5/4/13 Matt Nguyen won second prize during the undergraduate poster session. Congratulations!

3/5/13 Prof. Santos presents an invited lecture at the 14th Annual Florida Heterocyclic and Synthetic Chemistry Conference.

2/6/13 Wenyu and Jessica's paper about discovering a novel binding mode toward HIV-1 RNA is accepted in Chemical Communications. Congratulations!

1/5/13 We welcome two new graduate students in the lab. Cheryl Peck comes from Longwood College and Beth Childress is a graduate of the College of William and Mary.

1/1/13 Two publications from the Santos group are highlighted in Chemistry Portal. Joe's silylation protocol and Brandon's borylation protocol.

8/27/12 Dr. Mithun Raje secures a postdoctoral position with Prof. Takashi Tsukamoto at Johns Hopkins. Good luck!

8/21/12 Prof. Santos presents at the Young Investigator Symposium at the ACS conference in Philadelphia.

8/21/12 Joe Calderone gives a talk about his beta silylation protocol at the ACS conference in Philadelphia.

7/31/12 Congratulations to Dr. Jason Crumpton. He will start as an assistant professor of chemistry at Lynchburg College. Well done!

7/17/12 Joe's paper on aqueous silylation is highlighted in Synfacts (2012, 8, 781). Congrats Joe!

7/10/12 Mithun's paper describing selective sphingosine kinase 2 inhibitor SLR080811's role in lowering S1P level in mice is published in Biochemical Journal. Great Job!

7/7/12 The Virginia Tech Center for Drug Discovery is official! Click here for more info.

7/1/12 Dr. Mithun Raje started as a postdoc in the Carlier group while Dr. Brandon Thorpe assumed principal scientist role at SphynKx Therapeutics. Good luck to both of you!

6/1/12 Best of luck to Dr. David Bryson who joins Prof. David Liu as a postdoc fellow at Harvard University.

5/30/12 We welcome James Gumkowski as a Fralin Summer Undergrad Research Fellow. He comes to us from Muhlenberg College.

5/20/12 Analyn Carreon, a visiting scholar from the Philippines, has arrived!

4/30/12 Congratulations to Julie Ta for winning 1st place in the undergraduate research poster session.

4/23/12 The reagent developed in our lab, PDIPA diboron, is now in the "electronic Encyclopedia of Reagents for Organic Synthesis (eROS)". The article is contributed by Brandon Thorpe.

 

 

 

 

 

 


Publications

2013

32• Zhang, W.; Bryson, D.I.; Crumpton, J.B.; Wynn, J. and Santos, W. L. A Cell Permeable Branched Peptide Boronic Acid that Selectively Binds to HIV-1 RRE RNA. 2013, submitted.

 

31• Daengngam, C.; Thorpe, S.; Guo, X.; Stoianov, S.; Santos, W. L.; Morris, J.; Robinson, H. High Photoreactiviety of O-Nitrobenzyl Ligands on Gold. 2013, submitted.

 

30• Zhang, W.; Bryson, D.I.; Crumpton, J.B.; Wynn, J. and Santos, W. L. Branched Peptide Boronic Acids (BPBAs): A Novel Mode of Binding Towards RNA. Chem. Commun. 2013, 49, 2436-2438. DOI: 10.1039/C3CC00243H.

2012

29• Kharel, Y.; Raje, M.; Gao, M.; Gellett, A.M.; Tomsig, J.L.; Lynch, K.R. and Santos, W.L. Sphingosine kinase type 2 inhibition elevates circulating sphingosine-1-phosphate. Biochem. J. 2012, 447, 149-157. doi:10.1042/BJ20120609

28• Thorpe, S.B. and Santos, W.L. 4,8-Dimethyl-2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1,3,6,2-dioxazaborocane, 2012, Encyclopedia of Reagents for Organic Synthesis [Online], John Wiley & Sons, Ltd. DOI: 10.1002/047084289X.rn01517

27• Calderone, J.A. and Santos, W.L. Copper(II)-Catalyzed Silyl Conjugate Addition to α,β-Unsaturated Conjugated Compounds: Brønsted Base-Assisted Activation of Si–B Bond in Water. Org. Lett. 2012, 14, 2090-2093. DOI: 10.1021/ol300618j

This article was recently highlighted in

Synfacts, 2012, 8, 781.

