Juan I Luengo
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Explore the profile of Juan I Luengo including associated specialties, affiliations and a list of published articles.
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22
Citations
520
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Recent Articles
1.
Pappalardi M, Keenan K, Cockerill M, Kellner W, Stowell A, Sherk C, et al.
Nat Cancer
. 2021 Nov;
2(10):1002-1017.
PMID: 34790902
DNA methylation, a key epigenetic driver of transcriptional silencing, is universally dysregulated in cancer. Reversal of DNA methylation by hypomethylating agents, such as the cytidine analogs decitabine or azacytidine, has...
2.
Lin H, Luengo J
Bioorg Med Chem Lett
. 2020 Jul;
30(19):127442.
PMID: 32730944
Active or allosteric site arginines can form diverse interactions with ligands including different types of cation-π interactions, H-bond interactions and non-bond, non-canonical interactions. This provides many opportunities for creative structure-based...
3.
Lin H, Wang M, Zhang Y, Tong S, Leal R, Shetty R, et al.
ACS Med Chem Lett
. 2019 Jul;
10(7):1033-1038.
PMID: 31312404
Protein arginine methyltransferase 5 (PRMT5) is known to symmetrically dimethylate numerous cytosolic and nuclear proteins that are involved in a variety of cellular processes. Recent findings have revealed its potential...
4.
Lin H, Luengo J
Bioorg Med Chem Lett
. 2019 Apr;
29(11):1264-1269.
PMID: 30956011
Protein Arginine Methyltransferase 5 (PRMT5) is known to symmetrically dimethylate numerous cytosolic and nuclear proteins that are involved in a variety of cellular processes. Recent findings have revealed its potential...
5.
Chakravorty S, Chan J, Greenwood M, Popa-Burke I, Remlinger K, Pickett S, et al.
SLAS Discov
. 2018 Apr;
23(6):532-545.
PMID: 29699447
High-throughput screening (HTS) hits include compounds with undesirable properties. Many filters have been described to identify such hits. Notably, pan-assay interference compounds (PAINS) has been adopted by the community as...
6.
Lin H, Zeng J, Xie R, Schulz M, Tedesco R, Qu J, et al.
ACS Med Chem Lett
. 2016 Mar;
7(3):217-22.
PMID: 26985301
A novel series of potent and selective hexokinase 2 (HK2) inhibitors, 2,6-disubstituted glucosamines, has been identified based on HTS hits, exemplified by compound 1. Inhibitor-bound crystal structures revealed that the...
7.
Yu H, Moore M, Erhard K, Hardwicke M, Lin H, Luengo J, et al.
ACS Med Chem Lett
. 2014 Jun;
4(2):230-4.
PMID: 24900655
A series of novel [3a,4]dihydropyrazolo[1,5a]pyrimidines were identified, which were highly potent and selective inhibitors of PI3Kβ. The template afforded the opportunity to develop novel SAR for both the hinge-binding (R3)...
8.
Lin H, Schulz M, Xie R, Zeng J, Luengo J, Squire M, et al.
ACS Med Chem Lett
. 2014 Jun;
3(7):524-9.
PMID: 24900504
A novel thiazolopyrimidinone series of PI3K-beta selective inhibitors has been identified. This chemotype has provided an excellent tool compound, 18, that showed potent growth inhibition in the PTEN-deficient breast cancer...
9.
Knight S, Adams N, Burgess J, Chaudhari A, Darcy M, Donatelli C, et al.
ACS Med Chem Lett
. 2014 Jun;
1(1):39-43.
PMID: 24900173
Phosphoinositide 3-kinase α (PI3Kα) is a critical regulator of cell growth and transformation, and its signaling pathway is the most commonly mutated pathway in human cancers. The mammalian target of...
10.
Sanchez R, Erhard K, Hardwicke M, Lin H, McSurdy-Freed J, Plant R, et al.
Bioorg Med Chem Lett
. 2012 Apr;
22(9):3198-202.
PMID: 22475557
A series of 1,2,4-triazolo[1,5-a]pyrimidin-7(3H)-ones with excellent enzyme inhibition, improved isoform selectivity, and excellent inhibition of downstream phosphorylation of AKT has been identified. Several compounds in the series demonstrated potent (∼...