Publications

2024

 

135. Salamoun, J.M.; Krinos, E.L.; Fout, M.A.; Hargett, S.R.; Beretta, M.; Shrestha, R.; Hoehn, K.L.; Santos, W.L. Design, synthesis, and biological evaluation of imidazo[4,5-b]pyridine mitochondrial uncouplers for the treatment of metabolic dysfunction-associated steatohepatitis (MASH). 2024, under review.

134. Li, C.; Byrne, F.; Vancuylenburg, C.; Olzomer, E.; Hargreaves, A.; Santos, W.L.; Hoehn, K.L. Beneficial effects of MGL-3196 and BAM15 combination in a mouse model of fatty liver disease. Acta Physiol. 2024, accepted.

 

133. Cheng, Y.; Jones, J. P.; Yu, T. T.; Olzomer, E. M.; Su, J.; Katen, A.; Black, D. S.; Hart-Smith, G.; Childress, E. S.; Wilkins, M. R.; Santos, W. L.; Hoehn, K. L.; Byrne, F. L.; Kumar, N. Design, Synthesis and Biological Evaluation of Glucose Metabolism Inhibitors as Anticancer Agents. Bioorg. Chem. 2024, accepted.

 

132. Duse, D. A., Schröder, N. H., Srivastava, T., Benkhoff, M., Vogt, J., Nowak, M. K., Funk, F., Semleit, N., Wollnitzke, P., Erkens, R., Kötter, S., Meuth, S. G., Keul, P., Santos, W., Polzin, A., Kelm, M., Krüger, M., Schmitt, J., & Levkau, B. Deficiency of the sphingosine-1-phosphate (S1P) transporter Mfsd2b protects the heart against hypertension-induced cardiac remodeling by suppressing the L-type-Ca2+ channel. Basic Res. Cardiol. 2024, in press. https://doi.org/10.1007/s00395-024-01073-x

 

131. Grams, J.R.; Shrader, C.W.; Murray, J.H.; Rosenblum, C.A.; Slebodnick, C.; Santos, W.L. Regio- and Stereoselective Umpolung α-Addition of Tricyclohexylphosphine to Propiolamides, 2024, submitted.

 

130. Buchbinder, N.W.; Nguyen, L.H.; Beck, O.N.; Bage, A.D.; Slebodnick, C.; Santos, W.L. Chemo-, Regio- and Stereoselective cis-Hydroboration of 1,3-Enynes: Copper-catalyzed Access to (Z,Z)- and (Z,E)-2-Boryl-1,3-dienes. Org. Lett. 2024, 26, 6136–6141.  DOI: 10.1021/acs.orglett.4c01929

129. Kharel, Y.; Huang, T.; Dunnavant, K..; Foster, D.; Souza G. M. P. R.; Nimchuk, K. T.; Merchak, A. R.; Pavelec, C. M.; Gaultier, A.; Abbott, S. B. G.; Shin, J. B.; Xu, W.; Leitinger, N.; Santos, W. L.; Lynch, K. R. Assessing Spns2-Dependent S1P Transport as a Prospective Therapeutic Target Using a New Chemical Probe. Preprint. bioRxiv. 2024. doi.org/10.1101/2024.03.26.586765

 

 

128. Foster, D.; Dunnavant, K.; Shrader, C. W.; LoPresti, M. Q.; Seay, S.; Kharel, Y.; Huang, T.; Brown, A. M.; Lynch, K. R.; Santos, W. L. Discovery of Potent, Orally Bioavailable Sphingosine-1-Phosphate Transporter (Spns2) Inhibitor. J. Med. Chem. 2024, 67, 11273–11295. doi/10.1021/acs.jmedchem.4c00879

127. Li, W.; Ricker, R.; Chan, K.L.; Lau, P.F.; Buchbinder, N.W.; Krebs, J.; Friedrich, A.; Lin, Z.; Santos, W.L.; Radius, U.; Marder, T.B. Phosphine-catalyzed 1,2-cis-diboration of 1,3-butadiynes. Chem. Eur. J. 2024, e202401235. DOI:10.1002/chem.202401235

126. Chen, S-Y.; Telfser, A.; Olzomer, E.; Vancuylenberg, C.; Zhou, M.; Beretta, M.; Li, C.; Alexopoulos, S.; Turner, N.; Byrne, F.; Santos, W.L.; Hoehn, K.L. Beneficial effects of simultaneously targeting calorie intake and calorie efficiency in diet-induced obese mice. Clin. Sci. 2024, 138, 173-187. DOI:10.1042/CS20231016

