5/24/18 Congrats to Laura Wonilowitz! She recieved the Biochemistry Department's 2018 Thomas O. Sitz Scholarship.

05/14/18 We welcome Justin Grams to the Santos group!

04/27/18 Three awards for the Santos group: Outstanding research (Russell Fritzemier), Graduate teacher (Ashley Gates), Undergrad research fellowship (Greg Traversa)

03/29/18 Congrats to Jose and Jacob for passing their prelims with flying colors!

01/01/18 We welcome 4 new first years to the group:

Jonathan Bowen (Wake Forest), Chris Garcia (Cal State), Daniel Foster (Purdue)& Connor Szwetkowski (Rider)

11/29/17 Beth's review on mitochondrial uncouplers is accepted in J. Med. Chem. Great job!

11/14/17 Congrats to the boss! His endowed A.C. Lilly Faculty fellowship is renewed.

9/13/17 We welcome postdoc Joe Salamoun! He comes from the Wipf group at Pitt.

9/11/17 Russell's trans silaboration of triple bonds is published in Chem. Eur. J. Fantastic work!

7/20/17 Our collaboration with the Ratajczak Lab has provided a role for Sphingosine kinase inhibitors in the egress of stem cells--oncogene.

7/12/17 Jessica's paper in using branched peptides as antimicrobials is accepted in ACS Med. Chem. Lett. Awesome job!

7/1/17 Congrats to Ashley Peralta for winning an ACS BIOL travel award.

6/22/17 Kuddos to Dr. Childress for successfully defending her dissertation. She is off to the Lindsley Lab at Vanderbilt University.

5/1/17 Congrats to Beth Childress for winning the dept of chemistry graduate research award!

4/14/17 Beth Childress's work on developing sphingosine kinase inhibitors is accepted in J. Med. Chem. Congrats!

4/5/17 Our twins (Eric Medici & Chris Sibley) passed their prelims. Woohoo!

3/14/17 Laura Wonilowicz was selected as an Amgen Scholar in UC Berkeley's Summer Research Program. Best of luck Laura!

3/6/17 Russell Fritzemeier and Ashley Gates passed their prelims. Well done!

3/2/17 Astha and Russell's work on transition metal-free diboration is published in Angew. Chemie. Congrats!

12/12/16 Congrats to the Santos lab! A seed grant to study sphingosine kinase inhibitors and multiple sclerosis was recently funded.

11/15/16 Congrats to Beth Childress for winning a student travel award from the lipids conference at SERCL.

11/9/16 Congratulations to Ashley Peralta and Yumin Dai for winning best poster at the VT Center for Drug Discovery Poster session.

10/27/16 Our latest PhD from the Santos Lab: Dr. Amanda Nelson. Congrats!!!

9/1/16 Jessica accepted a position at Merck Inc.

8/23/16 Molly Congdon accepted a postdoc position at NIH/NCI with Jeff Gildersleeve. Good luck!

8/19/16 Congrats to Cheryl Peck for receiving a College of Science Doctoral assistantship award!

8/19/16 Dr. Srinath Pashikanti moves to Idaho State University as an assistant professor. Best of luck Sri!

8/17/16 Cheryl's paper is highlighted in organic chemistry portal.

8/17/16 Thanks to NIH/NIGMS for funding our RO1 grant! Cheers to the Santos lab.

8/16/16 Our expert opinion on sphingosine kinase therapeutics is accepted for publication.

7/19/2016 Molly successfully defended her Ph.D. Congrats Dr. Congdon!!!

7/15/2016 Congratulations to Dr. Jessica Wynn for passing her Ph.D. defense with flying colors!

6/2/2016 Jessica's paper on inhibiting HIV-1 replication in cells is accepted in MedChemComm. Fantastic work Jess!

5/25/2016 Astha's chapter on copper-catalyzed organoboron cross-coupling has been accepted. Great job, Astha!

5/3/2016 Congrats to Sri, Joe, Chris, and Matt. Their hydrosilylation of allenes work in water is accepted by Org. Lett.

4/23/2016 Molly received a travel award from the ACS Med Chem division to attend the ACS meeting in Philly this fall. Awesome Molly!

