Mapp publications

Dugan A, Majmudar CY, Pricer R, Niessen S, Lancia JK, Fung HY, Cravatt BF, Mapp AK (2016). Discovery of in vivo targets of transcriptional activators via in vivo covalent chemical capture.  J. Am. Chem. Soc. 2016, 138, 12629-35. PubMed link

Bruno PA, Morriss-Andrews A, Henderson AR, Brooks III CL, Mapp AK (2016).  A synthetic loop replacement peptide blocks canonical NF-κB signaling.  Angew. Chemie Int. Ed.  55 (48), pp. 14997-15001.  PubMed link

Law SM, Gagnon JK, Mapp AK, Brooks CL (2014).   Prepaying the entropic cost for allosteric regulation in KIX. 3rd. Proc Natl Acad Sci U S A.  111(33), pp. 12067-72. PubMed link

Wang N, Lodge JM, Fierke CA, Mapp AK. (2014).  Dissecting allosteric effects of activator-coactivator complexes using a covalent small molecule ligand. Proc Natl Acad Sci U S A. 19;111(33)pp. 12061 - 12066. PubMed link

Mapp AK, Pricer R, Sturlis S. (2015). Targeting transcription is no longer a quixotic quest.  Nat Chem Biol., 11(12), pp. 891 - 894. PubMed link

Xie, X., Piao, L., Cavey, G.S., Old, M., Teknos, T.N., Mapp, A.K., Pan, Q. (2013). Phosphorylation of Nanog is essential to regulate Bmi1 and promote tumorigenesis. Oncogene. In Press. PubMed link

Wang, N., Majmudar, C.Y., Pomerantz, W.C., Gagnon, J.K., Sadowsky, J.D., Meagher, J.L., Johnson, T.K., Stuckey, J.A., Brooks III, C.L., Wells, J.A., Mapp, A.K. (2013). Ordering a dynamic protein Via a small-molecule stabilizer. Journal of the American Chemical Society 135(9):3363-3366. PubMed link

Majmudar, C.Y., Højfeldt, J.W., Arevang, C.J., Pomerantz, W.C., Gagnon, J.K., Schultz, P.J., Cesa, L.C., Doss, C.H., Rowe, S.P., Vásquez, V., Tamayo-Castillo, G., Cierpicki, T., Brooks III, C.L., Sherman, D.H., Mapp, A.K. (2012). Sekikaic acid and lobaric acid target a dynamic interface of the coactivator CBP/p300. Angewandte Chemie - International Edition, 51 (45), pp. 11258-11262. PubMed link

Thompson, A.D., Dugan, A., Gestwicki, J.E., Mapp, A.K. (2012). Fine-tuning multiprotein complexes using small molecules. ACS Chemical Biology, 7 (8), pp. 1311-1320. PubMed link

Pomerantz, W.C., Wang, N., Lipinski, A.K., Wang, R., Cierpicki, T., Mapp, A.K. (2012). Profiling the dynamic interfaces of fluorinated transcription complexes for ligand discovery and characterization. ACS Chemical Biology, 7 (8), pp. 1345-1350. PubMed link

Taylor, C.E., Pan, Q., Mapp, A.K. (2012). Synergistic enhancement of the potency and selectivity of small molecule transcriptional inhibitors. ACS Medicinal Chemistry Letters, 3 (1), pp. 30-34. PubMed link

Krishnamurthy, M., Dugan, A., Nwokoye, A., Fung, Y.H., Lancia, J.K., Majmudar, C.Y., Mapp, A.K. (2011). Caught in the act: covalent cross-linking captures activator-coactivator interactions in vivo. ACS Chemical Biology, 6 (12), pp. 1321-1326. Letter. PubMed link

Højfeldt, J.W., Van Dyke, A.R., Mapp, A.K. (2011). Transforming ligands into transcriptional regulators: Building blocks for bifunctional molecules. Chemical Society Reviews, 40 (8), pp. 4286-4294. Review. PubMed link

Wands, A.M., Wang, N., Lum, J.K., Hsieh, J., Fierke, C.A., Mapp, A.K. (2011). Transient-state kinetic analysis of transcriptional activator·DNA complexes interacting with a key coactivator. Journal of Biological Chemistry, 286 (18), pp. 16238-16245. PubMed link

Bates, C.A., Pomerantz, W.C., Mapp, A.K. (2011). Transcriptional tools: Small molecules for modulating CBP KIX-dependent transcriptional activators. Biopolymers, 95 (1), pp. 17-23. PubMed link

Mapp, A. (2011). Human disease and transcriptional misregulation have strengthened. Biopolymers, 95(1). Editorial. PubMed link

Past Publications

Danowitz, A.M., Taylor, C.E., Shrikian, T.M., Mapp, A.K. (2010). Palladium-catalyzed [3,3]-rearrangement for the facile synthesis of allenamides. Organic Letters, 12 (11), pp. 2574-2577. PubMed link

