Samuel L Graham
Overview
Explore the profile of Samuel L Graham including associated specialties, affiliations and a list of published articles.
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44
Citations
395
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Recent Articles
11.
Hills I, Holloway M, de Leon P, Nomland A, Zhu H, Rajapakse H, et al.
Bioorg Med Chem Lett
. 2009 Jul;
19(17):4993-5.
PMID: 19640712
During our ongoing efforts to develop a small molecule inhibitor targeting the beta-amyloid cleaving enzyme (BACE-1), we discovered a class of compounds bearing an aminoimidazole motif. Initial optimization led to...
12.
Bell I, Bednar R, Corcoran H, Fay J, Gallicchio S, Johnston V, et al.
Bioorg Med Chem Lett
. 2009 Jul;
19(16):4740-2.
PMID: 19577468
A series of tricyclic CGRP receptor antagonists was optimized in order to improve oral bioavailability. Attenuation of polar surface area and incorporation of a weakly basic indoline nitrogen led to...
13.
Tang C, Kuo Y, Pudvah N, Ellis J, Michener M, Egbertson M, et al.
Biochem Pharmacol
. 2009 Jun;
78(6):642-7.
PMID: 19481060
Brain penetration of drugs which are subject to P-glycoprotein (Pgp)-mediated efflux is attenuated, as manifested by the fact that the cerebrospinal fluid concentration (C(CSF)), a good surrogate of the unbound...
14.
Stachel S, Coburn C, Rush D, Jones K, Zhu H, Rajapakse H, et al.
Bioorg Med Chem Lett
. 2009 May;
19(11):2977-80.
PMID: 19409780
We have developed a novel series of heteroaromatic BACE-1 inhibitors. These inhibitors interact with the enzyme in a unique fashion that allows for potent binding in a non-traditional paradigm. In...
15.
Nantermet P, Rajapakse H, Stanton M, Stauffer S, Barrow J, Gregro A, et al.
ChemMedChem
. 2008 Dec;
4(1):37-40.
PMID: 19085994
No abstract available.
16.
Steele T, Hills I, Nomland A, de Leon P, Allison T, McGaughey G, et al.
Bioorg Med Chem Lett
. 2008 Nov;
19(1):17-20.
PMID: 19036583
A small molecule inhibitor of beta-secretase with a unique binding mode has been developed. Crystallographic determination of the enzyme-inhibitor complex shows the catalytic aspartate residues in the active site are...
17.
Stump C, Bell I, Bednar R, Bruno J, Fay J, Gallicchio S, et al.
Bioorg Med Chem Lett
. 2008 Nov;
19(1):214-7.
PMID: 19010673
Rational modification of a previously identified spirohydantoin lead structure has identified a series of potent spiroazaoxindole CGRP receptor antagonists. The azaoxindole was found to be a general replacement for the...
18.
Theberge C, Bednar R, Bell I, Corcoran H, Fay J, Hershey J, et al.
Bioorg Med Chem Lett
. 2008 Oct;
18(23):6122-5.
PMID: 18947992
The previously disclosed spirohydantoin-based CGRP receptor antagonists were optimized for potency through modification of the benzimidazolone substituents. Compounds were identified which had minimal shift in the cAMP functional assay containing...
19.
Sankaranarayanan S, Holahan M, Colussi D, Crouthamel M, Devanarayan V, Ellis J, et al.
J Pharmacol Exp Ther
. 2008 Oct;
328(1):131-40.
PMID: 18854490
beta-Site amyloid precursor protein (APP)-cleaving enzyme (BACE) 1 cleavage of amyloid precursor protein is an essential step in the generation of the potentially neurotoxic and amyloidogenic A beta 42 peptides...
20.
Barrow J, Stauffer S, Rittle K, Ngo P, Yang Z, Selnick H, et al.
J Med Chem
. 2008 Sep;
51(20):6259-62.
PMID: 18811140
A high-throughput screen at 100 microM inhibitor concentration for the BACE-1 enzyme revealed a novel spiropiperidine iminohydantoin aspartyl protease inhibitor template. An X-ray cocrystal structure with BACE-1 revealed a novel...