Brian L Hodous
Overview
Explore the profile of Brian L Hodous including associated specialties, affiliations and a list of published articles.
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17
Citations
318
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Recent Articles
1.
Davis A, Brooijmans N, Brubaker J, Stevison F, LaBranche T, Albayya F, et al.
Sci Transl Med
. 2024 May;
16(749):eabp8334.
PMID: 38809966
Fibrodysplasia ossificans progressiva (FOP) is a rare genetic disease driven by gain-of-function variants in activin receptor-like kinase 2 (ALK2), the most common variant being ALK2. In FOP, ALK2 variants display...
2.
Caldwell R, Qiu H, Askew B, Bender A, Brugger N, Camps M, et al.
J Med Chem
. 2019 Aug;
62(17):7643-7655.
PMID: 31368705
Bruton's tyrosine kinase (BTK) inhibitors such as ibrutinib hold a prominent role in the treatment of B cell malignancies. However, further refinement is needed to this class of agents, particularly...
3.
Gardino A, Evans E, Kim J, Brooijmans N, Hodous B, Wolf B, et al.
Mol Cell Oncol
. 2018 Sep;
5(3):e1435183.
PMID: 30250891
Cancer genomics and mechanistic studies have revealed that heterogeneous mutations within a single kinase can result in a variety of activation mechanisms. The challenge has been to match these insights...
4.
Evans E, Gardino A, Kim J, Hodous B, Shutes A, Davis A, et al.
Sci Transl Med
. 2017 Nov;
9(414).
PMID: 29093181
Targeting oncogenic kinase drivers with small-molecule inhibitors can have marked therapeutic benefit, especially when administered to an appropriate genomically defined patient population. Cancer genomics and mechanistic studies have revealed that...
5.
Geuns-Meyer S, Cee V, Deak H, Du B, Hodous B, Nguyen H, et al.
J Med Chem
. 2015 May;
58(13):5189-207.
PMID: 25970324
Efforts to improve upon the physical properties and metabolic stability of Aurora kinase inhibitor 14a revealed that potency against multidrug-resistant cell lines was compromised by increased polarity. Despite its high...
6.
Nguyen H, Cee V, Deak H, Du B, Faber K, Gunaydin H, et al.
J Org Chem
. 2012 Mar;
77(8):3887-906.
PMID: 22458369
Herein we describe a general three-step synthesis of 4-substituted chlorophthalazines in good overall yields. In the key step, N,N-dimethylaminophthalimide (8a) directs the selective monoaddition of alkyl, aryl, and heteroaryl organometallic...
7.
Payton M, Bush T, Chung G, Ziegler B, Eden P, McElroy P, et al.
Cancer Res
. 2010 Oct;
70(23):9846-54.
PMID: 20935223
In mammalian cells, the aurora kinases (aurora-A, -B, and -C) play essential roles in regulating cell division. The expression of aurora-A and -B is elevated in a variety of human...
8.
Cee V, Schenkel L, Hodous B, Deak H, Nguyen H, Olivieri P, et al.
J Med Chem
. 2010 Aug;
53(17):6368-77.
PMID: 20684549
The discovery of aurora kinases as essential regulators of cell division has led to intense interest in identifying small molecule aurora kinase inhibitors for the potential treatment of cancer. A...
9.
Cee V, Cheng A, Romero K, Bellon S, Mohr C, Whittington D, et al.
Bioorg Med Chem Lett
. 2008 Dec;
19(2):424-7.
PMID: 19062275
Selective small molecule inhibitors of Tie-2 kinase are important tools for the validation of Tie-2 signaling in pathological angiogenesis. Reported herein is the optimization of a nonselective scaffold into a...
10.
Deak H, Newcomb J, Nunes J, Boucher C, Cheng A, DiMauro E, et al.
Bioorg Med Chem Lett
. 2007 Dec;
18(3):1172-6.
PMID: 18083554
N-3-(Phenylcarbamoyl)arylpyrimidine-5-carboxamides are a novel class of selective Lck inhibitors. This series of compounds derives its selectivity from a hydrogen bond with the gatekeeper Thr316 of the enzyme. X-ray co-crystal structural...