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» Authors » James F Callahan

James F Callahan

Explore the profile of James F Callahan including associated specialties, affiliations and a list of published articles. Areas
Snapshot
Articles 23
Citations 1473
Followers 0
Related Specialties
Chemistry
Pharmacology
Biochemistry
Top 10 Co-Authors
Yolanda Sanchez
Jeffrey K Kerns
Patricia L Podolin
Hongxing Yan
Thomas G Davies
Caroline Richardson
Brian J Bolognese
Edward F Nemeth
David Norton
Henriette M G Willems
Published In
J Med Chem
J Pharmacol Exp Ther
Bioorg Med Chem
Mol Pharmacol
Bone
Affiliations
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Recent Articles
1.
Exploration of the P1 residue in 3CL protease inhibitors leading to the discovery of a 2-tetrahydrofuran P1 replacement
Barton L, Callahan J, Cantizani J, Concha N, Cotillo Torrejon I, Goodwin N, et al.
Bioorg Med Chem . 2024 Feb; 100:117618. PMID: 38309201
The virally encoded 3C-like protease (3CL) is a well-validated drug target for the inhibition of coronaviruses including Severe Acute Respiratory Syndrome Coronavirus-2 (SARS-CoV-2). Most inhibitors of 3CL are peptidomimetic, with...
2.
NRF2 Activation Reprograms Defects in Oxidative Metabolism to Restore Macrophage Function in Chronic Obstructive Pulmonary Disease
Ryan E, Sadiku P, Coelho P, Watts E, Zhang A, Howden A, et al.
Am J Respir Crit Care Med . 2023 Feb; 207(8):998-1011. PMID: 36724365
Chronic obstructive pulmonary disease (COPD) is a disease characterized by persistent airway inflammation and disordered macrophage function. The extent to which alterations in macrophage bioenergetics contribute to impaired antioxidant responses...
3.
Fragment-Guided Discovery of Pyrazole Carboxylic Acid Inhibitors of the Kelch-like ECH-Associated Protein 1: Nuclear Factor Erythroid 2 Related Factor 2 (KEAP1:NRF2) Protein-Protein Interaction
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...
4.
Structure-Activity and Structure-Conformation Relationships of Aryl Propionic Acid Inhibitors of the Kelch-like ECH-Associated Protein 1/Nuclear Factor Erythroid 2-Related Factor 2 (KEAP1/NRF2) Protein-Protein Interaction
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...
5.
Discovery of a crystalline sulforaphane analog with good solid-state stability and engagement of the Nrf2 pathway in vitro and in vivo
Boehm J, Davis R, Murar C, Li T, McCleland B, Dong S, et al.
Bioorg Med Chem . 2019 Jan; 27(4):579-588. PMID: 30626555
The antioxidant natural product sulforaphane (SFN) is an oil with poor aqueous and thermal stability. Recent work with SFN has sought to optimize methods of formulation for oral and topical...
6.
Characterization of the Potent, Selective Nrf2 Activator, 3-(Pyridin-3-Ylsulfonyl)-5-(Trifluoromethyl)-2-Chromen-2-One, in Cellular and In Vivo Models of Pulmonary Oxidative Stress
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...
7.
Discovering Drugs with DNA-Encoded Library Technology: From Concept to Clinic with an Inhibitor of Soluble Epoxide Hydrolase
Belyanskaya S, Ding Y, Callahan J, Lazaar A, Israel D
Chembiochem . 2017 Mar; 18(9):837-842. PMID: 28281333
DNA-encoded chemical library technology was developed with the vision of its becoming a transformational platform for drug discovery. The hope was that a new paradigm for the discovery of low-molecular-weight...
8.
Monoacidic Inhibitors of the Kelch-like ECH-Associated Protein 1: Nuclear Factor Erythroid 2-Related Factor 2 (KEAP1:NRF2) Protein-Protein Interaction with High Cell Potency Identified by Fragment-Based Discovery
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...
9.
Structure of the BTB domain of Keap1 and its interaction with the triterpenoid antagonist CDDO
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...
10.
Analytical approaches for quantification of a Nrf2 pathway activator: overcoming bioanalytical challenges to support a toxicity study
Perez H, Junnotula V, Knecht D, Nie H, Sanchez Y, Boehm J, et al.
Analyst . 2014 Feb; 139(8):1902-12. PMID: 24563904
Activation of the Nrf2 stress pathway is known to play an important role in the defense mechanism against electrophilic and oxidative damage to biological macromolecules (DNA, lipids, and proteins). Chemical...