125. Liu, S.; Ebel, E.R.; Luniewski, A.; Zulawinska, J.; Simpson, M.L.; Kim, J.; Ene, N.; Braukmann, T.W.A.; Congdon, M.; Santos, W.L.; Yeh, E.; Guler, J. L. Direct long read visualization reveals metabolic interplay between two antimalarial drug targets, 2024,  submitted, bioRxiv: 10.1101/2023.02.13.528367

124. Campbell, R.; Buchbinder, N.; Szwetkowski, C.; Zhu, Y.; Piedl, K.; Truong, M.; Matson, J.; Santos, W.L.; Mevers, E. Design, synthesis, and antifungal activity of 3-substituted-2(5H)-Oxaboroles, ACS Med. Chem. Lett. 2024, 15, 349–354. DOI: https://doi.org/10.1021/acsmedchemlett.3c00463

 

123. Grams, R.J.; Santos, W.L.; Scorei, I.R.; Abad-Garcia, A.; Bita, A.; Cerecettto, H.; Vinas, C.; Soriano-Ursua, M.A. The Rise of Boron-Containing Compounds: Advancements in Synthesis, Medicinal Chemistry and Emerging Pharmacology. Chem. Rev. 2024, 124, 2441–2511. DOI: 10.1021/acs.chemrev.3c00663

122. Chen, S-Y, Beretta, M; Olzomer, E.M.; Alexopoulos, S.J.; Shah, D.P.; Byrne, F.L.; Salamoun, J.M.; Garcia, C.J.; Smith, G.C.; Larance, M.; Philp, A.; Turner, N.; Santos, W.L.; Cantley, J.; Hoehn, K.L. Head-to-head comparison of BAM15, semaglutide, rosiglitazone, NEN, and calorie restriction on metabolic physiology in female db/db mice. Biochim. Biophys. Acta – Mol. Basis Dis. 2024, 1870, 166908. https://doi.org/10.1016/j.bbadis.2023.166908

2023

121. Beretta, M.; Dai, Y.; Olzomer, E.M.; Vancuylenburg,  C.S.; Santiago-Rivera, J.A.;  Philp, A.M.; Hargett, S.R.; Li, K.; Shah, D.P.; Chen, S-Y.; Alexopulos, S.J.; Harris, T.E.; Lee, B.; Walthier, M.; Cermak, J.M.; Tucker, S.P.; Turner, N.;  Bayliss, D.A.; Philp, A.; Byrne, F.L.; Santos, W.L.; Hoehn, K.L. Liver-selective imidazolopyrazine mitochondrial uncoupler SHD865 reverses adiposity and glucose intolerance in mice. Diabetes 2023, db230233. https://doi.org/10.2337/db23-0233

 

120. Shrader, C.W.; Foster, D.; Kharel, Y.; Huang, T.; Lynch, K.R.; Santos, W.L. Imidazole-Based Sphingosine-1-phosphate Transporter Spns2 Inhibitors. Bioorg. Med. Chem. Lett.  2023, 96, 129516. https://doi.org/10.1016/j.bmcl.2023.129516

119. Akram, M.O.; Vogels, C.M.; Santos, W.L.; Westcott, S.A.; Martin, C.D. Addition of a Phosphinoboronate Ester to Borole and Borafluorene. SynLett 2023, 34, 2193-2196.  DOI: 10.1055/a-2158-9726

 

118. Burgio, A.L.; Buchbinder, N.W.; Santos, W.L. Regio- and Stereoselective Copper-Catalyzed Borylation-Protodeboronation of 1,3-Diynes: Access to (Z)-1,3-Enynes. Org. Lett. 2023, 25, 2652–2656. https://pubs.acs.org/doi/full/10.1021/acs.orglett.3c00711

117. Li, H.; Ehnstrom, J.; Milton, M.; Santos, W.L.; Zell, M.; Dai, Y. Identification and Enrichment of a UV-induced Degradant of Anagrelide Drug Substance. J.  Pharm. Biomed. Anal. 2023, 229, 115352. https://doi.org/10.1016/j.jpba.2023.115352

