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Matthew Waldbrook

Explore the profile of Matthew Waldbrook including associated specialties, affiliations and a list of published articles. Areas
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Articles 12
Citations 350
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Recent Articles
1.
Johnson Jr J, Focken T, Karimi Tari P, Dube C, Goodchild S, Andrez J, et al.
Br J Pharmacol . 2024 Jun; 181(20):3993-4011. PMID: 38922847
Background And Purpose: Inhibitors of voltage-gated sodium channels (Nas) are important anti-epileptic drugs, but the contribution of specific channel isoforms is unknown since available inhibitors are non-selective. We aimed to...
2.
Goodchild S, Shuart N, Williams A, Ye W, Parrish R, Soriano M, et al.
ACS Chem Neurosci . 2024 Feb; 15(6):1169-1184. PMID: 38359277
Voltage-gated sodium channel (Na) inhibitors are used to treat neurological disorders of hyperexcitability such as epilepsy. These drugs act by attenuating neuronal action potential firing to reduce excitability in the...
3.
Cutts A, Chowdhury S, Ratkay L, Eyers M, Young C, Namdari R, et al.
J Pharmacol Exp Ther . 2023 Mar; 386(1):4-14. PMID: 36958846
Divalent metal transporter 1 (DMT1) cotransports ferrous iron and protons and is the primary mechanism for uptake of nonheme iron by enterocytes. Inhibitors are potentially useful as therapeutic agents to...
4.
Johnson J, Focken T, Khakh K, Karimi Tari P, Dube C, Goodchild S, et al.
Elife . 2022 Mar; 11. PMID: 35234610
NBI-921352 (formerly XEN901) is a novel sodium channel inhibitor designed to specifically target Na1.6 channels. Such a molecule provides a precision-medicine approach to target -related epilepsy syndromes (-RES), where gain-of-function...
5.
Safina B, McKerrall S, Sun S, Chen C, Chowdhury S, Jia Q, et al.
J Med Chem . 2021 Mar; 64(6):2953-2966. PMID: 33682420
Na1.7 is an extensively investigated target for pain with a strong genetic link in humans, yet in spite of this effort, it remains challenging to identify efficacious, selective, and safe...
6.
Focken T, Burford K, Grimwood M, Zenova A, Andrez J, Gong W, et al.
J Med Chem . 2019 Sep; 62(21):9618-9641. PMID: 31525968
Nonselective antagonists of voltage-gated sodium (Na) channels have been long used for the treatment of epilepsies. The efficacy of these drugs is thought to be due to the block of...
7.
Sun S, Jia Q, Zenova A, Wilson M, Chowdhury S, Focken T, et al.
J Med Chem . 2018 Dec; 62(2):908-927. PMID: 30499663
Herein, we report the discovery and optimization of a series of orally bioavailable acyl sulfonamide Na1.7 inhibitors that are selective for Na1.7 over Na1.5 and highly efficacious in in vivo...
8.
Bankar G, Goodchild S, Howard S, Nelkenbrecher K, Waldbrook M, Dourado M, et al.
Cell Rep . 2018 Sep; 24(12):3133-3145. PMID: 30231997
Selective block of Na1.7 promises to produce non-narcotic analgesic activity without motor or cognitive impairment. Several Na1.7-selective blockers have been reported, but efficacy in animal pain models required high multiples...
9.
Focken T, Chowdhury S, Zenova A, Grimwood M, Chabot C, Sheng T, et al.
J Med Chem . 2018 May; 61(11):4810-4831. PMID: 29737846
The sodium channel Na1.7 has emerged as a promising target for the treatment of pain based on strong genetic validation of its role in nociception. In recent years, a number...
10.
Focken T, Liu S, Chahal N, Dauphinais M, Grimwood M, Chowdhury S, et al.
ACS Med Chem Lett . 2016 Mar; 7(3):277-82. PMID: 26985315
We report on a novel series of aryl sulfonamides that act as nanomolar potent, isoform-selective inhibitors of the human sodium channel hNaV1.7. The optimization of these inhibitors is described. We...