4/22/2016 Amanda and Cheryl's borylation of alkynoates and alkynamides in water is accepted in JOC. Great job to both!

4/22/2016 Congrats to Molly Congdon for winning an outstanding graduate research award!

4/5/16 Undergrad Laura Wonilowicz won a Fralin Summer Fellowship to work in our lab this summer. Well done Laura!

4/4/16 Jessica's paper regarding branched peptide boronic acids is accepted at Bioorganic and Medicinal Chemistry. Great Job!

3/22/16 Beth Childress was selected for a prestigious P.E.O. Scholar Award. Congrats and well done!

3/14/16 Congratulations to Molly! Her sphingosine kinase work is featured on the front cover of ACS. Med. Chem. Lett.

3/1/16 Dr. Astha Verma leaves the lab for a job at KBI Biopharma. Best of luck!

2/15/16 We welcome two first year students: Chris Sibley and Eric Medici.

2/3/16 Molly's naphthalene-based Sphingosine Kinase inhibitors is available online at ACS Med. Chem. Lett. Congrats Molly!

12/7/15 Beth Childress won a CCG Research Excellence Student Travel Award from the Division of Medicinal Chemistry-ACS. Congrats!

11/6/15 Congratulations to Beth Childress and Jessica Wynn for winning awards during VT's Center for Drug Discovery Poster Session!

10/01/15 Prof. Santos is now a fellow of the Institute for Creativity, Arts, and Technology (ICAT).

8/26/15 Congrats to Beth Childress for receiving a College of Science Doctoral assistantship award!

8/4/15 Congrats to Emily, Molly, and team sphingosine kinase for their hard work. The in vivo effects of inhibitors is published in JPET.

7/24/15 Emily Morris recently accepted a teaching position at Manassas Park High School. Woohoo!

7/15/15 Alumni Matthew Nguyen will be attending VCU Medical School this fall. Congrats Matt!

7/1/15 Thanks to ARDRAF for funding our work with sphingosine kinase and Alzheimer's Disease.

6/22/15 Jessica Wynn receives a travel award from the BIOL division of the ACS. Great job!

6/11/15 Joe Calderone's paper dealing with mitochondrial uncouplers for the treatment of diabetes is accepted in BMCL. Congrats!

6/11/15 Fulbright scholar, Amanda Nelson, is highlighed in VT news!

4/28/15 Jessica's review of branched peptide is published in Org. Biomol. Chem. Congrats!

4/25/15 Congratulations to Amanda Nelson for receiving a Fulbright Scholarship! She will be spending a year in Germany with Todd Marder.

3/16/15 Congratulations to Molly on her work with the SAR of sphingosine kinases, which is published in Bioorg. Med. Chem. Lett.!

3/12/15 Cheryl's paper on aqueous borylation of alkynoates is published in Synthesis. Congrats!

3/03/15 Xi and Amanda's paper regarding unsymmetrical diboration is published in ACS Catalysis. Well done!

2/04/15 Neeraj and Emily's selective inhibitors of SphKs is published in J. Med. Chem. Congrats!

1/08/15 Congratulations to Jessica Wynn for receiving a graduate school doctoral assistantship award.

11/20/14 Our review of sphingosine kinases appears in ACS Chemical Biology.

11/6/14 Congratulations to Dr. Xi Guo for passing her dissertation defense. Fantastic job!

10/15/14 Dr. Santos is a recipient of Fralin/ICTAS Innovator's Award from Virginia Tech.

9/30/14 Dr. Santos is named as Cliff and Agnes Faculty Fellow.

8/25/14 Dr. Santos presents at IME Boron Conference in Prague, Czech Republic.

7/16/14 Joe Calderone's Angewandte paper is highlighted in SynFacts. Great job Joe!

6/25/14 Ashley Peralta joins the Santos group.

6/20/14 Jessica Wynn won second prize oral presentation at BORAM XIV, an international meeting of boron chemists. Congrats!