116. Burgio, A.; Shrader, C.W.; Kharel, Y.; Huang, T.; Salamoun, J.; Lynch, K.R.; Santos, W.L. 2-Aminobenzoxazole Derivatives as Potent Inhibitors of the Sphingosine-1-phosphate Transporter Spinster Homolog 2 (Spns2). J. Med. Chem. 2023, 66, 5873–5891. https://doi.org/10.1021/acs.jmedchem.3c00149

115. Kharel, Y.; Huang, T.; Santos, W.L.; Lynch, K.R. Assays for the Sphingosine 1-phosphate Transporter Spinster Homolog 2 (Spns2). SLAS Disc. 2023, 28, 284-287.    https://doi.org/10.1016/j.slasd.2023.07.001

 

114. Murray, J.; Burgio, A.; Beretta, M.; Hargett, S.; Olzomer, E.; Grams, R.J.; Garcia, C.; Li, C.; Salamoun, J.; Hoehn, K.; Santos, W.L. Oxadiazolopyridine Derivatives as Efficacious Mitochondrial Uncouplers in the Prevention of Diet-Induced Obesity. J. Med. Chem. 2023, 66, 3876–3895. https://doi.org/10.1021/acs.jmedchem.2c01573

113.  Chen, S-Y.; Beretta, M.; Olzomer, E.M.; Wong, D.Y.; Alexopoulos, S.J.; Shah, D.P.; Aleksovska, I.; Salamoun, J.M.; Garcia, C.J.; Cochran, B.J.; Smith, G.C.; Byrne, F.L.; Morris, M.M.; Santos, W.L.; Cantley, J.; Hoehn, K.L. Targeting negative energy balance with calorie restriction and mitochondrial uncoupling in db/db mice. Mol. Metab. 2023, 69, 101684. https://doi.org/10.1016/j.molmet.2023.101684

 

2022

112. Dye, K.J.; Vogelaar, N.J.; O’Hara, M.; Sobrado, P.; Santos, W.L.; Carlier, P.R.; Yang, Z. Discovery of two inhibitors of the type IV pilus assembly ATPase as potential antivirulence compounds. Microbiol. Spectr. 2022, e0387722,  in press. DOI: 10.1128/spectrum.03877-22

111. Jos, S.; Tan, C.; Thilmany, P.; Saadane, A.; Evano, G.; Santos, W.L. Phosphine-Catalyzed Regio- and Stereo-selective Hydroboration of Ynamides to (Z)-β-borylenamides. Chem. Commun. 2022, 58, 13751-13754. DOI:https://pubs.rsc.org/en/content/articlelanding/2022/cc/d2cc04543e

110. Tanaka, S.; Zheng, S.; Kharel, Y.; Fritzemeier, R.G.; Huang, T.; Foster, D.; Poudel, N.; Goggins, E.; Yamaoka, Y.; Rudnicka, K.P.; Lipsey, J.E.; Radel, H.V.; Ryuh, S.M.; Inoue, T.; Yao, J.; Rosin, D.L.; Schwab, S.R.; Santos, W.L.; Lynch, K.R.; Okusa, M.D. S1P signaling in perivascular cells enhances inflammation and fibrosis in the kidney. Science Trans. Med. 2022, 14, eabj2681. https://doi.org/10.1126/scitranslmed.abj2681

• highlighted in a commentary: Idowu and Parikh, Sci. Transl. Med. 2022, 14, eadd2826.

109. Dai, Y.; Santiago-Rivera, J.A.; Hargett, S.; Salamoun, J.M.; Hoehn, K.L.; Santos, W.L.  Conversion of oxadiazolo[3,4-b]pyrazines to imidazo[4,5-b]pyrazine via a tandem reduction-cyclization sequence generates new mitochondrial uncouplers. Bioorg. Med. Chem. Lett. 2022, 73, 128912. doi.org/10.1016/j.bmcl.2022.128912

108. Jos, S.; Szwetkowski, C.; Slebodnick, C.; Ricker, R.; Chan, K.L.; Chan, W.C.; Radius, U.; Lin, Z.; Marder, T.B.; Santos, W.L. Transition Metal-Free Regio- and Stereo- Selective trans Hydroboration of 1,3-Diynes: A Phosphine Catalyzed Access to (E)-1-Boryl-1,3-Enynes. Chem. Eur. J. 2022, e202202349. DOI: 10.1002/chem.202202349