ChemInform, 2012, 43, no. doi: 10.1002/chin.201231192

Organic Chemistry Portal

26•Gude, L.; Berkovitch, S.S.; Santos, W.L.; Kutchukian, P.S.; Pawloski, A.R.; Kuimelis, R.; McGall, G. and Verdine, G.L. Mapping targetable sites on the human telomerase RNA pseudoknot/template domain using 2'-OMe RIPtide microarrays. J. Biol. Chem. 2012, 287, 18843-18853. click here.

25• Thorpe, S.B.; Calderone, J.A. and Santos, W.L. Unexpected copper (II) catalysis:  Catalytic amine base promoted β-borylation of α,β-unsaturated carbonyl compounds in water. Org. Lett. 2012, 14, 1918-1921. DOI: 10.1021/ol300575d.

This article was recently highlighted in ChemInform, 2012, 43, no. doi: 10.1002/chin.201231192

Chemistry Portal

24• Knott, K.; Kharel, Y.; Raje, M.R.; Lynch, K.R. and Santos, W.L. Effect of alkyl chain length on sphingosine kinase 2 selectivity. Bioorg. Med. Chem. Lett. 2012, 22, 6817-6820. DOI: 10.1016/j.bmcl.2012.01.050.

23• Crumpton, J.B. and Santos, W.L. Site-specific incorporation of diamondoids on DNA using click chemistry. Chem. Commun. 2012, 48, 2018 - 2020. DOI:10.1039/C2CC16860J.

22• Raje, M.R.; Knott, K.; Kharel, Y.; Bissel, P.; Lynch, K.R. and Santos, W.L. Design, synthesis and biological activity of sphingosine kinase 2 selective inhibitors. Bioorg. Med. Chem. 2012, 20, 183-194. DOI:10.1016/j.bmc.2011.11.011.

21• Bryson, D.R.; Zhang, W.; McLendon, P.M.; Reineke, T.M. and Santos, W.L. Toward Targeting RNA Structure:  Branched Peptides as Cell-Permeable Ligands to TAR RNA. ACS Chem. Biol. 2012, 7, 210–217. DOI: 10.1021/cb200181v.

2011

20• Gao, M.; Thorpe, S.B.; Kleeberg, C.; Slebodnick, C.; Marder, T.B. and Santos, W.L. Structure and reactivity of a preactivated sp2-sp3 diboron reagent: Catalytic regioselective boration of alph, beta-unsaturated conjugated compounds. J. Org. Chem. 2011, 76, 3997–4007. DOI: 10.1021/jo2003488.

This article was recently highlighted in:

Synfacts, 2011, 9, 995

ChemInform, 2011, 42, no. doi: 10.1002/chin.201133182

19• Sun, J.; Perfetti, M.T. and Santos, W.L. A method for the deprotection of alkylpinacolyl boronate esters. J. Org. Chem. 2011, 76, 3571–3575. DOI: 10.1021/jo200250y.

18• Crumpton, J.B.; Zhang, W. and Santos, W.L. Facile analysis and sequencing of linear and branched peptide boronic acids by MALDI Mass Spectrometry. Anal. Chem. 2011, 83, 3548–3554. DOI: 10.1021/ac2002565.

17• Thorpe, S.B.; Guo, Xi and Santos, W.L. Regio- and stereoselective copper-catalyzed b-borylation of allenoates by a preactivated diboron. Chem. Commun. 2011, 47, 424-426. [pdf version]

This paper is part of an "Emerging Investigator Issue".

2010

16• Knott, K.; Fishovitz, J; Thorpe, S.B., Lee, I and Santos, W.L. N-terminal peptidic boronic acids selectively inhibit human ClpXP. Org. Biomol. Chem. 2010, 8, 3451. [pdf version]

This paper is part of an Organic & Biomolecular Chemistry web theme issue on chemical biology.

N-terminal Boronic Acids

 

2009

15• Gao, M.; Thorpe, S.B. and Santos, W.L. Sp2-Sp3 Hybridized Mixed Diboron: Synthesis, Characterization and Copper-Catalyzed β-Boration of α, β-Unsaturated Conjugated Compounds. Org. Lett. 2009, 11, 3478-3481. [pdf version]

Mixed Diboron

14• Bryson, D.I.; Zhang, W. and Santos, W.L. Screening of a Branched Peptide Library with HIV-1 TAR RNA. Mol. BioSyst. 2009, 5, 1070-1073. [pdf version]

This paper is part of an "Emerging Investigator Issue". For biography of the contributors, click here.

