Allen A Thomas, PhD

Assistant Professor

  • 1117 Citations
  • 14 h-Index
19952019
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Research Output 1995 2019

  • 1117 Citations
  • 14 h-Index
  • 25 Article
  • 1 Conference article
2019

L-Type amino acid transporter 1 activity of 1,2,3-triazolyl analogs of L-histidine and L-tryptophan

Hall, C., Wolfe, H., Wells, A., Chien, H. C., Colas, C., Schlessinger, A., Giacomini, K. M. & Thomas, A. A., Aug 15 2019, In : Bioorganic and Medicinal Chemistry Letters. 29, 16, p. 2254-2258 5 p.

Research output: Contribution to journalArticle

Amino Acid Transport Systems
Triazoles
Histidine
Tryptophan
Amino Acids
2018
9 Citations (Scopus)

Reevaluating the Substrate Specificity of the L-Type Amino Acid Transporter (LAT1)

Chien, H. C., Colas, C., Finke, K., Springer, S., Stoner, L., Zur, A. A., Venteicher, B., Campbell, J., Hall, C., Flint, A., Augustyn, E., Hernandez, C., Heeren, N., Hansen, L., Anthony, A., Bauer, J., Fotiadis, D., Schlessinger, A., Giacomini, K. M. & Thomas, A. A., Aug 23 2018, In : Journal of Medicinal Chemistry. 61, 16, p. 7358-7373 16 p.

Research output: Contribution to journalArticle

Amino Acid Transport Systems
Substrate Specificity
Amino Acids
Large Neutral Amino Acid-Transporter 1
Essential Amino Acids
2016
15 Citations (Scopus)

LAT1 activity of carboxylic acid bioisosteres: Evaluation of hydroxamic acids as substrates

Zur, A. A., Chien, H. C., Augustyn, E., Flint, A., Heeren, N., Finke, K., Hernandez, C., Hansen, L., Miller, S., Lin, L., Giacomini, K. M., Colas, C., Schlessinger, A. & Thomas, A. A., Jan 1 2016, In : Bioorganic and Medicinal Chemistry Letters. 26, 20, p. 5000-5006 7 p.

Research output: Contribution to journalArticle

Large Neutral Amino Acid-Transporter 1
Hydroxamic Acids
Carboxylic Acids
Amino Acids
Substrates
18 Citations (Scopus)

LAT-1 activity of meta-substituted phenylalanine and tyrosine analogs

Augustyn, E., Finke, K., Zur, A. A., Hansen, L., Heeren, N., Chien, H. C., Lin, L., Giacomini, K. M., Colas, C., Schlessinger, A. & Thomas, A. A., Jun 1 2016, In : Bioorganic and Medicinal Chemistry Letters. 26, 11, p. 2616-2621 6 p.

Research output: Contribution to journalArticle

Large Neutral Amino Acid-Transporter 1
Phenylalanine
Tyrosine
Amino Acids
Aromatic Amino Acids
2015
2 Citations (Scopus)

Mitigation of opioid off-target effects and identification of structural drivers of opioid receptor engagement for BACE-1 small molecule inhibitors

Diaz, D., Dambach, D., Siu, M., Hunt, K., Thomas, A., Lyssikatos, J., Liu, X., Lewin-Koh, S., Mccray, B. & Ford, K., Jul 24 2015, In : Toxicology Mechanisms and Methods. 25, 6, p. 478-486 9 p.

Research output: Contribution to journalArticle

Opioid Receptors
Opioid Analgesics
Safety
Molecules
Rats
2014
11 Citations (Scopus)

8-tetrahydropyran-2-yl chromans: Highly selective beta-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors

Thomas, A. A., Hunt, K. W., Newhouse, B., Watts, R. J., Liu, X., Vigers, G., Smith, D., Rhodes, S. P., Brown, K. D., Otten, J. N., Burkard, M., Cox, A. A., Geck Do, M. K., Dutcher, D., Rana, S., Delisle, R. K., Regal, K., Wright, A. D., Groneberg, R., Liao, J. & 4 others, Scearce-Levie, K., Siu, M., Purkey, H. E. & Lyssikatos, J. P., Dec 11 2014, In : Journal of Medicinal Chemistry. 57, 23, p. 10112-10129 18 p.