107.  Pashikanti, S.; Foster, D.; Kharel, Y.; Brown, A.; Bevan, D.; Lynch, K.R.; Santos, W.L. In Vivo Active Sphingosine Kinase 2 Inhibitors: Rigid Aliphatic Tail Derivatives Deliver Potent and Selective Analogs. ACS Bio. & Med. Chem. Au 2022, 2, 469-489. doi.org/10.1021/acsbiomedchemau.2c00017

106. Fritzemeier, R.; Foster, D.; Peralta, A.; Payette, M.; Kharel, Y.; Huang, T.; Lynch, K.R.; Santos, W.L. Discovery of in vivo active sphingosine-1-phosphate transporter (Spns2) inhibitors. J. Med. Chem. 2022, 65, 7656-7681. doi.org/10.1021/acs.jmedchem.1c02171

105. Bowen, J.; Slebodnick, C.; Santos, W.L. Phosphine-catalyzed Hydroboration of Propiolonitriles: Access to (E)-1,2-vinylcyanotrifluoroborate derivatives. Chem. Commun.  2022, 58, 5984 – 5987. doi.org/10.1039/D2CC00603K

104. Oyewole, O.; Dunnavant, K.; Bhattarai, S.; Kharel, Y.; Lynch, K.L.; Santos, W.L.; Reid, S.P. A Novel Sphingosine Kinase Inhibitor Suppresses Chikungunya Virus Infection. Viruses, 2022, 14, 1123. doi.org/10.3390/v14061123

 

103. Szwetkowski, C.; Slebodnick, C.; Santos, W.L. Regio- and stereoselective copper-catalyzed α,β-protoboration of allenoates: access to Z-β,γ-unsaturated β-boryl esters. Org. Biomol. Chem. 2022, 20, 3287-3291. DOI: 10.1039/D2OB00423B

102. Grams, R.J.; Lawal, M.M.; Szwetkowski, C.; Foster, D.; Rosenblum, C.A.; Slebodnick, C.; Welborn, V.V.; Santos, W.L. Organocatalytic trans Semireduction of Primary and Secondary Propiolamides: Substrate Scope and Mechanistic Studies. Adv. Syn. Cat. 2022, 364, 172-178. DOI 10.1002/adsc.202101020 

101. Gates, A.M.; Jos, S.; Santos, W.L. Ligand-free copper-catalyzed borylative defluorination: Access to gem-difluoroallyl boronic acid derivatives. Org. Biomol. Chem. 2022, 20, 366-374.  DOI: 10.1039/D1OB01533H.

selected as cover art:

2021

100. Bose, S.;* Mao, L.;* Kuehn, L.; Radius, U.;* Nekvinda, J.; Santos, W.L.;* Westcott, S.A.;* Steel, P.G.;* Marder, T.B.*  First-Row d-Block Element-Catalyzed Carbon-Boron Bond Formation and Related Processes. Chem. Rev. 2021, 121, 13238-13341. https://pubs.acs.org/doi/abs/10.1021/acs.chemrev.1c00255  * indicates corresponding author

99. Li, H.; Sibley, C.D.; Kharel, Y.; Huang, T.; Brown, A.M.; Wonilowicz, L.G.; Bevan, D.R.; Lynch, K.R.; Santos, W.L. Lipophilic Tail Modifications of (R)-Prolinol Scaffold Reveal Dual Sphingosine Kinase 1 and 2 Inhibitors. Bioorg. Med. Chem. 2021, 30, 115941. https://doi.org/10.1016/j.bmc.2020.115941

98. Murray, J.H.; Santos, W.L. Bis(1,1-dimethylethyl)[2′,4′,6′-tris-(1-methylethyl)[1,1′-biphenyl]-2-yl]-phosphine and Dicyclohexyl[2′,4′,6′-tris(1-methylethyl)[1,1′-biphenyl]-2-yl]phosphine (XPhos). e-EROS Encyclopedia of Reagents for Organic Synthesis, 2021, https://onlinelibrary.wiley.com/doi/10.1002/047084289X.rn00923.pub4.

