The Penn Center for
Molecular Discovery

Institute for Medicine and Engineering
1024 Vagelos Research Laboratories
The University of Pennsylvania
Philadelphia, PA 19104

Tel 215-573-5702 (office)
Tel 215-573-5704 (lab)
Fax 215-573-7227

Email pcmd@seas.upenn.edu

Publications

The following are selected recent publications by PCMD scientists.

Neeves KB, Illing DA, Diamond SL. Thrombin flux and wall shear rate regulate fibrin fiber deposition state during polymerization under flow. Biophys J Apr 7 2010; 98 (7): 1344-1352.

Pagano N, Wong EY, Breiding T, Liu H, Wilbuer A, Bregman H, Shen Q, Diamond SL, Meggers E. From imide to lactam metallo-pyridocarbazoles: distinct scaffolds for the design of selective protein kinase inhibitors. J Org Chem Dec 4 2009; 74 (23): 8997-9009.

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 Mar 18 2005; 44 (13): 1984-1987.

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 May 2005; 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 May 18 2005; 127 (19): 6948-6949.

Radivoyevitch T, Kashlan OB, Cooperman BS. Rational polynomial representation of ribonucleotide reductase activity. BMC Biochem 2005; 6 8.

Ma H, Horiuchi KY, Wang Y, Kucharewicz SA, Diamond SL. Nanoliter homogenous ultra-high throughput screening microarray for lead discoveries and IC50 profiling. Assay Drug Dev Technol Apr 2005; 3 (2): 177-187.

Gosalia DN, Salisbury CM, Maly DJ, Ellman JA, Diamond SL. Profiling serine protease substrate specificity with solution phase fluorogenic peptide microarrays. Proteomics Apr 2005; 5 (5): 1292-1298.

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 May 2005; 4 (5): 626-636.

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.

Zhang L, Carroll P, Meggers E. Ruthenium complexes as protein kinase inhibitors. Org Lett Feb 19 2004; 6 (4): 521-523.

Smith AB, 3rd, Adams CM, Barbosa SA, Degnan AP. A unified approach to the tedanolides: total synthesis of (+)-13-deoxytedanolide. Proc Natl Acad Sci U S A Aug 17 2004; 101 (33): 12042-12047.

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 Apr 6 2004; 101 (14): 5036-5041.

Lo K, Diamond SL. Blood coagulation kinetics: high throughput method for real-time reaction monitoring. Thromb Haemost Oct 2004; 92 (4): 874-882.

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): 1473-1484.

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 Apr 5 2004; 14 (7): 1651-1654.

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 Jun 2004; 93 (6): 1537-1544.

Bregman H, Williams DS, Atilla GE, Carroll PJ, Meggers E. An organometallic inhibitor for glycogen synthase kinase 3. J Am Chem Soc Oct 27 2004; 126 (42): 13594-13595.

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 Nov 26 2003; 125 (47): 14435-14445.

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-ben zazepine (SB-414796): a potent and selective dopamine D3 receptor antagonist. J Med Chem Nov 6 2003; 46 (23): 4952-4964.

Gosalia DN, Diamond SL. Printing chemical libraries on microarrays for fluid phase nanoliter reactions. Proc Natl Acad Sci U S A Jul 22 2003; 100 (15): 8721-8726.

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 Aug 2003; 8 (4): 453-462.

Gao Y, Liehr S, Cooperman BS. Affinity-driven selection of tripeptide inhibitors of ribonucleotide reductase. Bioorg Med Chem Lett Feb 25 2002; 12 (4): 513-515.

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 Jun 26 1992; 35 (13): 2347-2354.