Brent A Appleton
Overview
Explore the profile of Brent A Appleton including associated specialties, affiliations and a list of published articles.
Author names and details appear as published. Due to indexing inconsistencies, multiple individuals may share a name, and a single author may have variations. MedLuna displays this data as publicly available, without modification or verification
Snapshot
Snapshot
Articles
28
Citations
1390
Followers
0
Related Specialties
Related Specialties
Top 10 Co-Authors
Top 10 Co-Authors
Published In
Published In
Affiliations
Affiliations
Soon will be listed here.
Recent Articles
1.
Goodwin J, Walkup 4th W, Hooper K, Li T, Kishi-Itakura C, Ng A, et al.
Sci Adv
. 2021 Oct;
7(40):eabj2485.
PMID: 34597140
Adaptive changes in lysosomal capacity are driven by the transcription factors TFEB and TFE3 in response to increased autophagic flux and endolysosomal stress, yet the molecular details of their activation...
2.
Ramurthy S, Taft B, Aversa R, Barsanti P, Burger M, Lou Y, et al.
J Med Chem
. 2019 May;
63(5):2013-2027.
PMID: 31059256
Direct pharmacological inhibition of RAS has remained elusive, and efforts to target CRAF have been challenging due to the complex nature of RAF signaling, downstream of activated RAS, and the...
3.
Jain R, Mathur M, Lan J, Costales A, Atallah G, Ramurthy S, et al.
Bioorg Med Chem Lett
. 2018 Sep;
28(19):3197-3201.
PMID: 30170943
Utilizing the already described 3,4-bi-aryl pyridine series as a starting point, incorporation of a second ring system with a hydrogen bond donor and additional hydrophobic contacts yielded the azaindole series...
4.
Skepper C, Moreau R, Appleton B, Benton B, Drumm 3rd J, Feng B, et al.
J Med Chem
. 2018 Mar;
61(8):3325-3349.
PMID: 29551072
In the preceding manuscript [ Moreau et al. 2018 , 10.1021/acs.jmedchem.7b01691 ] we described a successful fragment-based lead discovery (FBLD) strategy for discovery of bacterial phosphopantetheine adenylyltransferase inhibitors (PPAT, CoaD)....
5.
Moreau R, Skepper C, Appleton B, Blechschmidt A, Balibar C, Benton B, et al.
J Med Chem
. 2018 Mar;
61(8):3309-3324.
PMID: 29498517
The discovery and development of new antibiotics capable of curing infections due to multidrug-resistant and pandrug-resistant Gram-negative bacteria are a major challenge with fundamental importance to our global healthcare system....
6.
Smith A, Ni Z, Poon D, Huang Z, Chen Z, Zhang Q, et al.
Bioorg Med Chem Lett
. 2017 Nov;
27(23):5221-5224.
PMID: 29107542
A series of imidazo[1,2-a]pyridin-6-yl-benzamide analogs was designed as inhibitors of B-RAF. Medicinal chemistry techniques were employed to explore the SAR for this series and improve selectivity versus P38 and VEGFR2.
7.
Nishiguchi G, Rico A, Tanner H, Aversa R, Taft B, Subramanian S, et al.
J Med Chem
. 2017 May;
60(12):4869-4881.
PMID: 28557458
RAS oncogenes have been implicated in >30% of human cancers, all representing high unmet medical need. The exquisite dependency on CRAF kinase in KRAS mutant tumors has been established in...
8.
Williams T, Subramanian S, Verhagen J, McBride C, Costales A, Sung L, et al.
ACS Med Chem Lett
. 2015 Sep;
6(9):961-5.
PMID: 26396681
Abrogation of errant signaling along the MAPK pathway through the inhibition of B-RAF kinase is a validated approach for the treatment of pathway-dependent cancers. We report the development of imidazo-benzimidazoles...
9.
Jain R, Mathur M, Lan J, Costales A, Atallah G, Ramurthy S, et al.
J Med Chem
. 2015 Aug;
58(17):6766-83.
PMID: 26270416
While the p90 ribosomal S6 kinase (RSK) family has been implicated in multiple tumor cell functions, the full understanding of this kinase family has been restricted by the lack of...
10.
Ernst A, Appleton B, Ivarsson Y, Zhang Y, Gfeller D, Wiesmann C, et al.
J Mol Biol
. 2014 Aug;
426(21):3509-19.
PMID: 25158098
PDZ (PSD-95/Discs-large/ZO1) domains are interaction modules that typically bind to specific C-terminal sequences of partner proteins and assemble signaling complexes in multicellular organisms. We have analyzed the existing database of...