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» Authors » Terrence R Burke Jr

Terrence R Burke Jr

Explore the profile of Terrence R Burke Jr including associated specialties, affiliations and a list of published articles. Areas
Snapshot
Articles 157
Citations 2530
Followers 0
Related Specialties
Biochemistry
Chemistry
Biology
Top 10 Co-Authors
Xue Zhi Zhao
Yves Pommier
Stephen H Hughes
Robert J Fisher
Steven J Smith
Christophe Marchand
Fa Liu
Karen M Worthy
Marc C Nicklaus
David Hymel
Published In
Bioorg Med Chem Lett
J Med Chem
Bioorg Med Chem
Proc Natl Acad Sci U S A
J Biol Chem
Affiliations
Soon will be listed here.
Recent Articles
1.
Application of a bivalent "click" approach to target tyrosyl-DNA phosphodiesterase 1 (TDP1)
Zhao X, Wang W, Mahmud M, Agama K, Pommier Y, Burke Jr T
RSC Med Chem . 2025 Feb; PMID: 39990162
Although inhibiting the DNA repair enzyme tyrosyl-DNA phosphodiesterase 1 (TDP1) synergizes with topoisomerase type I (TOP1) inhibitors in anticancer therapy, development of TDP1 inhibitors has been highly challenging. This may...
2.
Comparative Analyses of Antiviral Potencies of Second-Generation Integrase Strand Transfer Inhibitors (INSTIs) and the Developmental Compound 4d Against a Panel of Integrase Quadruple Mutants
Smith S, Zhao X, Hughes S, Burke Jr T
Viruses . 2025 Jan; 17(1). PMID: 39861910
Second-generation integrase strand transfer inhibitors (INSTIs) are strongly recommended for people living with HIV-1 (PLWH). The emergence of resistance to second-generation INSTIs has been infrequent and has not yet been...
3.
Targeted sulfur(VI) fluoride exchange-mediated covalent modification of a tyrosine residue in the catalytic pocket of tyrosyl-DNA phosphodiesterase 1
Zhao X, Barakat I, Lountos G, Wang W, Agama K, Mahmud M, et al.
Commun Chem . 2024 Sep; 7(1):208. PMID: 39284936
Developing effective inhibitors of the DNA repair enzyme tyrosyl-DNA phosphodiesterase 1 (TDP1) has been challenging because of the enzyme shallow catalytic pocket and non-specific substrate binding interactions. Recently, we discovered...
4.
Affinity enhancement of polo-like kinase 1 polo box domain-binding ligands by a bivalent approach using a covalent kinase-binding component
Tsuji K, Tamamura H, Burke Jr T
RSC Chem Biol . 2024 Aug; 5(8):721-728. PMID: 39092437
The polo-like kinase 1 (Plk1) is an important cell cycle regulator that is recognized as a target molecule for development of anti-cancer agents. Plk1 consists of a catalytic kinase domain...
5.
Application of a Fluorescence Recovery-Based Polo-Like Kinase 1 Binding Assay to Polo-Like Kinase 2 and Polo-Like Kinase 3
Tsuji K, Tamamura H, Burke Jr T
Biol Pharm Bull . 2024 Jul; 47(7):1282-1287. PMID: 38987177
Assay systems for evaluating compound protein-binding affinities are essential for developing agonists and/or antagonists. Targeting individual members of a protein family can be extremely important and for this reason it...
6.
Enhancing precision in colorectal cancer surgery: development of an LGR5-targeting RSPO1 peptide mimetic as a contrast agent for intraoperative fluorescence molecular imaging
Parasido E, Ribeiro P, Chingle R, Rohwetter T, Gupta N, Avetian G, et al.
Cell Cycle . 2024 Jul; :1-12. PMID: 38984667
Colorectal cancer (CRC) is the third most common cancer worldwide. In the United States alone, CRC was responsible for approximately 52,550 deaths in 2023, with an estimated 153,020 new cases....
7.
-Substituted Bicyclic Carbamoyl Pyridones: Integrase Strand Transfer Inhibitors that Potently Inhibit Drug-Resistant HIV-1 Integrase Mutants
Mahajan P, Smith S, Li M, Craigie R, Hughes S, Zhao X, et al.
ACS Infect Dis . 2024 Feb; 10(3):917-927. PMID: 38346249
HIV-1 integrase (IN) is an important molecular target for the development of anti-AIDS drugs. A recently FDA-approved second-generation integrase strand transfer inhibitor (INSTI) cabotegravir (CAB, 2021) is being marketed for...
8.
Mechanisms of HIV-1 integrase resistance to dolutegravir and potent inhibition of drug-resistant variants
Li M, Oliveira Passos D, Shan Z, Smith S, Sun Q, Biswas A, et al.
Sci Adv . 2023 Jul; 9(29):eadg5953. PMID: 37478179
HIV-1 infection depends on the integration of viral DNA into host chromatin. Integration is mediated by the viral enzyme integrase and is blocked by integrase strand transfer inhibitors (INSTIs), first-line...
9.
Synthetic Approaches to a Key Pyridone-carboxylic Acid Precursor Common to the HIV-1 Integrase Strand Transfer Inhibitors Dolutegravir, Bictegravir, and Cabotegravir
Mahajan P, Burke Jr T
Org Process Res Dev . 2023 May; 27(5):847-853. PMID: 37229216
Dolutegravir (DTG), Bictegravir (BIC), and Cabotegravir (CAB) are the second-generation integrase strand transfer inhibitors (INSTIs) that have been FDA-approved for the treatment of HIV-1 infection. Preparation of these INSTIs utilizes...
10.
Identification of multidentate tyrosyl-DNA phosphodiesterase 1 (TDP1) inhibitors that simultaneously access the DNA, protein and catalytic-binding sites by oxime diversification
Zhao X, Wang W, Lountos G, Kiselev E, Tropea J, Needle D, et al.
RSC Chem Biol . 2023 May; 4(5):334-343. PMID: 37181631
Tyrosyl-DNA phosphodiesterase 1 (TDP1) is a member of the phospholipase D family that can downregulate the anticancer effects of the type I topoisomerase (TOP1) inhibitors by hydrolyzing the 3'-phosphodiester bond...