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Steven Fletcher

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Articles 94
Citations 1465
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Recent Articles
1.
Tulapurkar M, Shirey K, Lugkey K, Luo W, Lal R, Galan A, et al.
J Pharmacol Exp Ther . 2025 Feb; 392(3):100031. PMID: 39969269
We previously identified a small molecule, UM101, predicted to bind to the substrate-binding groove of p38α mitogen-activated protein kinase (MAPK) near the binding site of its proinflammatory substrate, mitogen-activated protein...
2.
Goodis C, Eberly C, Chan A, Kim M, Lowe B, Civin C, et al.
Eur J Med Chem . 2025 Jan; 285:117190. PMID: 39813774
Current treatments for acute myeloid leukemias (AMLs) cure fewer than 30 % of patients. This low efficacy is due, in part, to the inter-patient and intra-patient heterogeneity of AMLs; accordingly,...
3.
Chan A, Mitchell A, Grogan L, Shapiro P, Fletcher S
Bioorg Med Chem . 2024 Apr; 104:117680. PMID: 38582047
Many disease states require multiple drugs to inhibit multiple targets for their effective treatment/management, i.e. a drug cocktail regimen, or "polypharmacy". Polypharmacology, in contrast, is the development of single agents...
4.
Truong N, Cottingham A, Dharmaraj S, Shaw J, Lasola J, Goodis C, et al.
Bioeng Transl Med . 2024 Jan; 9(1):e10611. PMID: 38193117
Excessive immune activation and immunosuppression are opposing factors that contribute to the dysregulated innate and adaptive immune responses seen in severe inflammation and sepsis. Here, a novel analog of the...
5.
Chen L, Lowe B, Fletcher S
RSC Adv . 2023 Nov; 13(49):34322-34334. PMID: 38024975
Overexpression of the anti-apoptotic protein MCL-1 is associated with a plethora of human cancers, and it reduces the sensitivity of cancer cells to approved chemotherapies. Accordingly, the discovery of MCL-1...
6.
Shukla S, Riveros C, Al-Toubat M, Chardon-Robles J, Osumi T, Serrano S, et al.
Cancers (Basel) . 2023 Aug; 15(15). PMID: 37568667
Bromodomains (BD) are epigenetic readers of histone acetylation involved in chromatin remodeling and transcriptional regulation of several genes including protooncogene cellular myelocytomatosis (c-Myc). c-Myc is difficult to target directly by...
7.
Chauhan J, Yoshioka M, Pogash S, Strovel J, Fletcher S
Bioorg Med Chem Lett . 2023 Mar; 86:129220. PMID: 36905966
The bromodomain and extra-terminal domain (BET) proteins are epigenetic readers involved in the regulation of gene transcription. Inhibitors of the BET proteins, in particular BRD4, have demonstrated anti-tumour activities and...
8.
Chen L, Chauhan J, Yap J, Goodis C, Wilder P, Fletcher S
RSC Med Chem . 2023 Feb; 14(1):103-112. PMID: 36760746
The anti-apoptotic protein MCL-1, which is overexpressed in multiple cancers, is presently a focus for the development of targeted drugs in oncology. We previously discovered inhibitors of MCL-1 based on...
9.
Truong N, Goodis C, Cottingham A, Shaw J, Fletcher S, Pearson R
ACS Pharmacol Transl Sci . 2022 Nov; 5(11):1128-1141. PMID: 36407956
Histone deacetylase inhibitors (HDACi) induce potent anti-inflammatory responses when used to treat inflammatory diseases. Suberoylanilide hydroxamic acid (SAHA), a pan-HDACi, decreases pro-inflammatory cytokine levels and attenuates cytokine storm in sepsis;...
10.
Chen L, Chan A, Wilder P, Fletcher S
Drug Dev Res . 2022 Oct; 83(8):1879-1889. PMID: 36281026
MCL-1 is a member of the BCL-2 family of proteins that regulates the mitochondrial pathway of apoptosis. Overexpression of MCL-1 is associated with the development and progression of a range...