R L Magolda
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Explore the profile of R L Magolda including associated specialties, affiliations and a list of published articles.
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37
Citations
1901
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Recent Articles
1.
Xue C, He X, Corbett R, Roderick J, Wasserman Z, Liu R, et al.
J Med Chem
. 2001 Oct;
44(21):3351-4.
PMID: 11585440
SAR exploration at P1' using an anti-succinate-based macrocyclic hydroxamic acid as a template led to the identification of several bulky biphenylmethyl P1' derivatives which confer potent porcine TACE and anti-TNF-alpha...
2.
Yao W, Wasserman Z, Chao M, Reddy G, Shi E, Liu R, et al.
J Med Chem
. 2001 Oct;
44(21):3347-50.
PMID: 11585439
A pharmacophore model of the P1' site, specific for aggrecanase, was defined using the specificity studies of the matrix metalloproteinases and the similar biological activity of aggrecanase and MMP-8. Incorporation...
3.
Xue C, Voss M, Nelson D, Duan J, Cherney R, Jacobson I, et al.
J Med Chem
. 2001 Jul;
44(16):2636-60.
PMID: 11472217
To search for TNF-alpha (tumor necrosis factor alpha) converting enzyme (TACE) inhibitors, we designed a new class of macrocyclic hydroxamic acids by linking the P1 and P2' residues of acyclic...
4.
Jaffee B, Manos E, Collins R, Czerniak P, Favata M, Magolda R, et al.
Biochem Biophys Res Commun
. 2000 Feb;
268(2):647-51.
PMID: 10679258
The MAP kinase pathway has been well-characterized as a cascade of sequential protein phosphorylation events leading to the upregulation of a variety of genes in response to growth factors and...
5.
Abbaszade I, Liu R, Yang F, Rosenfeld S, ROSS O, Link J, et al.
J Biol Chem
. 1999 Aug;
274(33):23443-50.
PMID: 10438522
Aggrecan is responsible for the mechanical properties of cartilage. One of the earliest changes observed in arthritis is the depletion of cartilage aggrecan due to increased proteolytic cleavage within the...
6.
Arner E, Pratta M, Decicco C, Xue C, Newton R, Trzaskos J, et al.
Ann N Y Acad Sci
. 1999 Jul;
878:92-107.
PMID: 10415722
In arthritic diseases there is a gradual erosion of cartilage that leads to a loss of joint function. Aggrecan, which provides cartilage with its properties of compressibility and elasticity, is...
7.
Tortorella M, Burn T, Pratta M, Abbaszade I, Hollis J, Liu R, et al.
Science
. 1999 Jun;
284(5420):1664-6.
PMID: 10356395
We purified, cloned, and expressed aggrecanase, a protease that is thought to be responsible for the degradation of cartilage aggrecan in arthritic diseases. Aggrecanase-1 [a disintegrin and metalloproteinase with thrombospondin...
8.
Pinto D, Batt D, PITTS W, Petraitis J, Orwat M, Wang S, et al.
Bioorg Med Chem Lett
. 1999 May;
9(7):919-24.
PMID: 10230611
The discovery of terphenyl derivatives as highly selective COX-2 inhibitors resulted from our efforts to overcome poor pharmacokinetics demonstrated by the COX-2 selective diarylthiophene DuP 697 [2-bromo-4-(4'-sulfonylmethyl)phenyl-5-(4'-fluoro)phenylthiophe ne]. Detailed SAR...
9.
Duncia J, Santella 3rd J, Higley C, PITTS W, Wityak J, Frietze W, et al.
Bioorg Med Chem Lett
. 1999 Jan;
8(20):2839-44.
PMID: 9873633
In search of antiinflammatory drugs with a new mechanism of action, U0126 was found to functionally antagonize AP-1 transcriptional activity via noncompetitive inhibition of the dual specificity kinase MEK with...
10.
Batt D, Petraitis J, Sherk S, Copeland R, Dowling R, Taylor T, et al.
Bioorg Med Chem Lett
. 1999 Jan;
8(13):1745-50.
PMID: 9873427
Structure-activity relationships were explored for some analogs of Brequinar having a linking atom between the 2-biphenyl substituent and the quinoline ring. Activities as inhibitors of dihydroorotate dehydrogenase and the mixed...