Thomas Kodadek
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Explore the profile of Thomas Kodadek including associated specialties, affiliations and a list of published articles.
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169
Citations
3056
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Recent Articles
1.
Balzarini M, Tong J, Gui W, Jayalath I, Schell B, Kodadek T
ACS Chem Biol
. 2024 Oct;
19(11):2323-2335.
PMID: 39439063
Targeted protein degradation (TPD) is a promising strategy for drug development. Most degraders function by forcing the association of the target protein (TP) with an E3 Ubiquitin (Ub) ligase, which,...
2.
Abboud S, Kodadek T
JACS Au
. 2024 Aug;
4(8):3018-3027.
PMID: 39211620
This study introduces a novel solid-phase macrocyclization method generating 2-pyridone rings. This method relies on the intramolecular condensation between secondary and tertiary dimethoxy-propionic amide units. This selective reaction leads to...
3.
Li B, Parker J, Tong J, Kodadek T
J Am Chem Soc
. 2024 May;
146(21):14633-14644.
PMID: 38752889
Macrocyclic peptides (MPs) are a class of compounds that have been shown to be particularly well suited for engaging difficult protein targets. However, their utility is limited by their generally...
4.
Castanha P, McEnaney P, Park Y, Bouwer A, Chaves E, Lins R, et al.
Proc Natl Acad Sci U S A
. 2024 May;
121(21):e2312755121.
PMID: 38743628
Antigenic similarities between Zika virus (ZIKV) and other flaviviruses pose challenges to the development of virus-specific diagnostic tools and effective vaccines. Starting with a DNA-encoded one-bead-one-compound combinatorial library of 508,032...
5.
Kodadek T
Angew Chem Int Ed Engl
. 2023 Dec;
63(11):e202316726.
PMID: 38064411
Many of the highest priority targets in a wide range of disease states are difficult-to-drug proteins. The development of reversible small molecule inhibitors for the active sites of these proteins...
6.
Abboud S, Kodadek T
Chemistry
. 2023 Nov;
30(2):e202302937.
PMID: 37939246
This study presents an efficient method for on-resin dimer generation through self-condensation of 3,3-dimethoxypropionic acid-modified molecules, resulting in 2-pyridones. The approach demonstrated remarkable versatility by producing homodimers of peptides, peptoids,...
7.
Gui W, Kodadek T
Chembiochem
. 2023 Jul;
24(18):e202300392.
PMID: 37449865
Many proteins exist as oligomers (homodimers, homotrimers, etc.). A proven strategy for the development of high affinity ligands for such targets is to link together two modest affinity ligands that...
8.
Gui W, Giardina S, Balzarini M, Barany F, Kodadek T
ACS Chem Biol
. 2023 Jul;
18(7):1582-1593.
PMID: 37422908
PROteolysis TArgeting Chimeras (PROTACs) are of significant current interest for the development of probe molecules and drug leads. However, they suffer from certain limitations. PROTACs are rule-breaking molecules with sub-optimal...
9.
Gui W, Kodadek T
Chembiochem
. 2022 Jul;
23(18):e202200275.
PMID: 35802347
Proteolysis targeting chimeras are of keen interest as probe molecules and drug leads. Their activity is highly sensitive to the length and nature of the linker connecting the E3 Ubiquitin...
10.
Koesema E, Roy A, Paciaroni N, Coito C, Tokmina-Roszyk M, Kodadek T
Angew Chem Int Ed Engl
. 2022 Feb;
61(18):e202116999.
PMID: 35192245
There is considerable interest in the development of libraries of non-peptidic macrocycles as a source of ligands for difficult targets. We report here the solid-phase synthesis of a DNA-encoded library...