Michael Siu
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Explore the profile of Michael Siu including associated specialties, affiliations and a list of published articles.
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31
Citations
551
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Recent Articles
1.
Tellis J, Wei B, Siu M, An L, Chan G, Chen Y, et al.
ACS Med Chem Lett
. 2024 Sep;
15(9):1606-1614.
PMID: 39291002
Hematopoietic progenitor kinase 1 (HPK1) serves a key immunosuppressive role as a negative regulator of T-cell receptor (TCR) signaling. HPK1 loss-of-function is associated with augmentation of immune function and has...
2.
Hu D, Patel S, Chen H, Wang S, Staben S, Dimitrova Y, et al.
J Med Chem
. 2021 Nov;
65(17):11500-11512.
PMID: 34779204
VPS34 is a class III phosphoinositide 3-kinase involved in endosomal trafficking and autophagosome formation. Inhibitors of VPS34 were believed to have value as anticancer agents, but genetic and pharmacological data...
3.
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...
4.
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...
5.
Ladi E, Everett C, Stivala C, Daniels B, Durk M, Harris S, et al.
J Med Chem
. 2019 Jul;
62(15):7032-7041.
PMID: 31283222
The pan-proteasome inhibitor bortezomib demonstrated clinical efficacy in off-label trials of Systemic Lupus Erythematosus. One potential mechanism of this clinical benefit is from the depletion of pathogenic immune cells (plasmablasts...
6.
Zak M, Hanan E, Lupardus P, Brown D, Robinson C, Siu M, et al.
Bioorg Med Chem Lett
. 2019 Apr;
29(12):1522-1531.
PMID: 30981576
Disruption of interleukin-13 (IL-13) signaling with large molecule antibody therapies has shown promise in diseases of allergic inflammation. Given that IL-13 recruits several members of the Janus Kinase family (JAK1,...
7.
Weissman S, Siu M, Ferm S, Hassan A
Cureus
. 2019 Jan;
10(11):e3578.
PMID: 30656082
Ranitidine is a widely used over-the-counter antacid medication, and is generally very well tolerated. To our knowledge, anaphylaxis secondary to ranitidine is exceedingly rare, and has only been reported in...
8.
Siu M, Sengupta Ghosh A, Lewcock J
J Med Chem
. 2018 Jun;
61(18):8078-8087.
PMID: 29863360
Dual leucine zipper kinase (DLK, MAP3K12) is an essential driver of the neuronal stress response that regulates neurodegeneration in models of acute neuronal injury and chronic neurodegenerative diseases such as...
9.
Patel S, Meilandt W, Erickson R, Chen J, Deshmukh G, Estrada A, et al.
J Med Chem
. 2017 Sep;
60(19):8083-8102.
PMID: 28929759
Significant data exists to suggest that dual leucine zipper kinase (DLK, MAP3K12) is a conserved regulator of neuronal degeneration following neuronal injury and in chronic neurodegenerative disease. Consequently, there is...
10.
Le Pichon C, Meilandt W, Dominguez S, Solanoy H, Lin H, Ngu H, et al.
Sci Transl Med
. 2017 Aug;
9(403).
PMID: 28814543
Hallmarks of chronic neurodegenerative disease include progressive synaptic loss and neuronal cell death, yet the cellular pathways that underlie these processes remain largely undefined. We provide evidence that dual leucine...