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2012

Luciferase-based assay for adenosine: Application to S -adenosyl- l -homocysteine hydrolase, Burgos, E. S., Gulab S. A., Cassera M. B., and Schramm V. L. , Analytical Chemistry, Volume 84, Number 8, p.3593-3598, (2012) Abstract

2011

Entropy-driven binding of picomolar transition state analogue inhibitors to Human 5′-methylthioadenosine phosphorylase, Guan, R., Ho M. - C., Brenowitz M., Tyler P. C., Evans G. B., Almo S. C., and Schramm V. L. , Biochemistry, Volume 50, Number 47, p.10408-10417, (2011) Abstract

Growth and metastases of human lung cancer are inhibited in mouse xenografts by a transition state analogue of 5′-methylthioadenosine phosphorylase, Basu, I., Locker J., Cassera M. B., Belbin T. J., Merino E. F., Dong X., Hemeon I., Evans G. B., Guha C., and Schramm V. L. , Journal of Biological Chemistry, Volume 286, p.4902-4911, (2011) Abstract

Plasmodium falciparum parasites are killed by a transition state analogue of purine nucleoside phosphorylase in a primate animal model, Cassera, M. B., Hazleton K. Z., Merino E. F., Obaldia N., Ho M. - C., Murkin A. S., DePinto R., Gutierrez J. A., Almo S. C., Evans G. B., et al. , PLoS ONE, Volume 6, Number 11, (2011) Abstract

2010

Conformational states of human purine nucleoside phosphorylase at rest, at work, and with transition state analogues, Edwards, A. A., Tipton J. D., Brenowitz M. D., Emmett M. R., Marshall A. G., Evans G. B., Tyler P. C., and Schramm V. L. , Biochemistry, Volume 49, p.2058-2067, (2010) Abstract

Design and synthesis of potent "sulfur-free" transition state analogue inhibitors of 5′-methylthioadenosine nucleosidase and 5′-methylthioadenosine phosphorylase, Longshaw, A. I., Adanitsch F., Gutierrez J. A., Evans G. B., Tyler P. C., and Schramm V. L. , Journal of Medicinal Chemistry, Volume 53, p.6730-6746, (2010) Abstract

Four generations of transition-state analogues for human purine nucleoside phosphorylase, Ho, M. - C., Shi W., Rinaldo-Matthis A., Tyler P. C., Evans G. B., Clinch K., Almo S. C., and Schramm V. L. , Proceedings of the National Academy of Sciences of the United States of America, Volume 107, p.4805-4812, (2010) Abstract

Transport of purines and purine salvage pathway inhibitors by the Plasmodium falciparum equilibrative nucleoside transporter PfENT1, Riegelhaupt, P. M., Cassera M. B., Fröhlich R. F. G., Hazleton K. Z., Hefter J. J., Schramm V. L., and Akabas M. H. , Molecular and Biochemical Parasitology, Volume 169, p.40-49, (2010) Abstract

2009

Altered enthalpy-entropy compensation in picomolar transition state analogues of human purine nucleoside phosphorylase, Edwards, A. A., Mason J. M., Clinch K., Tyler P. C., Evans G. B., and Schramm V. L. , Biochemistry, Volume 48, p.5226-5238, (2009) Abstract

Structural and metabolic specificity of methylthiocoformycin for malarial adenosine deaminases, Ho, M. - C., Cassera M. B., Madrid D. C., Ting L. - M., Tyler P. C., Kim K., Almo S. C., and Schramm V. L. , Biochemistry, Volume 48, p.9618-9626, (2009) Abstract

Syntheses of 5-chlorouracils/thymines with 1-[phosphono(methyl/ difluoromethyl)]-1,2-unsaturated-moiety-substituted methyl groups at N(1) and human thymidine phosphorylase inhibitory activity, Birck, M. R., Clinch K., Gainsford G. J., Schramm V. L., and Tyler P. C. , Helvetica Chimica Acta, Volume 92, p.823-838, (2009) Abstract

Third-generation immucillins: Syntheses and bioactivities of acyclic immucillin inhibitors of human purine nucleoside phosphorylase, Clinch, K., Evans G. B., Frohlich R. F. G., Furneaux R. H., Kelly P. M., Legentil L., Murkin A. S., Li L., Schramm V. L., Tyler P. C., et al. , Journal of Medicinal Chemistry, Volume 52, p.1126-1143, (2009) Abstract

