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David F Wiemer

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Recent Articles
1.
Ayub Ali M, Maalouf M, Feng D, Rashid M, Gehrke N, Chhonker Y, et al.
Bioorg Med Chem . 2025 Mar; 122:118140. PMID: 40043324
Geranylgeranyl diphosphate synthase (GGDPS) produces the 20-carbon isoprenoid species used in protein geranylgeranylation reactions. Inhibition of GGDPS has emerged as a novel means of disrupting the activity of geranylgeranylated proteins...
2.
Singh U, Pawge G, Kintigh P, Sarno J, Rani S, Hsiao C, et al.
Eur J Med Chem . 2025 Feb; 287:117345. PMID: 39919440
The most effective natural ligand for the butyrophilins is (E)-4-hydroxy-3-methyl-but-2-enyl diphosphate. However, due to its susceptibility to plasma hydrolysis and its high charge that limits passive diffusion across cell membranes,...
3.
Singh U, Pawge G, Rani S, Hsiao C, Wiemer D, Wiemer A
ACS Med Chem Lett . 2024 Oct; 15(10):1771-1777. PMID: 39411535
While ester-based phosphonate prodrugs excel at delivering payloads into cells, their instability in plasma is a hurdle for their advancement. Here, we synthesized new aryl/acyloxy prodrugs of a phosphonate BTN3A1...
4.
Gehrke N, Feng D, Ayub Ali M, Maalouf M, Holstein S, Wiemer D
Bioorg Med Chem Lett . 2024 Feb; 102:129659. PMID: 38373465
Depletion of cellular levels of geranylgeranyl diphosphate by inhibition of the enzyme geranylgeranyl diphosphate synthase (GGDPS) is a potential strategy for disruption of protein transport by limiting the geranylgeranylation of...
5.
Singh U, Pawge G, Rani S, Hsiao C, Wiemer A, Wiemer D
J Med Chem . 2023 Nov; 66(22):15309-15325. PMID: 37934915
Activation of Vγ9Vδ2 T cells with butyrophilin 3A1 (BTN3A1) agonists such as ()-4-hydroxy-3-methyl-but-2-enyl diphosphate (HMBPP) has the potential to boost the immune response. Because HMBPP is highly charged and metabolically...
6.
Harmon N, Gehrke N, Wiemer D
Tetrahedron Lett . 2023 Jul; 106. PMID: 37521200
Vinyl bisphosphonates can be readily prepared by condensation of an aromatic aldehyde with the tetraester of a methylenebisphosphonate, and reduction of the resulting olefin is an attractive strategy for the...
7.
Stockdale D, Beutler J, Wiemer D
Bioorg Med Chem Lett . 2022 Sep; 75:128980. PMID: 36096344
The stilbene moiety is commonly found in natural products and these compounds display an extraordinary range of biological activity. Efforts to derive useful drugs from stilbenes must address the potential...
8.
Lentini N, Huang X, Schladetsch M, Hsiao C, Wiemer D, Wiemer A
Bioorg Med Chem Lett . 2022 Apr; 66:128724. PMID: 35405283
Bis-amidate derivatives have been viewed as attractive phosphonate prodrug forms because of their straightforward synthesis, lack of phosphorus stereochemistry, plasma stability and nontoxic amino acid metabolites. However, the efficiency of...
9.
Harmon N, Poe M, Huang X, Singh R, Foust B, Hsiao C, et al.
ACS Med Chem Lett . 2022 Feb; 13(2):164-170. PMID: 35178171
Phosphoantigens (pAgs) are small organophosphorus compounds such as ()-4-hydroxy-3-methyl-but-2-enyl diphosphate (HMBPP) that trigger an immune response. These molecules bind to butyrophilin 3A1 (part of the HMBPP receptor) and activate Vγ9Vδ2...
10.
Schroeder C, Dey P, Beutler J, Wiemer D
J Org Chem . 2021 Oct; 86(23):16824-16833. PMID: 34714084
The natural schweinfurthins are stilbenes with significant antiproliferative activity and an uncertain mechanism of action. To obtain a fluorescent analogue with minimal deviation from the natural structure, a coumarin ring...