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R L Panek

Explore the profile of R L Panek including associated specialties, affiliations and a list of published articles. Areas
Snapshot
Articles 36
Citations 466
Followers 0
Related Specialties
Chemistry
Pharmacology
Biochemistry
Top 10 Co-Authors
G H Lu
T C Major
A M Doherty
J M Hamby
T K Dahring
A J Kraker
W L Cody
B L Batley
H D Showalter
S T Rapundalo
Published In
J Med Chem
J Pharmacol Exp Ther
Biochem Biophys Res Commun
J Cardiovasc Pharmacol
Mol Pharmacol
Affiliations
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Recent Articles
1.
p21-activated kinase-1 (PAK1) inhibition of the human scavenger receptor class B, type I promoter in macrophages is independent of PAK1 kinase activity, but requires the GTPase-binding domain
Hullinger T, Panek R, Xu X, Karathanasis S
J Biol Chem . 2001 Oct; 276(50):46807-14. PMID: 11585816
Scavenger receptor class B, type I (SR-BI), is a high density lipoprotein receptor that mediates the flux of cholesterol between high density lipoprotein and cells. Recent evidence suggests that SR-BI...
2.
Soluble 2-substituted aminopyrido[2,3-d]pyrimidin-7-yl ureas. Structure-activity relationships against selected tyrosine kinases and exploration of in vitro and in vivo anticancer activity
Schroeder M, Hamby J, CONNOLLY C, Grohar P, Winters R, Barvian M, et al.
J Med Chem . 2001 Jun; 44(12):1915-26. PMID: 11384237
In continuing our search for medicinal agents to treat proliferative diseases, we have discovered 2-substituted aminopyrido[2,3-d]pyrimidin-7-yl ureas as a novel class of soluble, potent, broadly active tyrosine kinase (TK) inhibitors....
3.
Synthesis and structure-activity relationships of 7-substituted 3-(2, 6-dichlorophenyl)-1,6-naphthyridin-2(1H)-ones as selective inhibitors of pp60(c-src)
Thompson A, Rewcastle G, Boushelle S, Hartl B, Kraker A, Lu G, et al.
J Med Chem . 2000 Aug; 43(16):3134-47. PMID: 10956222
7-substituted 3-(2,6-dichlorophenyl)-1,6-naphthyridin-2(1H)-ones are potent inhibitors of protein tyrosine kinases, with some selectivity for c-Src. The compounds were prepared by condensing 4, 6-diaminonicotinaldehyde with 2,6-dichlorophenylacetonitrile and selectively converting the 2- and...
4.
Progress in the development of inhibitors of SH2 domains
Cody W, Lin Z, Panek R, Rose D, Rubin J
Curr Pharm Des . 2000 Jan; 6(1):59-98. PMID: 10637372
SH2 domains are discrete structural motifs common to a variety of critical intracellular signaling proteins. Inhibitors of specific SH2 domains have become important therapeutic targets in the treatment and/or prevention...
5.
Structure-activity relationships for 5-substituted 1-phenylbenzimidazoles as selective inhibitors of the platelet-derived growth factor receptor
Palmer B, Kraker A, Hartl B, Panopoulos A, Panek R, Batley B, et al.
J Med Chem . 1999 Jul; 42(13):2373-82. PMID: 10395478
Following an earlier discovery of 1-phenylbenzimidazoles as ATP-site inhibitors of the platelet-derived growth factor receptor (PDGFR), further structure-activity relationships for analogues (particularly 5-substituted derivatives) are reported. The data are consistent...
6.
Structure-activity relationships for 1-phenylbenzimidazoles as selective ATP site inhibitors of the platelet-derived growth factor receptor
Palmer B, Smaill J, Boyd M, Boschelli D, Doherty A, Hamby J, et al.
J Med Chem . 1999 Jan; 41(27):5457-65. PMID: 9876115
1-Phenylbenzimidazoles are shown to be a new class of ATP-site inhibitors of the platelet-derived growth factor receptor (PDGFR). Structure-activity relationships (SARs) are narrow, with closely related heterocycles being inactive. A...
7.
Synthesis and tyrosine kinase inhibitory activity of a series of 2-amino-8H-pyrido[2,3-d]pyrimidines: identification of potent, selective platelet-derived growth factor receptor tyrosine kinase inhibitors
Boschelli D, Wu Z, KLUTCHKO S, Showalter H, Hamby J, Lu G, et al.
J Med Chem . 1998 Oct; 41(22):4365-77. PMID: 9784112
Screening of a compound library led to the identification of 2-amino-6-(2,6-dichlorophenyl)-8-methylpyrido[2,3-d]pyrimidine (1) as a inhibitor of the platelet-derived growth factor receptor (PDGFr), fibroblast growth factor receptor (FGFr), and c-src tyrosine...
8.
Design of peptidomimetics that inhibit the association of phosphatidylinositol 3-kinase with platelet-derived growth factor-beta receptor and possess cellular activity
Eaton S, Cody W, Doherty A, Holland D, Panek R, Lu G, et al.
J Med Chem . 1998 Oct; 41(22):4329-42. PMID: 9784108
Phosphorylated tyrosine residues of growth factor receptors that associate with intracellular proteins containing src-homology 2 (SH2) domains are integral components in several signal transduction pathways related to proliferative diseases such...
9.
Crystal structure of an angiogenesis inhibitor bound to the FGF receptor tyrosine kinase domain
Mohammadi M, Froum S, Hamby J, Schroeder M, Panek R, Lu G, et al.
EMBO J . 1998 Oct; 17(20):5896-904. PMID: 9774334
Angiogenesis, the sprouting of new blood vessels from pre-existing ones, is an essential physiological process in development, yet also plays a major role in the progression of human diseases such...
10.
2-Substituted aminopyrido[2,3-d]pyrimidin-7(8H)-ones. structure-activity relationships against selected tyrosine kinases and in vitro and in vivo anticancer activity
KLUTCHKO S, Hamby J, Boschelli D, Wu Z, Kraker A, Amar A, et al.
J Med Chem . 1998 Aug; 41(17):3276-92. PMID: 9703473
While engaged in therapeutic intervention against a number of proliferative diseases, we have discovered the 2-aminopyrido[2, 3-d]pyrimidin-7(8H)-ones as a novel class of potent, broadly active tyrosine kinase (TK) inhibitors. An...