5/17/14 Congratulations to our recent graduates. Dr. Wenyu Zhang will be a postdoc at NIH with Dr. Kuan Wang. Matt Nguyen will be a postbac researcher with Dr. Sidransky at NIH.

4/25/14 Congratulations to the Santos Lab. Award winners from the Chemistry Dept:

Outstanding graduate research: Wenyu Zhang

Outstanding Graduate Teaching Assistant: Molly Congdon

Second Place Poster Winner: Matthew Nguyen

Summer Research: Sean Rafferty

Schug Research Award: Webster Santos













71. Dai, Y.; Peralta, A.N.; Wynn, J.E.; Chringma, S.; Jayaraman, B.; Li, H.; Verma, A.; Frankel, A.D.; Le Grice, S.F.; Santos, W.L. Inhibition of HIV-1 Rev-RRE RNA Interaction via Unnatural Branched Peptides. 2018, submitted.


70. Fritzemeier, R.; Gates, A.; Guo, X.; Lin, Z.; Santos, W.L. Transition metal-free trans hydroboration of alkynoic acid derivatives: Experimental and theoretical studies. 2018, submitted.


69. Hemming, D.; Fritzemeier, R.; Wescott, S.A.; Santos, W.L.; Steel, P.G. Copper-Boryl Mediated Organic Synthesis. 2018, submitted.


68. Kharel, H.; Agah, S.; Mendelson, A.J.; Eletu, O.T.; Gesualdi, J.; Smith, J.S.; Santos, W.L.; Lynch, K.R. Saccharomyces cerevisiae as a Platform for Assessing Sphingolipid Lipid Kinase Inhibitors. PLoS ONE 2018, 13, e0192179. https://doi.org/10.1371/journal.pone.0192179


67. Childress, E. S.; Alexopoulos, S. J.; Hoehn, K. L.; Santos, W. L. Small Molecule Mitochondrial Uncouplers and Their Therapeutic Potential. J. Med. Chem. 2018, in press. DOI: 10.1021/acs.jmedchem.7b01182


66. Fritzemeier. R.; Santos, W.L. Brønsted Base Catalyzed Regio- and Stereoselective trans Silaboration of Propargylamides: Access to 1,2-Vinylborasilanes. Chem. Eur. J. 2017, 23, 15534-15537. http://dx.doi.org/10.1002/chem.201703774

65. Adamiak, M; Chelvarajan, L.; Lynch, K.R.; Santos, W.L.; Abdel-Latif, A. and Ratajczak, M. Mobilization studies in mice deficient in sphingosine kinase 2 support a crucial role of the plasma level of sphingosine-1-phosphate in the egress of hematopoietic stem progenitor cells. Oncogene 2017,8, 65588-65600. https://doi.org/10.18632/oncotarget.19514

64. Magill, B.; Guo, X.; Peck, C.; Reyes, R.; See, E.; Santos, W.L.; Robinson, H. Multi-photon patterning of photoactive o-nitrobenzyl ligands bound to gold surfaces. ACS Applied Materials & Interfaces, 2017, under revision.

63. See, E.M.; Peck, C.L.; Santos, W.L.; Robinson, H.D. Light-Directed Patchy Particle Fabrication and Assembly from Isotropic Silver Nanoparticles. Langmuir, 2017, 33, 10927–10935. DOI: 10.1021/acs.langmuir.7b02307

62. Wynn, J.E.; Zhang, W.; Falkinham, J.; Santos, W.L. Branched peptides: acridine and boronic acid derivatives as antimicrobial agents. ACS Med. Chem. Lett. 2017, 8, 820–823. DOI:http://dx.doi.org/10.1021/acsmedchemlett.7b00119 .

61. Childress, E.; Kharel, Y.; Brown, A.; Bevan, D.R.; Lynch, K.R.; Santos, W.L. Transforming Sphingosine Kinase 1 Inhibitors into Dual and Sphingosine Kinase 2 Selective Inhibitors: Design, Synthesis, and In Vivo Activity. J. Med. Chem. 2017, 60, 3933-3957. doi: 10.1021/acs.jmedchem.7b00233.