Lee, L.W., Mapp, A.K. (2010). Transcriptional switches: Chemical approaches to gene regulation. Journal of Biological Chemistry, 285 (15), pp. 11033-11038. Short survey. PubMed link

Lee, L.W., Taylor, C.E.C., Desaulniers, J.-P., Zhang, M., Højfeldt, J.W., Pan, Q., Mapp, A.K. (2009). Inhibition of ErbB2(Her2) expression with small molecule transcription factor mimics. Bioorganic and Medicinal Chemistry Letters, 19 (21), pp. 6233-6236. PubMed link

Majmudar, C.Y., Lee, L.W., Lancia, J.K., Nwokoye, A., Wang, Q., Wands, A.M., Wang, L., Mapp, A.K. (2009). Impact of nonnatural amino acid mutagenesis on the in vivo function and binding modes of a transcriptional activator. Journal of the American Chemical Society, 131 (40), pp. 14240-14242. PubMed link

Aminoff, D., Bochar, D.A., Fuller, A.A., Mapp, A.K., Showalter, H.D.H., Kirchhoff, P.D. (2009). Research into selective biomarkers of erythrocyte exposure to organophosphorus compounds. Analytical Biochemistry, 392 (2), pp. 155-161. PubMed link

Majmudar, C.Y., Wang, B., Lum, J.K., Hâkansson, K., Mapp, A.K. (2009). A high-resolution interaction map of three transcriptional activation domains with a key coactivator from photo-cross-linking and multiplexed mass spectrometry. Angewandte Chemie - International Edition, 48 (38), pp. 7021-7024. PubMed link

Majmudar, C.Y., Labut, A.E., Mapp, A.K. (2009). Tra1 as a screening target for transcriptional activation domain discovery. Bioorganic and Medicinal Chemistry Letters, 19 (14), pp. 3733-3735. PubMed link

Bao, L., Gorin, M.A., Zhang, M., Ventura, A.C., Pomerantz, W.C., Merajver, S.D., Teknos, T.N., Mapp, A.K., Pan, Q. (2009). Preclinical development of a bifunctional cancer cell homing, PKCe inhibitory peptide for the treatment of head and neck cancer. Cancer Research, 69 (14), pp. 5829-5834. PubMed link

Buhrlage, S.J., Bates, C.A., Rowe, S.P., Minter, A.R., Brennan, B.B., Majmudar, C.Y., Wemmer, D.E., Al-Hashimi, H., Mapp, A.K. (2009). Amphipathic small molecules mimic the binding mode and function of endogenous transcription factors. ACS Chemical Biology, 4 (5), pp. 335-344. PubMed link

Buhrlage, S.J., Chen, B., Mapp, A.K. (2009). A flexible synthetic route to isoxazolidine ß-proline analogs. Tetrahedron, 65 (16), pp. 3305-3313.

Casey, R.J., Desaulniers, J.-P., Hojfeldt, J.W., Mapp, A.K. (2009). Expanding the repertoire of small molecule transcriptional activation domains. Bioorganic and Medicinal Chemistry, 17 (3), pp. 1034-1043. PubMed link

Mapp, A., Romesberg, F.E. (2008). Editorial overview. Current Opinion in Chemical Biology, 12 (4), pp. 387-388. Editorial

Rowe, S.P., Mapp, A.K. (2008). Assessing the permissiveness of transcriptional activator binding sites. Biopolymers, 89 (7), pp. 578-581. PubMed link

Rowe, S.P., Casey, R.J., Brennan, B.B., Buhrlage, S.J., Mapp, A.K. (2007). Transcriptional up-regulation in cells mediated by a small molecule. Journal of the American Chemical Society, 129 (35), pp. 10654-10655. PubMed link

Lum, J.K., Wu, Z., Mapp, A.K. (2007). Disrupting mediator with a short peptide ligand. ChemBioChem, 8 (11), pp. 1233-1236. PubMed link

Kiessling, L.L., Doudna, J.A., Johnson, K., Mapp, A.K., Marletta, M.A., Seeberger, P.H., Williamson, J.R., Wedde, S.G. (2007). A higher degree of difficulty. ACS Chemical Biology, 2 (4), pp. 197-199. Editorial. PubMed link

Mapp, A.K., Ansari, A.Z. (2007). A TAD further: Exogenous control of gene activation. ACS Chemical Biology, 2 (1), pp. 62-75. Review. PubMed link

Lum, J.K., Majmudar, C.Y., Ansari, A.Z., Mapp, A.K. (2006). Converting inactive peptides into potent transcriptional activators.. ACS Chemical Biology, 1 (10), pp. 639-643. Letter. PubMed link

Bucholtz, T.J., Palfey, B., Mapp, A.K., Glick, G.D. (2006). Graduate education chemical biology at the University of Michigan.. ACS Chemical Biology, 1 (8), pp. 487-488. PubMed link

Ferguson, M.L., Senecal, T.D., Groendyke, T.M., Mapp, A.K. (2006). [3,3]-Rearrangements of phosphonium ylides. Journal of the American Chemical Society, 128 (14), pp. 4576-4577. PubMed link

