Robert J Kerns
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Explore the profile of Robert J Kerns including associated specialties, affiliations and a list of published articles.
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55
Citations
1406
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Recent Articles
1.
Yin T, Van Vranken J, Srivastava D, Mittal A, Buscaglia P, Moore A, et al.
Cell Chem Biol
. 2023 Jul;
30(8):933-942.e6.
PMID: 37453421
Insulin resistance (IR) is the root cause of type II diabetes, yet no safe treatment is available to address it. Using a high throughput compatible assay that measures real-time translocation...
2.
Carter H, Wildman B, Schwanz H, Kerns R, Aldred K
Int J Mol Sci
. 2023 Feb;
24(3).
PMID: 36769202
Fluoroquinolones are an important class of antibacterials, and rising levels of resistance threaten their clinical efficacy. Gaining a more full understanding of their mechanism of action against their target enzymes-the...
3.
Gruenwald H, Kerns R
ACS Omega
. 2023 Jan;
7(51):48332-48339.
PMID: 36591157
Triphenylphosphonium (TPP) conjugates are effective in targeting drugs and probes to the mitochondria due to their lipophilic character that allows them to readily cross membranes and their large cationic radius...
4.
Chheda P, Nieto N, Kaur S, Beck J, Beck J, Honzatko R, et al.
Eur J Med Chem
. 2022 Oct;
243:114751.
PMID: 36191407
Malaria is caused by the parasite Plasmodium falciparum, which contains an essential non-photosynthetic plastid called the apicoplast. A single DNA polymerase, apPOL, is targeted to the apicoplast, where it replicates...
5.
Fink B, Yu L, Coppey L, Obrosov A, Shevalye H, Kerns R, et al.
Pharmacol Res Perspect
. 2021 Feb;
9(1):e00701.
PMID: 33547885
Previous work by ourselves and others showed that mitoquinone (mitoQ) reduced oxidative damage and prevented hepatic fat accumulation in mice made obese with high-fat (HF) feeding. Here we extended these...
6.
Kulkarni C, Fink B, Gibbs B, Chheda P, Wu M, Sivitz W, et al.
J Med Chem
. 2021 Jan;
64(1):662-676.
PMID: 33395531
Mitochondrial dysfunction is an underlying pathology in numerous diseases. Delivery of diagnostic and therapeutic cargo directly into mitochondria is a powerful approach to study and treat these diseases. The triphenylphosphonium...
7.
Aguirre A, Chheda P, Lentz S, Held H, Groves N, Hiasa H, et al.
Bioorg Med Chem
. 2020 Apr;
28(10):115439.
PMID: 32234278
Fluoroquinolones are a class of antibacterial agents used clinically to treat a wide array of bacterial infections and target bacterial type-II topoisomerases (DNA gyrase and topoisomerase IV). Fluoroquinolones, however potent,...
8.
Delgado J, Lentz S, Kulkarni C, Chheda P, Held H, Hiasa H, et al.
Eur J Med Chem
. 2019 Apr;
172:109-130.
PMID: 30959322
Fluoroquinolones substituted with N-1 biphenyl and napthyl groups were discovered to act as catalytically inhibitors of human topoisomerases I and II, and to possess anti-proliferative activity in vivo. Structural requirements...
9.
Lentz S, Chheda P, Oppegard L, Towle T, Kerns R, Hiasa H
Biochimie
. 2019 Feb;
160:24-27.
PMID: 30763638
A Mg-water bridge between the C-3, C-4 diketo moiety of fluoroquinolones and the conserved amino acid residues in the GyrA/ParC subunit is critical for the binding of a fluoroquinolone to...
10.
Oppegard L, Delgado J, Kulkarni C, Towle T, Hart D, Williams B, et al.
Invest New Drugs
. 2018 Sep;
37(2):378-383.
PMID: 30198058
Fluoroquinolone-class agents selectively target the bacterial type IIA topoisomerases DNA gyrase and topoisomerase IV, with a few exceptions that target eukaryotic type IIA topoisomerases. Fluoroquinolones bind and stabilize type IIA...