Access the recommendation on F1000Prime

60. See, E.; Peck, C.; Guo, X.; Santos, W.L.; Robinson, H. Plasmon-Induced Photoreaction of ortho-Nitrobenzyl Based Ligands Under 550nm Light. J. Phys. Chem. 2017, 121, 13114–13124. DOI: 10.1021/acs.jpcc.7b00707

59. Verma, A.; Snead, R.F.; Dai, Y.; Slebodnick, C.; Yang, Y.; Yu, H.; Yao, F.; Santos, W.L. Substrate-assisted, Transition Metal-free Diboration of Alkynamides with Mixed Diboron: Regio- and Stereoselective Access to trans 1,2-Vinyldiboronates. Angew. Chem. Int. Ed. 2017, 56, 5111-5115. DOI: 10.1002/anie.201700946

This article was recently highlighted in Synfacts, 2017, 13, 0644.


58. Valenciano, A.; Ramsey, A.C.; Santos, W.L.; Mackey, Z.B. Discovery and antiparasitic activity of AZ960 as a Trypanosoma brucei ERK8 inhibitor, Bioorg. Med. Chem. Lett. 2016, 24, 4647-4651. DOI: 10.1016/j.bmc.2016.07.069

57. Verma, A.; Santos, W.L. Copper-Catalyzed Coupling Reactions of Organoboron Compounds. Boron Reagents in Synthesis, 2016, 313-356. DOI:10.1021/bk-2016-1236.ch010


56. Wynn, J.E.; Zhang, W.; Tebit, D.M.; Gray, L.R.; hammarskjold, M-L.; Rekosh, D.R. and Santos, W.L. Synergistic Effect of Intercalator and Lewis Acid-base Branched Peptide Complexes: Boosting Affinity Towards HIV-1 RRE RNA, MedChemComm, 2016, 7, 1436-1440. DOI: 10.1039/C6MD00171H .

55. Pashikanti, S.; Calderone, J.A.; Nguyen, M.K.; Sibley, C.D.; Santos, W.L. Regio- and Stereoselective Copper(II)-Catalyzed Hydrosilylation of Activated Allenes in Water: A Convenient Access to Vinylsilanes. Org. Lett. 2016, 18, 2443-2446. DOI:10.1021/acs.orglett.6b00981.

This article was recently highlighted in Synfacts, 2016, 12, 836.

54. Lynch, K.R.; Thorpe, S.B.; Santos, W.L. Sphingosine kinase inhibitors: a patent review (2005-2015). Exp. Op. Ther. Pat. 2016, 26, 1409-1416. DOI: dx.doi.org/10.1080/13543776.2016.1226282.


53. Nelson, A.K.; Peck, C.L.; Rafferty, S.M.; Santos, W.L. Chemo-, Regio-, and Stereoselective Copper(II)-Catalyzed Boron Addition to Acetylenic Esters and Amides in Aqueous Medium. J. Org. Chem. 2016, 81, 4269-4279. DOI: 10.1021/acs.joc.6b00648.

52. McDaniels, J.M.; Carter, S.A.; Congdon, M.; Santos, W.L.; Phillips, M.A.; Rathod, P.K.; Guler, J. A. The Generation of Extra-chromosomal DNA Amplicons in Antimalarial Resistant Plasmodium falciparum, 2016, submitted.



51. Wynn, J.E.; Zhang, W.; Tebit, D.M.; Gray, L.R.; Hammarskjold, M-L.; Rekosh, D.R. and Santos, W.L. Characterization and in vitro activity of a branched peptide boronic acid that interacts with HIV-1 RRE RNA, Bioorg. Med. Chem. 2016, 24, 3947-3952. http://dx.doi.org/10.1016/j.bmc.2016.04.009

50. Congdon, M.; Kharel, Y.; Brown, A.; Lewis, S.L.; Bevan, D.R.; Lynch, K.R. and Santos, W.L. Structure-activity relationship studies and molecular modeling of naphthalene-based sphingosine kinase 2 inhibitors. ACS Med. Chem. Lett. 2016, 7, 229-234. DOI: 10.1021/acsmedchemlett.5b00304.

This work is featured on the journal front cover.