Transition state analogues rescue ribosomes from saporin-L1 ribosome inactivating protein, Sturm, M. B., Tyler P. C., Evans G. B., and Schramm V. L. , Biochemistry, Volume 48, p.9941-9948, (2009) Abstract

2008

Azetidine based transition state analogue inhibitors of N-ribosyl hydrolases and phosphorylases, Evans, G. B., Furneaux R. H., Greatrex B., Murkin A. S., Schramm V. L., and Tyler P. C. , Journal of Medicinal Chemistry, Volume 51, p.948-956, (2008) Abstract

Immucillins in custom catalytic-site cavities, Murkin, A. S., Clinch K., Mason J. M., Tyler P. C., and Schramm V. L. , Bioorganic and Medicinal Chemistry Letters, Volume 18, p.5900-5903, (2008) Abstract

L-enantiomers of transition state analogue inhibitors bound to human purine nucleoside phosphorylase, Rinaldo-Matthis, A., Murkin A. S., Ramagopal U. A., Clinch K., Mee S. P. H., Evans G. B., Tyler P. C., Furneaux R. H., Almo S. C., and Schramm V. L. , Journal of the American Chemical Society, Volume 130, p.842-844, (2008) Abstract

Structural Insights into Intermediate Steps in the Sir2 Deacetylation Reaction, Hawse, W. F., Hoff K. G., Fatkins D. G., Daines A., Zubkova O. V., Schramm V. L., Zheng W., and Wolberger C. , Structure, Volume 16, p.1368-1377, (2008) Abstract

Transition-state interactions revealed in purine nucleoside phosphorylase by binding isotope effects, Murkin, A. S., Tyler P. C., and Schramm V. L. , Journal of the American Chemical Society, Volume 130, p.2166-2167, (2008) Abstract

A β-fluoroamine inhibitor of purine nucleoside phosphorylase, Mason, J. M., Murkin A. S., Li L., Schramm V. L., Gainsford G. J., and Skelton B. W. , Journal of Medicinal Chemistry, Volume 51, p.5880-5884, (2008) Abstract

2007

Acyclic ribooxacarbenium ion mimics as transition state analogues of human and malarial purine nucleoside phosphorylases, Taylor, E. A., Clinch K., Kelly P. M., Li L., Evans G. B., Tyler P. C., and Schramm V. L. , Journal of the American Chemical Society, Volume 129, p.6984-6985, (2007) Abstract

Inhibition and structure of Trichomonas vaginalis purine nucleoside phosphorylase with picomolar transition state analogues, Rinaldo-Matthis, A., Wing C., Ghanem M., Deng H., Wu P., Gupta A., Tyler P. C., Evans G. B., Furneaux R. H., Almo S. C., et al. , Biochemistry, Volume 46, p.659-668, (2007) Abstract

Picomolar inhibitors as transition-state probes of 5′-methylthioadenosine nucleosidases, Gutierrez, J. A., Luo M., Singh V., Li L., Brown R. L., Norris G. E., Evans G. B., Furneaux R. H., Tyler P. C., Painter G. F., et al. , ACS Chemical Biology, Volume 2, p.725-734, (2007) Abstract

Synthesis of 5′-methylthio coformycins: Specific inhibitors for malarial adenosine deaminase, Tyler, P. C., Taylor E. A., Fröhlich R. F. G., and Schramm V. L. , Journal of the American Chemical Society, Volume 129, p.6872-6879, (2007) Abstract

Transition state analogue inhibitors of N-ribosyltransferases: new drugs by targeting nucleoside processing enzymes., Evans, G. B., Furneaux R. H., Kelly P. M., Schramm V. L., and Tyler P. C. , Nucleic acids symposium series (2004), p.63-64, (2007) Abstract

2006

Syntheses and bio-activities of the l-enantiomers of two potent transition state analogue inhibitors of purine nucleoside phosphorylases, Clinch, K., Evans G. B., Fleet G. W. J., Furneaux R. H., Johnson S. W., Lenz D. H., Mee S. P. H., Rands P. R., Schramm V. L., Taylor Ringia E. A., et al. , Organic and Biomolecular Chemistry, Volume 4, p.1131-1139, (2006) Abstract

Transition state analogue discrimination by related purine nucleoside phosphorylases, Taylor Ringia, E. A., Tyler P. C., Evans G. B., Furneaux R. H., Murkin A. S., and Schramm V. L. , Journal of the American Chemical Society, Volume 128, p.7126-7127, (2006) Abstract