Majmudar, C.Y., Mapp, A.K. (2005). Chemical approaches to transcriptional regulation. Current Opinion in Chemical Biology, 9 (5), pp. 467-474. Review. PubMed link

Buhrlage, S.J., Brennan, B.B., Minter, A.R., Mapp, A.K. (2005). Stereochemical promiscuity in artificial transcriptional activators. Journal of the American Chemical Society, 127 (36), pp. 12456-12457. PubMed link

Lu, Z., Rowe, S.P., Brennan, B.B., Davis, S.E., Metzler, R.E., Nau, J.J., Majmudar, C.Y., Mapp, A.K., Ansari, A.Z. (2005). Unraveling the mechanism of a potent transcriptional activator. Journal of Biological Chemistry, 280 (33), pp. 29689-29698. PubMed link

Lum, J.K., Mapp, A.K. (2005). Artificial transcriptional activation domains. ChemBioChem, 6 (8), pp. 1311-1315. Short survey. PubMed link

Chen, B., Mapp, A.K. (2005). Thermal and catalyzed [3,3]-phosphorimidate rearrangements. Journal of the American Chemical Society, 127 (18), pp. 6712-6718. PubMed link

Fuller, A.A., Chen, B., Minter, A.R., Mapp, A.K. (2005). Succinct synthesis of ß-amino acids via chiral isoxazolines. Journal of the American Chemical Society, 127 (15), pp. 5376-5383. PubMed link

Majmudar, C.Y., Lum, J.K., Prasov, L., Mapp, A.K. (2005). Functional specificity of artificial transcriptional activators. Chemistry and Biology, 12 (3), pp. 313-321. PubMed link

Mapp, A.K. (2004). Finding their groove: Bifunctional molecules arrest growth of cancer cells. Chemistry and Biology, 11 (11), pp. 1480-1482. Short survey. PubMed link

Minter, A.R., Brennan, B.B., Mapp, A.K. (2004). A small molecule transcriptional activation domain. Journal of the American Chemical Society, 126 (34), pp. 10504-10505. PubMed link

Fuller, A.A., Chen, B., Minter, A.R., Mapp, A.K. (2004). Synthesis and structural characteristics of geminally disubstituted ß-amino acids. Synlett, (8), pp. 1409-1413.

Chen, B., Mapp, A.K. (2004). A Phosphorimidate Rearrangement for the Facile and Selective Preparation of Allylic Amines. Journal of the American Chemical Society, 126 (17), pp. 5364-5365. PubMed link

Wu, Z., Belanger, G., Brennan, B.B., Lum, J.K., Minter, A.R., Rowe, S.P., Plachetka, A., Majmudar, C.Y., Mapp, A.K. (2003). Targeting the transcriptional machinery with unique artificial transcriptional activators. Journal of the American Chemical Society, 125 (41), pp. 12390-12391. PubMed link

Mapp, A.K. (2003). Regulating transcription: A chemical perspective. Organic and Biomolecular Chemistry, 1 (13), pp. 2217-2220. Review. PubMed link

Minter, A.R., Fuller, A.A., Mapp, A.K. (2003). A concise approach to structurally diverse ß-amino acids. Journal of the American Chemical Society, 125 (23), pp. 6846-6847. PubMed link

Ansari, A.Z., Mapp, A.K. (2002). Modular design of artificial transcription factors. Current Opinion in Chemical Biology, 6 (6), pp. 765-772. PubMed link

Ansari, A.Z., Mapp, A.K., Nguyen, D.H., Dervan, P.B., Ptashne, M. (2001). Towards a minimal motif for artificial transcriptional activators. Chemistry and Biology, 8 (6), pp. 583-592. PubMed link

Mapp, A.K., Dervan, P.B. (2000). Preparation of thioesters for the ligation of peptides with non-native substrates. Tetrahedron Letters, 41 (49), pp. 9451-9454.

Mapp, A.K., Ansari, A.Z., Ptashne, M., Dervan, P.B. (2000). Activation of gene expression by small molecule transcription factors. Proceedings of the National Academy of Sciences of the United States of America, 97 (8), pp. 3930-3935. PubMed link

Mapp, A.K., Heathcock, C.H. (1999). Total synthesis of myxalamide A. Journal of Organic Chemistry, 64 (1), pp. 23-27. PubMed link

Caron, S., Stoermer, D., Mapp, A.K., Heathcock, C.H. (1996). Total synthesis of zaragozic acid A (squalestatin S1). Synthesis of the relay compound. Journal of Organic Chemistry, 61 (26), pp. 9126-9134.

Marshall, K.A., Mapp, A.K., Heathcock, C.H. (1996). Synthesis of a 2,7-dioxatricyclo[4.2.1.03,8]nonane: A model study for possible application in a synthesis of dictyoxetane. Journal of Organic Chemistry, 61 (26), pp. 9135-9145.