49. Babahosseini, H.; Srinivasarahavan, V.; Zhao, Z.; Gillam, F.; Childress, E.; Strobl, J.; Santos, W.L.; Zhang, C.; Agah, M. The Impact of Sphingosine Kinase Inhibitor-Loaded Nanoparticles on Bioelectrical and Biomechanical Properties of Cancer Cells, Lab on a Chip, 2016, 16, 23-31. doi: 10.1039/c5lc01201e


48. Kharel, Y.; Morris, E.A.; Congdon, M.; Thorpe, S.B.; Tomsig, J.L.; Santos, W.L. and Lynch, K.R. Sphingosine Kinase Type 2 and Blood S1P. J. Pharm. Exp. Ther. 2015, 355, 23–31. DOI: 10.1124/jpet.115.225862

This article was recently highlighted in J. Pharm. Exp. Ther. 2015, 355, 1.

47. Kenwood, B.M.; Calderone, J.A.; Taddeo, E.P.; Hoehn, K.L. and Santos, W.L. Structure-activity relationships of furazano[3,4-b]pyrazines as mitochondrial uncouplers. Bioorg. Med. Chem. Lett. 2015, 25, 4858-4861. DOI: 10.1016/j.bmcl.2015.06.040. Invited contribution by Prof. Dale Boger, 25th anniversary symposium-in-print.

46. Wynn, J. and Santos, W.L. HIV-1 Drug Discovery: Targeting Folded RNA Structures With Branched Peptides. Org. Biomol. Chem., 2015, 13, 5848-5858. DOI: 10.1039/C5OB00589B.

This article was recently highlighted in ChemInform, 2015,46, 29. DOI: 10.1002/chin.201529310.

45. Peck, C.L.; Calderone, J.A. and Santos, W.L. Copper(II)-catalyzed β-Borylation of Acetylenic Esters in Water. Synthesis, 2015, 47, 2242-2248. DOI: 10.1055/s-0034-1380524. Invited contribution on conjugate addition themed edition by Prof. Erick Carreira.

Highlighted in organic chemistry portal.

This article was recently highlighted in ChemInform, 2015,46, 50.DOI: 10.1002/chin.201550171.

44. Congdon, M.D.; Childress, E.S.; Patwardhan, N.N.; Gumkowski, J.; Morris, E.A.; Kharel, Y.; Lynch, K.R. and Santos, W.L. Structure-activity relationship studies of the lipophilic tail region of sphingosine kinase 2 inhibitors,Bioorg. Med. Chem. Lett., 2015, 25, 4956-4960. DOI:10.1016/j.bmcl.2015.03.041. Invited contribution by Prof. Dale Boger, 25th anniversary symposium-in-print.

43. Guo, X.; Nelson, A.K.; Slebodnick, C. and Santos, W.L. Regio- and Chemoselective Diboration of Allenes with Unsymmetrical Diboron: Formation of Vinyl and Allyl Boronic Acid Derivatives, ACS Catal., 2015, 5, 2172−2176. DOI: 10.1021/acscatal.5b00387.

42. Patwardhan, N.N.; Morris, E.A.; Raje, M.R.; Gao, M.; Kharel, Y.; Tomsig, J.L.; Lynch, K.R. and Santos, W.L.  “Structure-Activity Relationship Studies and In Vivo Activity of Guanidine-based Sphingosine Kinase Inhibitors: Discovery of SphK 1 and 2 Selective Inhibitors.” J. Med. Chem. 2015,  58 , 1879–1899. DOI: 10.1021/jm501760d.