Structure and inhibition of a quorum sensing target from Streptococcus pneumoniae, Singh, V., Shi W., Almo S. C., Evans G. B., Furneaux R. H., Tyler P. C., Painter G. F., Lenz D. H., Mee S., Zheng R., et al. , Biochemistry, Volume 45, p.12929-12941, (2006) Abstract

2005

Femtomolar transition state analogue inhibitors of 5′- methylthioadenosine/S-adenosylhomocysteine nucleosidase from Escherichia coli, Singh, V., Evans G. B., Lenz D. H., Mason J. M., Clinch K., Mee S., Painter G. F., Tyler P. C., Furneaux R. H., Lee J. E., et al. , Journal of Biological Chemistry, Volume 280, p.18265-18273, (2005) Abstract

Second generation transition state analogue inhibitors of human 5′-methylthioadenosine phosphorylase, Evans, G. B., Furneaux R. H., Lenz D. H., Painter G. F., Schramm V. L., Singh V., and Tyler P. C. , Journal of Medicinal Chemistry, Volume 48, p.4679-4689, (2005) Abstract

Structural rationale for the affinity of pico- and femtomolar transition state analogues of Escherichia coli 5′-methylthioadenosine/S- adenosylhomocysteine nucleosidase, Lee, J. E., Singh V., Evans G. B., Tyler P. C., Furneaux R. H., Cornell K. A., Riscoe M. K., Schramm V. L., and Howell P. L. , Journal of Biological Chemistry, Volume 280, p.18274-18282, (2005) Abstract

Targeting a novel Plasmodium falciparum purine recycling pathway with specific immucillins, Ting, L. - M., Shi W., Lewandowicz A., Singh V., Mwakingwe A., Birck M. R., Taylor Ringia E. A., Bench G., Madrid D. C., Tyler P. C., et al. , Journal of Biological Chemistry, Volume 280, p.9547-9554, (2005) Abstract

Energetic mapping of transition state analogue interactions with human and Plasmodium falciparum purine nucleoside phosphorylases, Lewandowicz, A., Ringia E. A. T., Ting L. - M., Kim K., Tyler P. C., Evans G. B., Zubkova O. V., Mee S., Painter G. F., Lenz D. H., et al. , Journal of Biological Chemistry, Volume 280, p.30320-30328, (2005) Abstract

2004

Assignment of Downfield Proton Resonances in Purine Nucleoside Phosphorylase·Immucillin-H Complex by Saturation-Transferred NOEs, Deng, H., Lewandowicz A., Cahill S. M., Furneaux R. H., Tyler P. C., Girvin M. E., Callender R. H., and Schramm V. L. , Biochemistry, Volume 43, p.1980-1987, (2004) Abstract

Inhibition of Ricin A-Chain with Pyrrolidine Mimics of the Oxacarbenium Ion Transition State, Roday, S., Amukele T., Evans G. B., Tyler P. C., Furneaux R. H., and Schramm V. L. , Biochemistry, Volume 43, p.4923-4933, (2004) Abstract

Inhibitors of ADP-Ribosylating Bacterial Toxins Based on Oxacarbenium Ion Character at Their Transition States, Zhou, G. - C., Parikh S. L., Tyler P. C., Evans G. B., Furneaux R. H., Zubkova O. V., Benjes P. A., and Schramm V. L. , Journal of the American Chemical Society, Volume 126, p.5690-5698, (2004) Abstract

Picomolar Transition State Analogue Inhibitors of Human 5′-Methylthioadenosine Phosphorylase and X-ray Structure with MT-Immucillin-A, Singh, V., Shi W., Evans G. B., Tyler P. C., Furneaux R. H., Almo S. C., and Schramm V. L. , Biochemistry, Volume 43, p.9-18, (2004) Abstract

Plasmodium falciparum purine nucleoside phosphorylase: Crystal structures, immucillin inhibitors, and dual catalytic function, Shi, W., Ting L. - M., Kicska G. A., Lewandowicz A., Tyler P. C., Evans G. B., Furneaux R. H., Kim K., Almo S. C., and Schramm V. L. , Journal of Biological Chemistry, Volume 279, p.18103-18106, (2004) Abstract

