Brian M Lacey
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Explore the profile of Brian M Lacey including associated specialties, affiliations and a list of published articles.
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Articles
18
Citations
572
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Recent Articles
1.
Chang W, Altman M, Lesburg C, Perera S, Piesvaux J, Schroeder G, et al.
J Med Chem
. 2022 Mar;
65(7):5675-5689.
PMID: 35332774
Stereochemically and structurally complex cyclic dinucleotide-based stimulator of interferon genes (STING) agonists were designed and synthesized to access a previously unexplored chemical space. The assessment of biochemical affinity and cellular...
2.
Vara B, Levi S, Achab A, Candito D, Fradera X, Lesburg C, et al.
ACS Med Chem Lett
. 2021 Apr;
12(4):653-661.
PMID: 33859804
Hematopoietic progenitor kinase 1 (HPK1), a serine/threonine kinase, is a negative immune regulator of T cell receptor (TCR) and B cell signaling that is primarily expressed in hematopoietic cells. Accordingly,...
3.
Quiroz R, Reutershan M, Schneider S, Sloman D, Lacey B, Swalm B, et al.
J Med Chem
. 2021 Mar;
64(7):3911-3939.
PMID: 33755451
Protein arginine methyltransferase 5 (PRMT5) is a type II arginine methyltransferase that catalyzes the post-translational symmetric dimethylation of protein substrates. PRMT5 plays a critical role in regulating biological processes including...
4.
Yu E, Methot J, Fradera X, Lesburg C, Lacey B, Siliphaivanh P, et al.
ACS Med Chem Lett
. 2021 Mar;
12(3):459-466.
PMID: 33738073
Hematopoietic progenitor kinase (HPK1), a negative regulator of TCR-mediated T-cell activation, has been recognized as a novel antitumor immunotherapy target. Structural optimization of kinase inhibitor through a systematic two-dimensional diversity...
5.
Pharmacological inhibition of hematopoietic progenitor kinase 1 positively regulates T-cell function
Wang Y, Zhang K, Georgiev P, Wells S, Xu H, Lacey B, et al.
PLoS One
. 2020 Dec;
15(12):e0243145.
PMID: 33270695
Hematopoietic progenitor kinase 1 (HPK1), a hematopoietic cell-specific Ste20-related serine/threonine kinase, is a negative regulator of signal transduction in immune cells, including T cells, B cells, and dendritic cells (DCs)....
6.
Palte R, Schneider S, Altman M, Hayes R, Kawamura S, Lacey B, et al.
ACS Med Chem Lett
. 2020 Sep;
11(9):1688-1693.
PMID: 32944135
Protein arginine methyltransferase 5 (PRMT5) belongs to a family of enzymes that regulate the posttranslational modification of histones and other proteins via methylation of arginine. Methylation of histones is linked...
7.
Development of High-Throughput Assays for Evaluation of Hematopoietic Progenitor Kinase 1 Inhibitors
Lacey B, Xu Z, Chai X, Laskey J, Fradera X, Mittal P, et al.
SLAS Discov
. 2020 Aug;
26(1):88-99.
PMID: 32844715
Hematopoietic progenitor kinase 1 (HPK1), also referred to as mitogen-activated protein kinase kinase kinase kinase 1 (MAP4K1), is a serine/threonine kinase that negatively regulates T-cell signaling by phosphorylating Ser376 of...
8.
Pan B, Perera S, Piesvaux J, Presland J, Schroeder G, Cumming J, et al.
Science
. 2020 Aug;
369(6506).
PMID: 32820094
Pharmacological activation of the STING (stimulator of interferon genes)-controlled innate immune pathway is a promising therapeutic strategy for cancer. Here we report the identification of MSA-2, an orally available non-nucleotide...
9.
Brown Z, Mapelli C, Farasat I, Shoultz A, Johnson S, Orvieto F, et al.
J Org Chem
. 2019 Oct;
85(3):1466-1475.
PMID: 31660743
The Myc transcription factor represents an "undruggable" target of high biological interest due to its central role in various cancers. An abbreviated form of the c-Myc protein, called Omomyc, consists...
10.
Siu T, Altman M, Baltus G, Childers M, Ellis J, Gunaydin H, et al.
ACS Med Chem Lett
. 2019 Jan;
10(1):92-97.
PMID: 30655953
Drugging large protein pockets is a challenge due to the need for higher molecular weight ligands, which generally possess undesirable physicochemical properties. In this communication, we highlight a strategy leveraging...