clausen S, et al.
J Med Chem
. 2022 Dec;
65(24):16589-16621.
PMID: 36455032
Small molecule inhibitors that target the phosphatidylinositol 3-kinase (PI3K) signaling pathway have received significant interest for the treatment of cancers. The class I isoform PI3Kα is most commonly associated with...
2.
Wei B, Robarge K, Labadie S, Chen J, Corson L, DiPasquale A, et al.
Bioorg Med Chem Lett
. 2022 Jan;
59:128576.
PMID: 35065235
Structure-based design was utilized to optimize 6,6-diaryl substituted dihydropyrone and hydroxylactam to obtain inhibitors of lactate dehydrogenase (LDH) with low nanomolar biochemical and single-digit micromolar cellular potencies. Surprisingly the replacement...
3.
Ultsch M, Holliday M, Gerhardy S, Moran P, Scales S, Gupta N, et al.
Commun Biol
. 2021 Jul;
4(1):916.
PMID: 34316015
Apolipoprotein L1 (ApoL1) is a circulating innate immunity protein protecting against trypanosome infection. However, two ApoL1 coding variants are associated with a highly increased risk of chronic kidney disease. Here...
4.
Huestis M, Durk M, Eigenbrot C, Gibbons P, Hunsaker T, La H, et al.
ACS Med Chem Lett
. 2021 May;
12(5):791-797.
PMID: 34055227
Structure-based optimization of a set of aryl urea RAF inhibitors has led to the identification of Type II pan-RAF inhibitor GNE-9815 (), which features a unique pyrido[2,3-]pyridazin-8(7)-one hinge-binding motif. With...
5.
Huestis M, Dela Cruz D, DiPasquale A, Durk M, Eigenbrot C, Gibbons P, et al.
J Med Chem
. 2021 Mar;
64(7):3940-3955.
PMID: 33780623
Optimization of a series of aryl urea RAF inhibitors led to the identification of type II pan-RAF inhibitor GNE-0749 (), which features a fluoroquinazolinone hinge-binding motif. By minimizing reliance on...
6.
Maun H, Vij R, Walters B, Morando A, Jackman J, Wu P, et al.
Nat Commun
. 2020 Dec;
11(1):6435.
PMID: 33353951
Human β-tryptase, a tetrameric trypsin-like serine protease, is an important mediator of allergic inflammatory responses in asthma. Antibodies generally inhibit proteases by blocking substrate access by binding to active sites...
7.
Crawford J, Lee W, Johnson A, Delatorre K, Chen J, Eigenbrot C, et al.
ACS Med Chem Lett
. 2020 Aug;
11(8):1588-1597.
PMID: 32832028
Bruton's tyrosine kinase (Btk) is thought to play a pathogenic role in chronic immune diseases such as rheumatoid arthritis and lupus. While covalent, irreversible Btk inhibitors are approved for treatment...
8.
Maun H, Jackman J, Choy D, Loyet K, Staton T, Jia G, et al.
Cell
. 2020 Jan;
180(2):406.
PMID: 31978350
No abstract available.
9.
Burdick D, Skelton N, Ultsch M, Beresini M, Eigenbrot C, Li W, et al.
ACS Chem Biol
. 2020 Jan;
15(2):425-436.
PMID: 31962046
Proprotein convertase subtilisin/kexin 9 (PCSK9) has become an important therapeutic target for lipid lowering, since it regulates low-density lipoprotein cholesterol (LDL-c) levels by binding to liver LDL receptors (LDLR) and...
10.
Maun H, Jackman J, Choy D, Loyet K, Staton T, Jia G, et al.
Cell
. 2019 Oct;
179(2):417-431.e19.
PMID: 31585081
Severe asthma patients with low type 2 inflammation derive less clinical benefit from therapies targeting type 2 cytokines and represent an unmet need. We show that mast cell tryptase is...