97. Jos, S.; Santos, W.L. Copper-catalyzed Synthesis of α-Trifluoromethylacrylates from Trifluoroborylacrylates via Stereoretentive Radical Trifluoromethylation. Adv. Syn. Catal. 2021, 363, 425–430. VIP communication https://doi.org/10.1002/adsc.202000937

selected as cover art:

96. Congdon, M.; Fritzemeier, R.G.;  Kharel, Y.; Brown, A.M.;  Serbulea, V.; Bevan, D.R.;  Lynch, K.R.; Santos, W.L. Probing the Substitution Pattern of Indole-Based Scaffold Reveal Potent and Selective Sphingosine Kinase 2 Inhibitors. Eur. J. Med. Chem. 2021, 212, 113121. https://doi.org/10.1016/j.ejmech.2020.113121

95. Chen, S-Y; Beretta, M.;  Alexopoulos, S.J.;  Shah, D.;  Olzomer, E.M.; Hargett, S.R.; Childress, E.S.; Salamoun, J.M.; Roseblade, A.; Cranfield, C.; Rawling, T.; Tucker, S.P.; Santos, W.L.; Hoehn, K.L. Potent mitochondrial uncoupler SHC517 reverses diet-induced obesity in mice. Metabolism 2021, 117, 154724. https://doi.org/10.1016/j.metabol.2021.154724 

94. McDaniels, J.M.; Huckaby, A.C.; Carter, S.A.; Lingeman, S.; Francis, A.; Congdon, M.; Santos, W.L.; Phillips, M.A.; Rathod, P.K.; Guler, J. A. Extra-chromosomal DNA amplicons in antimalarial resistant Plasmodium falciparum, Mol. Microbiol. 2021, 115, 574-590. https://doi.org/10.1111/mmi.14624

93. Snead, R. J.; Nekvinda, J.; Santos, W.L. Copper(II)-catalyzed Protoboration of Allenes in Aqueous Media and Open Air. New J. Chem. 2020, DOI: 10.1039/D0NJ02010A . Invited contribution: “Boron & Beyond – Todd B. Marder’s Contributions to Chemistry”

selected as cover art:

2020

92. Peck, C.; Nekvinda, J.; Santos, W.L. Diboration of 3-Substituted Propargylic Alcohols using a Bimetallic Catalyst System: Access to (Z)-Allyl, Vinyldiboronates. Chem. Commun. 2020, 56, 10313-10316.  https://doi.org/10.1039/D0CC03563G

• Selected as Editor’s Choice: Main group reagents and catalysts in organic reactions

91. Grams, R.J.; Garcia, C.J.; Szwetkowski, C.; Santos, W.L. Catalytic, Transition Metal-Free Semireduction of Propiolamide Derivatives: Scope and Mechanistic Investigation. Org. Lett. 2020,  22,  7013–7018. doi.org/10.1021/acs.orglett.0c02567

• highlighted in Organic Chemistry Portal

90. Fritzemeier, R.G.; Nekvinda, J.; Vogels, C.M.; Rosenblum, C.A.; Slebodnick, C.; Westcott, S.A.; Santos, W.L. Organocatalytic trans Phosphinoboration of Internal Alkynes, Angew. Chem. Int. Ed. 2020, 59, 14358 –14362. https://doi.org/10.1002/anie.202006096

89. Nekvinda, J.; Santos, W.L. Copper-Catalyzed Cross-Coupling Reactions of Organoboron Compounds in Anilkumar, G. and Saranya, S. (eds) Copper Catalysis in Organic Synthesis, Wiley-VCH: Weinheim, 2020,  p. 23-50.

 

88. Salamoun, J.M.; Garcia, C.J.; Hargett, S.R.; Murray, J.; Chen, S-Y; Beretta, M.; Alexopoulos, S.J.;  Shah, D.;  Olzomer, E.M.; Tucker, S.P.; Hoehn, K.L. and Santos, W.L. 6-Amino-[1,2,5]oxadiazolo[3,4-b]pyrazin-5-ol Derivatives as Efficacious Mitochondrial Uncouplers in STAM Mouse Model of Non-alcoholic Steatohepatitis,  J. Med. Chem. 2020, 63, 6203-6224. https://doi.org/10.1021/acs.jmedchem.0c00542

selected as journal cover:

87. Liu, X.;  Ming, W.; Luo, X.; Friedrich, A.; Maier, J.; Radius, U.; Santos, W.L.;  Marder, T.B. Regio- and Stereoselective Synthesis of 1,1-Diborylalkenes via Brønsted Base-Catalyzed Mixed Diboration of Alkynes with BpinBdan, Eur. J. Org. Chem. 2020, 1941-1946. http://dx.doi.org/10.1002/ejoc.202000128