Targeting the polyamine pathway with transition-state analogue inhibitors of 5′-methylthioadenosine phosphorylase, Evans, G. B., Furneaux R. H., Schramm V. L., Singh V., and Tyler P. C. , Journal of Medicinal Chemistry, Volume 47, p.3275-3281, (2004) Abstract

2003

8-Aza-immucillins as transition-state analogue inhibitors of purine nucleoside phosphorylase and nucleoside hydrolases, Evans, G. B., Furneaux R. H., Gainsford G. J., Hanson J. C., Kicska G. A., Sauve A. A., Schramm V. L., and Tyler P. C. , Journal of Medicinal Chemistry, Volume 46, p.155-160, (2003) Abstract

Achieving the ultimate physiological goal in transition state analogue inhibitors for purine nucleoside phosphorylase, Lewandowicz, A., Tyler P. C., Evans G. B., Furneaux R. H., and Schramm V. L. , Journal of Biological Chemistry, Volume 278, p.31465-31468, (2003) Abstract

Exploring structure-activity relationships of transition state analogues of human purine nucleoside phosphorylase, Evans, G. B., Furneaux R. H., Lewandowicz A., Schramm V. L., and Tyler P. C. , Journal of Medicinal Chemistry, Volume 46, p.3412-3423, (2003) Abstract

Ionic states of substrates and transition state analogues at the catalytic sites of N-ribosyltransferases, Sauve, A. A., Cahill S. M., Zech S. G., Basso L. A., Lewandowicz A., Santos D. S., Grubmeyer C., Evans G. B., Furneaux R. H., Tyler P. C., et al. , Biochemistry, Volume 42, p.5694-5705, (2003) Abstract

Over-the-barrier transition state analogues and crystal structure with Mycobacterium tuberculosis purine nucleoside phosphorylase, Lewandowicz, A., Shi W., Evans G. B., Tyler P. C., Furneaux R. H., Basso L. A., Santos D. S., Almo S. C., and Schramm V. L. , Biochemistry, Volume 42, p.6057-6066, (2003) Abstract

Synthesis of a transition state analogue inhibitor of purine nucleoside phosphorylase via the Mannich reaction, Evans, G. B., Furneaux R. H., Tyler P. C., and Schramm V. L. , Organic Letters, Volume 5, p.3639-3640, (2003) Abstract

Synthesis of Second-Generation Transition State Analogues of Human Purine Nucleoside Phosphorylase, Evans, G. B., Furneaux R. H., Lewandowicz A., Schramm V. L., and Tyler P. C. , Journal of Medicinal Chemistry, Volume 46, p.5271-5276, (2003) Abstract

2002

Atomic dissection of the hydrogen bond network for transition-state analogue binding to purine nucleoside phosphorylase, Kicska, G. A., Tyler P. C., Evans G. B., Furneaux R. H., Shi W., Fedorov A., Lewandowicz A., Cahill S. M., Almo S. C., and Schramm V. L. , Biochemistry, Volume 41, p.14489-14498, (2002) Abstract

Purine-less death in Plasmodium falciparum induced by immucillin-H, a transition state analogue of purine nucleoside phosphorylase, Kicska, G. A., Tyler P. C., Evans G. B., Furneaux R. H., Schramm V. L., and Kim K. , Journal of Biological Chemistry, Volume 277, p.3226-3231, (2002) Abstract

Transition state analogue inhibitors of purine nucleoside phosphorylase from Plasmodium falciparum, Kicska, G. A., Tyler P. C., Evans G. B., Furneaux R. H., Kim K., and Schramm V. L. , Journal of Biological Chemistry, Volume 277, p.3219-3225, (2002) Abstract

2001

Addition of lithiated 9-deazapurine derivatives to a carbohydrate cyclic imine: Convergent synthesis of the aza-C-nucleoside immucillins, Evans, G. B., Furneaux R. H., Hutchison T. L., Kezar H. S., Morris P. E., Schramm V. L., and Tyler P. C. , Journal of Organic Chemistry, Volume 66, p.5723-5730, (2001) Abstract

Immucillin H, a powerful transition-state analog inhibitor of purine nucleoside phosphorylase, selectively inhibits human T lymphocytes, Kicska, G. A., Long L., Hörig H., Fairchild C., Tyler P. C., Furneaux R. H., Schramm V. L., and Kaufman H. L. , Proceedings of the National Academy of Sciences of the United States of America, Volume 98, p.4593-4598, (2001) Abstract