Research output: Contribution to journalArticle

Chromans
Cathepsin D
Amyloid beta-Protein Precursor
Enzyme Inhibitors
Guanidines
20 Citations (Scopus)

Discovery of 5,6,7,8-tetrahydropyrido[3,4-d]pyrimidine inhibitors of Erk2

Blake, J. F., Gaudino, J. J., De Meese, J., Mohr, P., Chicarelli, M., Tian, H., Garrey, R., Thomas, A., Siedem, C. S., Welch, M. B., Kolakowski, G., Kaus, R., Burkard, M., Martinson, M., Chen, H., Dean, B., Dudley, D. A., Gould, S. E., Pacheco, P., Shahidi-Latham, S. & 5 others, Wang, W., West, K., Yin, J., Moffat, J. & Schwarz, J. B., Jun 15 2014, In : Bioorganic and Medicinal Chemistry Letters. 24, 12, p. 2635-2639 5 p.

Research output: Contribution to journalArticle

Drug Design
Extracellular Signal-Regulated MAP Kinases
Hep G2 Cells
Heterografts
Tumors
27 Citations (Scopus)

Discovery of 7-tetrahydropyran-2-yl chromans: β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors that reduce amyloid β-protein (Aβ) in the central nervous system

Thomas, A. A., Hunt, K. W., Volgraf, M., Watts, R. J., Liu, X., Vigers, G., Smith, D., Sammond, D., Tang, T. P., Rhodes, S. P., Metcalf, A. T., Brown, K. D., Otten, J. N., Burkard, M., Cox, A. A., Do, M. K. G., Dutcher, D., Rana, S., Delisle, R. K., Regal, K. & 7 others, Wright, A. D., Groneberg, R., Scearce-Levie, K., Siu, M., Purkey, H. E., Lyssikatos, J. P. & Gunawardana, I. W., Jan 7 2014, In : Journal of Medicinal Chemistry. 57, 3, p. 878-902 25 p.

Research output: Contribution to journalArticle

Guanidines
Chromans
Serum Amyloid A Protein
Cathepsin D
Amyloid beta-Protein Precursor
9 Citations (Scopus)

Synthesis, characterization, and PK/PD studies of a series of spirocyclic pyranochromene BACE1 inhibitors

Volgraf, M., Chan, L., Huestis, M. P., Purkey, H. E., Burkard, M., Geck Do, M., Harris, J., Hunt, K. W., Liu, X., Lyssikatos, J. P., Rana, S., Thomas, A. A., Vigers, G. P. A. & Siu, M., Jun 1 2014, In : Bioorganic and Medicinal Chemistry Letters. 24, 11, p. 2477-2480 4 p.

Research output: Contribution to journalArticle

Benzopyrans
Cytochrome P-450 CYP2D6
Scaffolds
Inhibitory Concentration 50
Rats
2013
13 Citations (Scopus)

Mechanistic Pharmacokinetic-Pharmacodynamic Modeling of BACE1 Inhibition in Monkeys: Development of a Predictive Model for Amyloid Precursor Protein Processings

Liu, X., Wong, H., Scearce-Levie, K., Watts, R. J., Coraggio, M., Shin, Y. G., Peng, K., Wildsmith, K. R., Atwal, J. K., Mango, J., Schauer, S. P., Regal, K., Hunt, K. W., Thomas, A. A., Siu, M., Lyssikatos, J., Deshmukh, G. & Hop, C. E. C. A., Jul 1 2013, In : Drug Metabolism and Disposition. 41, 7, p. 1319-1328 10 p.

Research output: Contribution to journalArticle

Amyloid beta-Protein Precursor
Haplorhini
Pharmacokinetics
Amyloid
Cerebrospinal Fluid
43 Citations (Scopus)

Spirocyclic β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors: From hit to lowering of cerebrospinal fluid (CSF) amyloid β in a higher species

Hunt, K. W., Cook, A. W., Watts, R. J., Clark, C. T., Vigers, G., Smith, D., Metcalf, A. T., Gunawardana, I. W., Burkard, M., Cox, A. A., Geck Do, M. K., Dutcher, D., Thomas, A. A., Rana, S., Kallan, N. C., Delisle, R. K., Rizzi, J. P., Regal, K., Sammond, D., Groneberg, R. & 6 others, Siu, M., Purkey, H., Lyssikatos, J. P., Marlow, A., Liu, X. & Tang, T. P., Apr 25 2013, In : Journal of Medicinal Chemistry. 56, 8, p. 3379-3403 25 p.