86. Murray, J.; Hargett, S.; Hoehn, K.L.; Santos, W.L. Anilinopyrazines as potential mitochondrial uncouplers, Bioorg. Med. Chem. Lett.  2020, 30, 127057. https://doi.org/10.1016/j.bmcl.2020.127057

85. Alexopoulos, S.J.; Chen, S.; Brandon, A.E.; Salamoun, J.M.; Byrne, F.L.; Garcia, C.J.; Beretta, M.; Olzomer, E.M.; Shah, D.P.; Philp, A.M.; Hargett, S.R.; Lawrence, R.T.; Lee, B.; Sligar, J.; Carrive, P.; Tucker, S.P.; Philp, A.; Lackner, C.; Turner, N.; Cooney, G.J.; Santos, W.L.; Hoehn, K.L. Mitochondrial uncoupler BAM15 reverses diet-induced obesity and insulin resistance in mice, Nat. Commun. 2020, 11, 2397. https://doi.org/10.1038/s41467-020-16298-2

• highlighted in Science Daily, VT News, News Break,  Medicalxpress 
• Top 50 read articles of 2020 at Nature Communications

84. Kharel, Y.; Huang, T.; Salamon, A.; Harris, T.E.; Santos, W.L.; Lynch, K.R. Clearance of sphingosine 1-phosphate from blood, Biochem. J. 2020, 477, 925–935. https://doi.org/10.1042/BCJ20190730

83. Childress, E.S.; Salamoun, J.M.; Hargett, S.R.; Santiago-Rivera, J.; Garcia, C.J.; Alexopoulos, S.J.; Chen, S-Y; Dai, Y.; Hoehn, K.L. and Santos, W.L. [1,2,5]Oxadiazolo[3,4-b]pyrazine-5,6-diamine Derivatives  as Mitochondrial Uncouplers for the Potential Treatment of Nonalcoholic Steatohepatitis, J. Med. Chem. 2020, 63, 2511-2526, https://doi.org/10.1021/acs.jmedchem.9b01440.

82. Sibley, C.D.; Morris, E.A.; Kharel, Y.; Brown, A.M.; Bevan, D.R.; Lynch, K.R.; Santos, W.L. Discovery of a Small Side Cavity in Sphingosine Kinase 2 that Enhances Inhibitor Potency and Selectivity, J. Med. Chem. 2020, 63, 1178-1198. https://pubs.acs.org/doi/10.1021/acs.jmedchem.9b01508

81. Blais-Lecours, P.; Laouafa, S.; Arias-Reyes, C.; Santos, W.L.; Joseph, V.; Halayko, A. J.; Soliz, J.; Marsolais, D. A. Metabolic adaptation of airway smooth muscle cells to a SPHK2 substrate precedes cytostasis. Am. J. Respir. Cell Mol. Biol. 2020, 62, 35-42. https://doi.org/10.1165/rcmb.2018-0397OC

80. Byrne, F.; Olzomer, E.; Marriott, G.; Quek, L.; Katen, A.; Su, J.; Nelson, M.; Hart-Smith, G.; Larance, M.; Sebesfi, V.; Cuff, J.; Martyn, G.; Childress, E.; Alexopoulos, S.p; Poon, I.; Faux, M.; Burgess, A.; Reid, G.; McCarroll, J.; Santos, W.; Quinlan, K.; Turner, N.; Fazakerley, D.; Kumar, N.; Hoehn, K. Phenotypic screen for oxygen consumption rate identifies a cancer-selective naphthoquinone that induces mitochondrial oxidative stress, Redox Biol. 2020,  28, 101374. https://doi.org/10.1016/j.redox.2019.101374.

2019

79. Fritzemeier, R.G.; Medici, E.J.; Szwetkowski, C.; Wonilowicz, L.G.; Sibley, C.D.; Slebodnick, C.; Santos, W.L. Facile Route to Air and Moisture Stable β-Difluoroboryl Acrylamides, Org. Lett. 2019,  21, 8053-8057. http://dx.doi.org/10.1021/acs.orglett.9b03031

78. Grams, R.J.; Fritzemeier, R.G.; Slebodnick, C.; Santos, W.L. Transition Metal-Free trans Hydroboration of Propiolamides: Access to Primary and Secondary (E)-beta-borylacrylamides. Org. Lett. 2019,  21, 6795-6799. https://pubs.acs.org/doi/full/10.1021/acs.orglett.9b02408

