Howard Bregman
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Explore the profile of Howard Bregman including associated specialties, affiliations and a list of published articles.
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32
Citations
834
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Recent Articles
1.
Bambouskova M, Gorvel L, Lampropoulou V, Sergushichev A, Loginicheva E, Johnson K, et al.
Nature
. 2018 Apr;
556(7702):501-504.
PMID: 29670287
Metabolic regulation has been recognized as a powerful principle guiding immune responses. Inflammatory macrophages undergo extensive metabolic rewiring marked by the production of substantial amounts of itaconate, which has recently...
2.
La D, Peterson E, Bode C, Boezio A, Bregman H, Chu-Moyer M, et al.
Bioorg Med Chem Lett
. 2017 Jun;
27(15):3477-3485.
PMID: 28629594
The voltage-gated sodium channel Na1.7 has received much attention from the scientific community due to compelling human genetic data linking gain- and loss-of-function mutations to pain phenotypes. Despite this genetic...
3.
Chakka N, Andrews K, Berry L, Bregman H, Gunaydin H, Huang L, et al.
Eur J Med Chem
. 2017 Jun;
137:63-75.
PMID: 28575722
Glycine receptors (GlyRs) are pentameric glycine-gated chloride ion channels that are enriched in the brainstem and spinal cord where they have been demonstrated to play a role in central nervous...
4.
Marx I, Dineen T, Able J, Bode C, Bregman H, Chu-Moyer M, et al.
ACS Med Chem Lett
. 2017 Mar;
8(3):378.
PMID: 28337335
[This corrects the article DOI: 10.1021/acsmedchemlett.6b00243.].
5.
Weiss M, Dineen T, Marx I, Altmann S, Boezio A, Bregman H, et al.
J Med Chem
. 2017 Mar;
60(14):5969-5989.
PMID: 28287723
Several reports have recently emerged regarding the identification of heteroarylsulfonamides as Na1.7 inhibitors that demonstrate high levels of selectivity over other Na isoforms. The optimization of a series of internal...
6.
Bregman H, Simard J, Andrews K, Ayube S, Chen H, Gunaydin H, et al.
J Med Chem
. 2016 Dec;
60(3):1105-1125.
PMID: 28001399
Current pain therapeutics suffer from undesirable psychotropic and sedative side effects, as well as abuse potential. Glycine receptors (GlyRs) are inhibitory ligand-gated ion channels expressed in nerves of the spinal...
7.
Marx I, Dineen T, Able J, Bode C, Bregman H, Chu-Moyer M, et al.
ACS Med Chem Lett
. 2016 Dec;
7(12):1062-1067.
PMID: 27994738
Human genetic evidence has identified the voltage-gated sodium channel Na1.7 as an attractive target for the treatment of pain. We initially identified naphthalene sulfonamide as a potent and selective inhibitor...
8.
Huang X, Shaffer P, Ayube S, Bregman H, Chen H, Lehto S, et al.
Nat Struct Mol Biol
. 2016 Dec;
24(2):108-113.
PMID: 27991902
Current therapies to treat persistent pain and neuropathic pain are limited by poor efficacy, side effects and risk of addiction. Here, we present a novel class of potent selective, central...
9.
DiMauro E, Altmann S, Berry L, Bregman H, Chakka N, Chu-Moyer M, et al.
J Med Chem
. 2016 Jul;
59(17):7818-39.
PMID: 27441383
The majority of potent and selective hNaV1.7 inhibitors possess common pharmacophoric features that include a heteroaryl sulfonamide headgroup and a lipophilic aromatic tail group. Recently, reports of similar aromatic tail...
10.
Liu L, Lee M, Kim J, Whittington D, Bregman H, Hua Z, et al.
Bioorg Med Chem
. 2016 May;
24(13):3093.
PMID: 27234892
No abstract available.