Research output: Contribution to journalArticle

Amyloid beta-Protein Precursor
Amyloid
Cerebrospinal Fluid
Alzheimer Disease
Brain
2008
26 Citations (Scopus)

Non-charged thiamine analogs as inhibitors of enzyme transketolase

Thomas, A. A., De Meese, J., Le Huerou, Y., Boyd, S. A., Romoff, T. T., Gonzales, S. S., Gunawardana, I., Kaplan, T., Sullivan, F., Condroski, K., Lyssikatos, J. P., Aicher, T. D., Ballard, J., Bernat, B., DeWolf, W., Han, M., Lemieux, C., Smith, D., Weiler, S., Wright, S. K. & 2 others, Vigers, G. & Brandhuber, B., Jan 15 2008, In : Bioorganic and Medicinal Chemistry Letters. 18, 2, p. 509-512 4 p.

Research output: Contribution to journalArticle

Transketolase
Thiamin Pyrophosphokinase
Thiamine
Enzyme Inhibitors
Cell proliferation
17 Citations (Scopus)

Prodrug thiamine analogs as inhibitors of the enzyme transketolase

Le Huerou, Y., Gunawardana, I., Thomas, A. A., Boyd, S. A., de Meese, J., deWolf, W., Gonzales, S. S., Han, M., Hayter, L., Kaplan, T., Lemieux, C., Lee, P., Pheneger, J., Poch, G., Romoff, T. T., Sullivan, F., Weiler, S., Wright, S. K. & Lin, J., Jan 15 2008, In : Bioorganic and Medicinal Chemistry Letters. 18, 2, p. 505-508 4 p.

Research output: Contribution to journalArticle

Transketolase
Thiamine
Prodrugs
Enzyme Inhibitors
Pharmacokinetics
36 Citations (Scopus)

Synthesis, in vitro and in vivo activity of thiamine antagonist transketolase inhibitors

Thomas, A. A., Le Huerou, Y., De Meese, J., Gunawardana, I., Kaplan, T., Romoff, T. T., Gonzales, S. S., Condroski, K., Boyd, S. A., Ballard, J., Bernat, B., DeWolf, W., Han, M., Lee, P., Lemieux, C., Pedersen, R., Pheneger, J., Poch, G., Smith, D., Sullivan, F. & 5 others, Weiler, S., Wright, S. K., Lin, J., Brandhuber, B. & Vigers, G., Mar 15 2008, In : Bioorganic and Medicinal Chemistry Letters. 18, 6, p. 2206-2210 5 p.

Research output: Contribution to journalArticle

Transketolase
Thiamine
Tumors
Neoplasms
Cells
2005
21 Citations (Scopus)

Oligo-α-hydroxy ester cross-linkers: Impact of cross-linker structure on biodegradable hydrogel networks

Eichenbaum, K. D., Thomas, A. A., Eichenbaum, G. M., Gibney, B. R., Needham, D. & Kiser, P. F., Dec 27 2005, In : Macromolecules. 38, 26, p. 10757-10762 6 p.

Research output: Contribution to journalArticle

Hydrogel
Hydrogels
Esters
Degradation
hydroxypropyl methacrylate
8 Citations (Scopus)

Symmetrical biodegradable crosslinkers for use in polymeric devices

Thomas, A. A., Kim, I. T. & Kiser, P. F., Dec 19 2005, In : Tetrahedron Letters. 46, 51, p. 8921-8925 5 p.

Research output: Contribution to journalArticle

glycolic acid
Lactic Acid
Hydrogels
Hydrogel
Equipment and Supplies
2002
168 Citations (Scopus)

Osmium-Catalyzed Dihydroxylation of Olefins in Acidic Media: Old Process, New Tricks

Dupau, P., Epple, R., Thomas, A. A., Fokin, V. V. & Sharpless, K. B., May 1 2002, In : Advanced Synthesis and Catalysis. 344, 3-4, p. 421-433 13 p.