77. Gates, A.M.; Santos, W.L. Diboron-mediated semireduction of terminal allenes.  Synthesis, 2019,  51, 4619–4624. https://www.thieme-connect.com/products/ejournals/pdf/10.1055/s-0039-1690207.pdf

76. Peralta, N.; Dai, Y.; Sherpa, C.; Le Grice, S.F.; Santos, W.L. Molecular Recognition of HIV-1 RNAs with Branched Peptides. Methods Enzymol. 2019, 623, 373-400. https://doi.org/10.1016/bs.mie.2019.04.021

75. Verma, A.; Grams, J.; Rastatter, B.P.; Santos, W.L. Transition metal-free α borylation-protodeborylation of alkynoic acids. Tetrahedron, 2019, 75, 2113-2117. (Special Issue on Frustrated Lewis Acids and Organoboranes) https://doi.org/10.1016/j.tet.2019.02.030 

74. Dai, Y.; Peralta, A.N.; Wynn, J.E.; Sherpa, C.; Li, H.; Verma, A.; Le Grice, S.F.J.; Santos, W.L. Molecular Recognition of a Branched Peptide with HIV-1 Rev Response Element. Bioorg. Med. Chem.2019, 27, 759-1765. https://doi.org/10.1016/j.bmc.2019.03.016  Invited article for a special issue on targeting RNA.

73. Worrell, B.L.; Brown, A.M.; Santos, W.L.; Bevan, D.R. In silico Characterization of Structural Distinctions Between Isoforms of Human and Mouse Sphingosine Kinases for Accelerating Drug Discovery.  ACS J. Chem. Inf. Model., 2019, 59, 2339-2351.  DOI: 10.1021/acs.jcim.8b00931.

72. Hoagland, D.; Santos, W.L.; Poelzing, S.; Gourdie, R. The Role Of The Gap Junction Perinexus In Cardiac Conduction: Potential As A Novel Anti-Arrhythmic Drug Target. Prog. Biophys. Mol. Biol. 2019, 144, 41-50. https://doi.org/10.1016/j.pbiomolbio.2018.08.003.

71. 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. Photochem. Photobiol. Sci.,  2019,18, 30-44 .

2018

70. Cao, R.; Li, J.; Kharel, Y.; Zhang, C.; Santos, W.L.; Lynch, K.R.; Zuo, Z.; Hu, S. Photoacoustic Microscopy Reveals the Hemodynamic Basis of Sphingosine 1-phosphate Neuroprotection against Ischemic Stroke. Theranostics, 2018, 8, 6111-6120. doi:10.7150/thno.29435.

69. 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. Discovery of a Branched Peptide that Recognizes the Rev Response Element (RRE) RNA and Blocks HIV-1 Replication. J. Med. Chem., 2018,  61, 9611-9620,  DOI: 10.1021/acs.jmedchem.8b01076.

68. Fritzemeier, R.; Gates, A.; Guo, X.; Lin, Z.; Santos, W.L. Transition metal-free trans hydroboration of alkynoic acid derivatives: Experimental and theoretical studies. J. Org. Chem. 2018, 83, 10436−10444. DOI: 10.1021/acs.joc.8b01493.

67. Hemming, D.; Fritzemeier, R.; Wescott, S.A.; Santos, W.L.; Steel, P.G. Copper-Boryl Mediated Organic Synthesis. Chem. Soc. Rev. 2018, 47, 7477-7494 .  DOI:10.1039/C7CS00816C

66. 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

65. Childress, E. S.; Alexopoulos, S. J.; Hoehn, K. L.; Santos, W. L. Small Molecule Mitochondrial Uncouplers and Their Therapeutic Potential. J. Med. Chem. 2018, 61, 4641-4655. DOI: 10.1021/acs.jmedchem.7b01182

2017

64. 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

63. 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. Oncogene2017,8, 65588-65600. https://doi.org/10.18632/oncotarget.19514

62. 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

61. 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 .

60. 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.

59. 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

58. 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.

2016

57. 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

56. 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

55. 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 .

54. 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.

53. 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.

52. 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.

 

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 was featured on the front cover of the journal.

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

2015

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.

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

2014

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. Express2014, 22, 12935–12943. DOI:10.1364/OE.22.012935

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.

2013

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.

2012

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.

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.

2011

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

This paper is part of an “Emerging Investigator Issue”.

2010

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.

2009

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]

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.

2008

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]

2006

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]

2005

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.

2004

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]

2002

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]

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]