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Brian M Lacey

Explore the profile of Brian M Lacey including associated specialties, affiliations and a list of published articles. Areas
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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.
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.
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...