Jeffrey K Kerns
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Explore the profile of Jeffrey K Kerns including associated specialties, affiliations and a list of published articles.
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Articles
16
Citations
365
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Recent Articles
1.
Norton D, Bonnette W, Callahan J, Carr M, Griffiths-Jones C, Heightman T, et al.
J Med Chem
. 2021 Oct;
64(21):15949-15972.
PMID: 34705450
The NRF2-mediated cytoprotective response is central to cellular homoeostasis, and there is increasing interest in developing small-molecule activators of this pathway as therapeutics for diseases involving chronic oxidative stress. The...
2.
Heightman T, Callahan J, Chiarparin E, Coyle J, Griffiths-Jones C, Lakdawala A, et al.
J Med Chem
. 2019 Apr;
62(9):4683-4702.
PMID: 30973731
The KEAP1-NRF2-mediated cytoprotective response plays a key role in cellular homoeostasis. Insufficient NRF2 signaling during chronic oxidative stress may be associated with the pathophysiology of several diseases with an inflammatory...
3.
Kerns J, Busch-Petersen J, Fu W, Boehm J, Nie H, Muratore M, et al.
ACS Med Chem Lett
. 2019 Jan;
9(12):1164-1169.
PMID: 30613320
IκB kinase β (IKKβ or IKK2) is a key regulator of nuclear factor kappa B (NF-κB) and has received attention as a therapeutic target. Herein we report on the optimization...
4.
Smith Iii A, Lin Q, Doughty V, Zhuang L, McBriar M, Kerns J, et al.
Angew Chem Int Ed Engl
. 2018 May;
40(1):196-199.
PMID: 29711943
No abstract available.
5.
Yonchuk J, Foley J, Bolognese B, Logan G, Wixted W, Kou J, et al.
J Pharmacol Exp Ther
. 2017 Aug;
363(1):114-125.
PMID: 28790194
Nuclear factor (erythroid-derived 2)-like 2 (Nrf2) is a key regulator of oxidative stress and cellular repair and can be activated through inhibition of its cytoplasmic repressor, Kelch-like ECH-associated protein 1...
6.
Davies T, Wixted W, Coyle J, Griffiths-Jones C, Hearn K, McMenamin R, et al.
J Med Chem
. 2016 Apr;
59(8):3991-4006.
PMID: 27031670
KEAP1 is the key regulator of the NRF2-mediated cytoprotective response, and increasingly recognized as a target for diseases involving oxidative stress. Pharmacological intervention has focused on molecules that decrease NRF2-ubiquitination...
7.
Cleasby A, Yon J, Day P, Richardson C, Tickle I, Williams P, et al.
PLoS One
. 2014 Jun;
9(6):e98896.
PMID: 24896564
The protein Keap1 is central to the regulation of the Nrf2-mediated cytoprotective response, and is increasingly recognized as an important target for therapeutic intervention in a range of diseases involving...
8.
Wilson A, Kerns J, Callahan J, Moody C
J Med Chem
. 2013 Jul;
56(19):7463-76.
PMID: 23837912
The Nrf2-Keap1 system plays a major role in cellular defense against oxidative stress. Upon exposure to electrophiles, the cysteine-rich protein Keap1 is covalently modified, and it is this modification of...
9.
Kerns J, Nie H, Bondinell W, Widdowson K, Yamashita D, Rahman A, et al.
Bioorg Med Chem Lett
. 2011 Jul;
21(15):4409-15.
PMID: 21733692
A series of azepanone inhibitors of cathepsin S is described. Selectivity over both cathepsin K and cathepsin L was achieved by varying the P2 substituent. Ultimately, a balanced potency and...
10.
Miller D, Bamborough P, Christopher J, Baldwin I, Champigny A, Cutler G, et al.
Bioorg Med Chem Lett
. 2011 Mar;
21(8):2255-8.
PMID: 21429745
The discovery and hit-to-lead exploration of a novel series of selective IKK-β kinase inhibitors is described. The initial lead fragment 3 was identified by pharmacophore-directed virtual screening. Homology model-driven SAR...