.......RNA Targeting

 

2008

13• Komazin-Meredith, G.; Petrella, R.; Santos, W.L.,Filman, D.J.; Hogle, J.M.; Verdine, G.L.; Karplus, M. and Coen, D.M. The Human Cytomegalovirus UL44 C Clamp Wraps around DNA. Structure 2008, 16, 1214-1226. [pdf version]

12• Komazin-Meredith, G.; Santos, W.L., Filman, D.J.; Hogle, J.M.; Verdine, G.L. and Coen, D.M. The positively charged surface of herpes simplex virus UL42 mediates DNA binding. J. Biol. Chem. 2008; doi:10.1074/jbc.M708691200. [pdf version]

11• Zhao, Z.; McKee, C.J.; Kessl, J.J.; Santos, W.L.; Daigle, J.E.; Engelman, A.; Verdine, G. and Kvaratshelia, M. Subunit specific protein footprinting reveals significant structural rearrangements and a role for N-terminal LYS-14 of HIV-1 integrase during viral DNA binding. J. Biol. Chem. 2008; doi:10.1074/jbc.M705241200. [pdf version]

2006

10• Banerjee, A.; Santos, W.L. and Verdine, G.L. Disulfide trapping and structural characterization of an early intermediate in the pathway of damage search by MutM. Science , 2006 , 311 , 1153. [pdf version]

see the following highlight on NSLS [pdf version]

9• Johnson, A.A.; Santos, W.L.; Marchand, C.; Amin, R.; Verdine, G.L. and Pommier, Y. Interaction between HIV-1 integrase Q148 and a viral DNA cytosine is required for strand transfer. J. Biol. Chem. 2006 , 281 , 461. [pdf version]

2004

8• Santos, W.L.; Heasely, B.H.; Jarosz, R.; Carter, K.M.; Lynch, K.R. and Macdonald, T.L. Synthesis and biological evaluation of phosphonic and thiophosphoric acid derivatives of lysophosphatidic acid. Bioorg. Med. Chem. Lett. 2004 , 14 , 3473. [pdf version]

2002

7• Kapetanovic, I.M.; Torchin, C.D.; Strong, J.M.; Yonekawa, W.D.; Lu, C.; Li, A.P.; Dieckhaus, C.M.; Santos, W.L .; Macdonald, T.L.; Sofia, R.D. and Kupferberg, H.J. Reactivity of atropaldehyde, a felbamate metabolite in human liver tissue in vitro. Chem. Biol. Interact. 2002 , 142 , 119-34. [pdf version]

6• Roller, S. G.; Dieckhaus, C. M.; Santos , W. L .; Duane Sofia, R. and Macdonald, T. L. Oxidation of 3-carbomoyl-2-phenylpropionaldehyde, a felbamate metabolite, by aldehyde dehydrogenase 1: significance in detoxification of felbamate. Chem. Res. Toxicol. 2002 , 15 , 815-24. [pdf version]

2001

5• Dieckhaus, C. M.; Roller, S.; Santos , W. L . and Macdonald, T. L. The role of glutathione s-transferases a1-1, p1-1 and m1-1 in the detoxification of 2-phenylpropenal, a reactive felbamate metabolite. Chem. Res. Toxicol. 2001 , 14 , 511-516. [pdf version]

4• Dieckhaus, C. M.; Santos , W. L . and Macdonald, T. L. The chemistry and toxicology of 4-hydroxy-5-phenyl-1,3-oxazaperhydroin-2-one: a reactive metabolite in felbamate bioactivation. Chem. Res. Toxicol. 2001, 14, 958-964. [pdf version]

3• Hooks, S. B.; Santos, W. L. ; Im, D-S., Heise, C. H.; Macdonald, T. L. and Lynch, K. R. Lysophosphatidic acid induced mitogenesis is regulated by lipid phosphate phosphatases and is Edg-receptor independent. J. Biol. Chem. 2001, 276 , 4611-4621. [pdf version]

2• Heise, C. E.; Santos, W. L .; Schreihofer, A. M.; Heasley, B. H.; Mukhin, Y. V.; Macdonald, T. L. and Lynch, K. R. Activity of 2-substituted lysophosphatidic acid (LPA) analogs at LPA receptors: discovery of a LPA 1 /LPA 3 receptor antagonist. Mol. Pharm. 2001 , 60 , 1173-1180. This work was highlighted in Mol. Pharm . 2001 , 60 , 1161-1164. [pdf version]

2000

1• Santos , W. L .; Rossi, J. R.; Boggs, S. D. and Macdonald, T. L. The molecular pharmacology of lysophosphatidate signaling. Ann. N. Y. Acad. Sci. 2000 , 905 , 232-242. [pdf version]

 

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