Mark E Fraley
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Explore the profile of Mark E Fraley including associated specialties, affiliations and a list of published articles.
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33
Citations
269
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Recent Articles
1.
Staas D, Bell I, Burgey C, Deng J, Gallicchio S, Lim J, et al.
Bioorg Med Chem Lett
. 2024 Sep;
112:129944.
PMID: 39233187
A novel series of 3-amino-piperidin-2-one-based calcitonin gene-related peptide (CGRP) receptor antagonists was invented based upon the discovery of unexpected structure-activity observations. Initial exploration of the structure-activity relationships enabled the generation...
2.
Fluorinated Isoindolinone-Based Glucosylceramide Synthase Inhibitors with Low Human Dose Projections
Loughran H, Schirripa K, Roecker A, Breslin M, Tong L, Fillgrove K, et al.
ACS Med Chem Lett
. 2024 Jan;
15(1):123-131.
PMID: 38229758
Inhibition of glucosylceramide synthase (GCS) has been proposed as a therapeutic strategy for the treatment of Parkinson's Disease (PD), particularly in patients where glycosphingolipid accumulation and lysosomal impairment are thought...
3.
Moore E, Bell I, Fraley M, Burgey C, White R, Li C, et al.
Cephalalgia
. 2024 Jan;
44(1):3331024231226186.
PMID: 38215228
Background: The trigeminal sensory neuropeptide calcitonin gene-related peptide (CGRP) is identified as an essential element in migraine pathogenesis. Methods: and studies evaluated pharmacologic properties of the CGRP receptor antagonist atogepant....
4.
Roecker A, Schirripa K, Loughran H, Tong L, Liang T, Fillgrove K, et al.
ACS Med Chem Lett
. 2023 Feb;
14(2):146-155.
PMID: 36793422
Parkinson's disease is the second most prevalent progressive neurodegenerative disorder characterized by the loss of dopaminergic neurons in the substantia nigra. Loss-of-function mutations in GBA, the gene that encodes for...
5.
Moore E, Fraley M, Bell I, Burgey C, White R, Li C, et al.
J Pharmacol Exp Ther
. 2020 Jan;
373(1).
PMID: 31992609
A growing body of evidence has implicated the calcitonin gene-related peptide (CGRP) receptors in migraine pathophysiology. With the recent approval of monoclonal antibodies targeting CGRP or the CGRP receptor, the...
6.
Crowley B, Stump C, Nguyen D, Potteiger C, McWherter M, Paone D, et al.
Bioorg Med Chem Lett
. 2015 Aug;
25(21):4777-4781.
PMID: 26231160
In our efforts to develop CGRP receptor antagonists as backups to MK-3207, 2, we employed a scaffold hopping approach to identify a series of novel oxazolidinone-based compounds. The development of...
7.
Garbaccio R, Brnardic E, Fraley M, Hartman G, Hutson P, OBrien J, et al.
ACS Med Chem Lett
. 2014 Jun;
1(8):406-10.
PMID: 24900224
Novel oxazolobenzimidazoles are described as potent and selective positive allosteric modulators of the metabotropic glutamate receptor 2. The discovery of this class and optimization of its physical and pharmacokinetic properties...
8.
Converso A, Hartingh T, Fraley M, Garbaccio R, Hartman G, Huang S, et al.
Bioorg Med Chem Lett
. 2014 May;
24(12):2737-40.
PMID: 24813734
Elevated plasma homocysteine (Hcy) levels are an independent risk factor for the onset and progression of Alzheimer's disease. Reduction of Hcy to normal levels therefore presents a new approach for...
9.
Roecker A, Mercer S, Schreier J, Cox C, Fraley M, Steen J, et al.
ChemMedChem
. 2013 Dec;
9(2):311-22.
PMID: 24376006
The field of small-molecule orexin antagonist research has evolved rapidly in the last 15 years from the discovery of the orexin peptides to clinical proof-of-concept for the treatment of insomnia....
10.
Dudkin V, Rickert K, Kreatsoulas C, Wang C, Arrington K, Fraley M, et al.
Bioorg Med Chem Lett
. 2012 Mar;
22(7):2609-12.
PMID: 22374217
Pyridyl aminothiazoles comprise a novel class of ATP-competitive Chk1 inhibitors with excellent inhibitory potential. Modification of the core with ethylenediamine amides provides compounds with low picomolar potency and very high...