Publications
The following are selected recent publications by PCMD scientists.
Neeves K, Illing DAR, and Diamond SL. Thrombin flux and wall shear rate regulate fibrin fiber deposition state during polymerization under flow. Biophysical Journal, in press.
Pagano N, Wong EY, Breiding T, Liu H, Wilbuer A, Bregman H, Shen Q, Diamond SL, and Meggers E. From Imide to Lactam Metallo-Pyridocarbazoles: Distinct Scaffolds for the Design of Selective Protein Kinase Inhibitors. J Org. Chem, in press.
Ma H, Horiuchi KY, Wang Y, Kucharewicz SA, Diamond SL.
Nanoliter
Homogenous Ultra-High Throughput Screening Microarray for Lead Discoveries
and IC(50) Profiling. Assay Drug Dev Technol. 2005 Apr;3(2):177-87.
Gosalia DN, Salisbury CM, Maly DJ, Ellman JA, Diamond SL.
Profiling
serine protease substrate specificity with solution phase fluorogenic
peptide microarrays. Proteomics. 2005 Apr;5(5):1292-8.
Gosalia DN, Salisbury CM, Ellman JA, Diamond SL.
High
Throughput Substrate Specificity Profiling of Serine and Cysteine
Proteases Using Solution-phase Fluorogenic Peptide Microarrays.
Mol Cell Proteomics. 2005 May;4(5):626-636. Epub 2005 Feb 10.
Lo K, Diamond SL.
Blood
coagulation kinetics: high throughput method for real-time reaction
monitoring. Thromb Haemost. 2004 Oct;92(4):874-82.
Gosalia DN, Diamond SL.
Printing
chemical libraries on microarrays for fluid phase nanoliter reactions.
Proc Natl Acad Sci U S A. 2003 Jul 22;100(15):8721-6. Epub 2003
Jul 8.
Trojanowski JQ, Smith AB, Huryn D, Lee VM.
Microtubule-stabilising drugs for therapy of Alzheimer's disease
and other neurodegenerative disorders with axonal transport impairments.
Expert Opin Pharmacother. 2005 May;6(5):683-686.
Smith AB 3rd, Mesaros EF, Meyer EA.
Total
synthesis of (-)-kendomycin exploiting a Petasis-Ferrier rearrangement/ring-closing
olefin metathesis synthetic strategy. J Am Chem Soc. 2005
May 18;127(19):6948-9.
Smith AB 3rd, Adams CM, Barbosa SA, Degnan AP.
Free
in PMC A unified approach to the tedanolides: total synthesis of
(+)-13-deoxytedanolide. Proc Natl Acad Sci U S A. 2004
Aug 17;101(33):12042-7. Epub 2004 May 26.
Si Z, Madani N, Cox JM, Chruma JJ, Klein JC, Schon A, Phan N, Wang
L, Biorn AC, Cocklin S, Chaiken I, Freire E, Smith AB 3rd, Sodroski
JG.
Small-molecule
inhibitors of HIV-1 entry block receptor-induced conformational
changes in the viral envelope glycoproteins. Proc Natl
Acad Sci U S A. 2004 Apr 6;101(14):5036-41. Epub 2004 Mar 29.
Smith AB 3rd, Pitram SM, Boldi AM, Gaunt MJ, Sfouggatakis C, Moser
WH.
Multicomponent
linchpin couplings. Reaction of dithiane anions with terminal epoxides,
epichlorohydrin, and vinyl epoxides: efficient, rapid, and stereocontrolled
assembly of advanced fragments for complex molecule synthesis.
J Am Chem Soc. 2003 Nov 26;125(47):14435-45.
Macdonald GJ, Branch CL, Hadley MS, Johnson CN, Nash DJ, Smith
AB, Stemp G, Thewlis KM, Vong AK, Austin NE, Jeffrey P, Winborn
KY, Boyfield I, Hagan JJ, Middlemiss DN, Reavill C, Riley GJ, Watson
JM, Wood M, Parker SG, Ashby Jr CR.
Design
and synthesis of trans-3-(2-(4-((3-(3-(5-methyl-1,2,4-oxadiazolyl))-
phenyl)carboxamido)cyclohexyl)ethyl)-7-methylsulfonyl-2,3,4,5-tetrahydro-1H-3-benzazepine
(SB-414796): a potent and selective dopamine D3 receptor antagonist.
J Med Chem. 2003 Nov 6;46(23):4952-64.
Williams DS, Atilla GE, Bregman H, Arzoumanian A, Klein PS, Meggers
E.
Switching
on a signaling pathway with an organoruthenium complex.
Angew Chem Int Ed Engl. 2005 Mar 18;44(13):1984-7.
Bregman H, Williams DS, Atilla GE, Carroll PJ, Meggers E.
An
organometallic inhibitor for glycogen synthase kinase 3. J Am
Chem Soc. 2004 Oct 27;126(42):13594-5.
Zhang L, Carroll P, Meggers E.
Ruthenium
complexes as protein kinase inhibitors. Org Lett. 2004
Feb 19;6(4):521-3.
Huryn DM, Konradi AW, Ashwell S, Freedman SB, Lombardo LJ, Pleiss
MA, Thorsett ED, Yednock T, Kennedy JD.
The
identification and optimization of orally efficacious, small molecule
VLA-4 antagonists. Curr Top Med Chem. 2004;4(14):1473-84.
Review.
Di L, Kerns EH, Gao N, Li SQ, Huang Y, Bourassa JL, Huryn DM.
Experimental
design on single-time-point high-throughput microsomal stability
assay. J Pharm Sci. 2004 Jun;93(6):1537-44.
Huryn DM, Ashwell S, Baudy R, Dressen DB, Gallaway W, Grant FS,
Konradi A, Ley RW, Petusky S, Pleiss MA, Sarantakis D, Semko CM,
Sherman MM, Tio C, Zhang L.
Synthesis,
characterization and evaluation of pro-drugs of VLA-4 antagonists.
Bioorg Med Chem Lett. 2004 Apr 5;14(7):1651-4. Erratum in: Bioorg
Med Chem Lett. 2004 Nov 1;14(21):5449.
Di L, Kerns EH, Hong Y, Kleintop TA, McConnell OJ, Huryn DM.
Optimization of a higher throughput microsomal stability screening
assay for profiling drug discovery candidates. J Biomol
Screen. 2003 Aug;8(4):453-62.
Huryn DM, Sluboski BC, Tam SY, Weigele M, Sim I, Anderson BD, Mitsuya
H, Broder S.
Synthesis and anti-HIV activity of isonucleosides. J Med
Chem. 1992 Jun 26;35(13):2347-54.
Radivoyevitch T, Kashlan OB, Cooperman BS.
Rational
polynomial representation of ribonucleotide reductase activity.
BMC Biochem. 2005 May 6;6(1):8.
Gao Y, Kashlan OB, Kaur J, Tan C, Cooperman BS.
Mechanisms
of action of peptide inhibitors of mammalian ribonucleotide reductase
targeting quaternary structure. Biopolymers. 2005;80(1):9-17.
Gao Y, Liehr S, Cooperman BS.
Affinity-driven
selection of tripeptide inhibitors of ribonucleotide reductase.
Bioorg Med Chem Lett. 2002 Feb 25;12(4):513-5.
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