41. Santos, W.L. and Lynch, K.R. Drugging Sphingosine Kinases. ACS Chem. Biol. 2015, 10, 225-223. DOI: 10.1021/cb5008426



40. Ashry, A.; Kandas, I.; Wei, X.; Calderone, J.A.; Zhang, B.; Robinson, H.; Heflin, J.R.; Santos, W.L. and Xu, Y. The Impact of Lithography on the Fluorescence Dynamics of Self-Assembled Fluorophores,Opt. Express 2014, 22, 12935-12943. DOI:10.1364/OE.22.012935

39. Tang, X.; Benesch, M.G.K.; Dewald, J.; Patwardhan, N.; Santos, W.L.; McMullen, T.P.W. and Brindley, D.N. Expression of lipid phosphate phosphatase-1 in cancer cells attenuates lysophosphatidate signaling and tumor growth and metastasis in mice, 2014. J. Lipid Res, 2014,  55, 2389-2400. doi: 10.1194/jlr.M053462

38. Islam, A. Zhang, B.; Khalifa, M.B.; Calderone, J.A.; Santos, W.L.; Heflin, J.R.; Robinson, H. and Xu, Y. Fluorescence Lifetime Based Characterization of Active and Tunable Plasmonic Nanostructures,Optics Express. 2014, 22, 20720-20726. dx.doi.org/10.1364/OE.22.020720

37. Calderone, J.A. and Santos, W.L. Copper(II)-Catalyzed Silylation of Activated Alkynes in Water: Diastereodivergent Access to (E)- or (Z)-β-Silyl-α,β-Unsaturated Carbonyl and Carboxyl Compounds. Angew. Chem. Int. Ed. 2014, 53, 4154 –4158. DOI: 10.1002/anie.201310695

This article was recently highlighted in Synfacts, 2014, 10, 731.

This article was recently highlighted in ChemInform, 2014, 45, 38. DOI: 10.1002/chin.201438046.


36• Carreon, A.; Santos, W.L.; Matson, J.B. and So, R. Cationic Polythiophenes as Responsive DNA-Binding Polymers. Polymer Chemistry, 2014, 5, 314-317. DOI: C3PY01069D

35. Kenwood, B.M.; Weaver, J.L.; Bajwa, A.; Byrne, F.L.; Poon, I.V.; Murrow, B.A.; Calderone, J.A.; Huang, L.; Divakaruni, A.S.; Okabe, K.; Columbus, L.; Yan, Z.; Saucerman, J.J.; Smith, J.S.; Holmes, J.W.; Lynch, K.R.; Ravichandran, K.S.; Uchiyama, S.; Santos, W.L.; Rogers, G.W.; Okusa, M.D.; Bayliss, D.A. and Hoehn, K.L. Identification of a novel mitochondrial uncoupler with a broad effective range. Mol. Met. 2014, 3, 114-123. DOI: 10.1016/j.molmet.2013.11.005.

This article was highlighted in: Mol. Met, 2014, 3, 86.



34• Zhang, W.; Bryson, D.I.; Crumpton, J.B.; Wynn, J. and Santos, W. L. Targeting folded RNA: A branched peptide boronic acid that binds to large surface area of HIV-1 RRE RNA. Org. Biomol. Chem. 2013, 11, 6263-6271. DOI:10.1039/C3OB41053F

This work was featured on the front cover of the journal.


33• Daengngam, C.; Thorpe, S.; Guo, X.; Stoianov, S.; Santos, W. L.; Morris, J.; Robinson, H. High Photoreactivity of O-Nitrobenzyl Ligands on Gold. J. Phys. Chem. C, 2013, 117, 14165–14175. DOI: dx.doi.org/10.1021/jp4019102

32• 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.


31• 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

30• 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

29• 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

28•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.

27• 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

26• 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.

25• 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.

24• 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.

23• 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.


22• 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

21• 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.

20• 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.

19• 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".


18• 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



17• 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

16• 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



15• 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]

14• 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]

13• 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]


12• 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]

11• 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]


10. Paz, Y.E.; Santos, W.L. and Verdine, G.L.  Toward determination of the structural basis for HIV-1 integrase substrate recognition.  Nucleus 2005, 83, 12-14.


9• 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]


8. 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]

7. Okusa, M.D., Ye, H., Huang, L.P., Heise, C.E., Santos, W.L., Macdonald, T.L., Lynch, K.R.A dual lysophosphatidic acid (LPA) antagonist (LPA(1)/LPA(3)), VPC 12249, reduces renal ischemia-reperfusion injury (IRI). J. Am. Soc. Neph. 2002, 13, 140A.

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]


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]


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]