Research output: Contribution to journalArticle

Osmium
Alkenes
Olefins
Citric acid
Citric Acid
2001
70 Citations (Scopus)

Isotope effects and the distinction between synchronous, asynchronous, and stepwise Diels-Alder reactions

Singleton, D. A., Schulmeier, B. E., Hang, C., Thomas, A. A., Leung, S. W. & Merrigan, S. R., Jun 11 2001, In : Tetrahedron. 57, 24, p. 5149-5160 12 p.

Research output: Contribution to journalArticle

Cycloaddition Reaction
Maleates
Isotopes
Alkynes
Kinetics
11 Citations (Scopus)

Rearrangement of methylenecamphor during electrophilic bromination: Remarkably clean access to the unnatural fenchyl (1,3,3-trimethylbicyclo[2.2.1]heptane) system

Thomas, A. A., Monk, K. A., Abraham, S., Lee, S. & Garner, C. M., Mar 18 2001, In : Tetrahedron Letters. 42, 12, p. 2261-2263 3 p.

Research output: Contribution to journalArticle

Heptanes
Stereochemistry
Halogenation
X ray crystallography
X Ray Crystallography
2000
1 Citation (Scopus)

Design and performance of poly(HPMA) hydrogels containing symmetrical biodegradable crosslinkers composed of oligo-lactate and oligo-glycolate esters

Kiser, P. F., Thomas, A. A., Eichenbaum, G. M., Needham, D. & Kim, I., Mar 1 2000, In : American Chemical Society, Polymer Preprints, Division of Polymer Chemistry. 41, 1, p. 712-713 2 p.

Research output: Contribution to journalConference article

hydroxypropyl methacrylate
glycolic acid
Hydrogels
Oligomers
Lactic Acid
1999
9 Citations (Scopus)
Stereochemistry
Cycloaddition Reaction
Isotopes
Labeling
Deuterium
116 Citations (Scopus)

The catalytic asymmetric aminohydroxylation of unsaturated phosphonates

Thomas, A. A. & Sharpless, K. B., Oct 29 1999, In : Journal of Organic Chemistry. 64, 22, p. 8379-8385 7 p.

Research output: Contribution to journalArticle

Organophosphonates
1998
1 Citation (Scopus)

Anti-tumor activity of a platinated polymer (AP5070) - Chemical optimization and confirmation of enhanaced therapeutic ratio

Luthy, C. L., Thomas, A. A., Callahan, E. H., Van Inwegen, R. G., Wilson, G., Evagorou, E. G., Gianasi, E. & Duncan, R., Jan 1 1998, In : Proceedings of the Controlled Release Society. 25, p. 132-133 2 p.

Research output: Contribution to journalArticle

1997
206 Citations (Scopus)

Experimental and theoretical kinetic isotope effects for asymmetric dihydroxylation. Evidence supporting a rate-limiting '(3+2)' cycloaddition

DelMonte, A. J., Haller, J., Houk, K. N., Sharpless, K. B., Singleton, D. A., Strassner, T. & Thomas, A. A., Nov 11 1997, In : Journal of the American Chemical Society. 119, 41, p. 9907-9908 2 p.

Research output: Contribution to journalArticle

Cycloaddition
Cycloaddition Reaction
Isotopes
Kinetics
1995
3 Citations (Scopus)

Allylic Metalation of Endo- and ExoCyclic Alkenes: Anomalous High Reactivity of β-Pinene

Garner, C. M. & Thomas, A. A., Oct 1 1995, In : Journal of Organic Chemistry. 60, 21, p. 7051-7054 4 p.

Research output: Contribution to journalArticle

Alkenes
beta-pinene
257 Citations (Scopus)

High-Precision Simultaneous Determination of Multiple Small Kinetic Isotope Effects at Natural Abundance

Singleton, D. A. & Thomas, A. A., Jan 1 1995, In : Journal of the American Chemical Society. 117, 36, p. 9357-9358 2 p.

Research output: Contribution to journalArticle