The Saez Laboratory

Publications

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Parker, C.G., Galmozzi, A., Wang, Y., Correia, B.E., Sasaki, K., Joslyn, C.M., Kim, A.S., Cavallaro, C.L., Lawrence, M., Johnson, S.R., Narvaiza, I., Saez, E.*, Cravatt, B.F.* Ligand and Target Discovery by Fragment-Based Screening in Human Cells. Cell 2017, 168:1-15. (*co-corresponding authors).

Chen, W., Dong, J., Plate, L., Mortenson, D.E., Brighty, G.J., Li, S., Liu, Y., Galmozzi, A., Lee, P.S., Hulce, J., Cravatt, B.F., Saez, E., Powers, E.T., Wilson, I.A., Sharpless, K.B., and J.W. Kelly. Arylfluorosulfates Inactivate Intracellular Lipid Binding Protein(s) through Chemoselective SuFEx Reaction with a Binding Site Tyr Residue. Journal American Chemical Society 2016, 138:7353-64.

Parsons, W.H., Kolar, M.J., Kamat, S.S., Cognetta, A.B., Hulce, J.J., Saez, E., Khan, B., Saghatelian, A. and B.F. Cravatt. AIG1 and ADTRP are atypical integral membrane hydrolases that degrade bioactive FAHFAs. Nature Chemical Biology 2016, 5:367-72

Ceperuelo-Mallafré,V., Ejarque, M., Serena, C., Duran, X., Montori-Grau, M., Rodríguez, M.A., Yanes, O., Núñez-Roa, C., Roche, K., Puthanveetil, P., Garrido, L., Saez, E., Tinahones, F., Garcia, P., Gómez, A., Saltiel, A.R., Vendrell, J. and S. Fernández-Veledo. Adipocyte glycogen accumulation underlies obesity-linked adipose tissue dysfunction in humans. Molecular Metabolism 2015, 1:5-18.

Cermenati, G., Audano, M., Giatti, S., Carozzi, V., Porretta-Serapiglia, C., Pettinato, E., Ferri, C., D’Antonio, M., De Fabiani, E., Crestani, M., Scurati, S., Saez, E., Azcoitia, I., Cavaletti, G., Garcia-Segura^, L., Melcangi, R.C., Caruso, D. and N. Mitro. Lack Of Sterol Regulatory Element Binding Factor-1c Imposes Glial Fatty Acid Utilization Leading To Peripheral Neuropathy. Cell Metabolism 2015, 21:571–583.

Galmozzi, A., Sonne, S.B., Keylin, S., Luijten, I., Chang, J.W., Sharp, L.Z., Cravatt, B.F., Saez, E.* and S. Kajimura.* ThermoMouse: an in vivo model to identify modulators of UCP1 expression in brown adipose tissue. Cell Reports 2014, 9:1584-93. (*co-corresponding authors).

Kok, B.P. and E. Saez. Activating PI 3-Kinase to dampen inflammation. Chemistry and Biology 2014, 21:917-8.

Dominguez, E., Galmozzi, A., Chang, J.W., Hsu, K., Pawlak, J., Li, W., Godio, C., Thomas, J., Partida, D., Niessen, S., O’Brien, P.E., Russell, A.P., Watt, M.J., Nomura, D.K., Cravatt, B.F. and E. Saez. Integrated phenotypic and activity-based profiling links Ces3 to obesity and diabetes. Nature Chemical Biology 2014, 10:113-121.

Galmozzi, A., Dominguez, E., Cravatt, B.F. and E. Saez. Application of Activity-Based Protein Profiling to study enzyme function in adipocytes. Methods in Enzymology 2014, 538:151-169.

Chou, W-L., Galmozzi, A., Partida, D., Yeung, H., Kwan, K., Su, A.I. and E. Saez. Identification of regulatory elements that control PPARg expression in adipocyte progenitors. PLoS One 2013, 8(8):e72511

Claudio Villanueva, C., Vergnes, L., Wang, J., Drew, B., Hong, C., Tu, Y., Hu, Y., Peng, X., Xu, P., Saez, E., Hevener, A., Reue, K., Loren Fong, L., Young, S. and P. Tontonoz. Adipose subtype-selective recruitment of TLE3 or Prdm16 by PPARg specifies lipid-storage versus thermogenic gene programs. Cell Metabolism 2013, 17:423-35.

Sanchez-Alavez, M., Conti, B., Wood, M.R., Bortell, N., Bustamante, E., Saez, E., Fox, H.S, and M.C.G. Marcondes. ROS and sympathetically mediated mitochondria activation in brown adipose tissue contribute to methamphetamine-induced hyperthermia. Frontiers in Endocrinology 2013, 4:44.

Galmozzi, A., Mitro, N., Ferrari, A., Gers, E., Gilardi, F., Godio, C., Cermenati, G., Gualerzi, A., Donetti, E., Rotili, D., Valente, S., Guerrini, U., Caruso, D., Mai, A., Saez, E., De Fabiani, E. and M. Crestani. Inhibition of Class I Histone Deacetylases Unveils a Mitochondrial Signature and Enhances Oxidative Metabolism in Skeletal Muscle and Adipose Tissue. Diabetes 2013, 62:732-42.

Jain, T., Papas, A., Jadhav, A. and E. Saez. In situ electroporation of surface-bound siRNAs in microwell arrays. Lab on a Chip 2012, 12:939-47.

Cermenati, G., Abbiati, F., Cermenati, S., Brioschi, E., Volonterio, A., Cavaletti, G., Saez, E., De Fabiani, E., Crestani, M., Garcia-Segura, L., Melcangi, R.C., Caruso, D. and Nico Mitro. Diabetes induced myelin abnormalities are associated with an altered lipid pattern: protective effects of LXR activation. Journal of Lipid Research 2012, 53:300-10.

Villanueva, C.J., Waki, H., Godio, C., Nielsen, R., Chou, W.-L., Vargas, L., Wrobleski, K., Schemdt, C., Chao, L. C., Boyadjian, R., Mandrup, S., Hevener, S., Saez, E.* and P. Tontonoz*. TLE3 is a dual function transcriptional coregulator of adipogenesis. Cell Metabolism 2011, 3:413-27. (*co-corresponding authors).

Cermenati, G., Giatti, S., Cavaletti, G., Bianchi, R., Maschi, O., Pesaresi, M., Abbiati, F., Volonterio, A., Saez, E., Caruso, D., Melcangi, R. and N. Mitro. Activation of the Liver X Receptor increases neuroactive steroid levels and protects from diabetes-induced peripheral neuropathy. Journal of Neuroscience 2010, 30:11896-901.

Teo, H., Ghosh, S., Luesch, H., Ghosh, A., Wong, E.T., Malik, N., Orth, A., De Jesus, P., Perry, A.S., Oliver, J.D., Tran, N.L., Speiser, L.J., Wong, M., Saez, E., Schultz, P., Chanda, S.K., Verma, I.M. and V. Tergaonkar. Telomere-independent Rap1 is an IKK adaptor and regulates NF-kappaB-dependent gene expression. Nature Cell Biology 2010, 8:758-67.

Epple. R., Cow, C., Xie, Y., Azimioara, M., Russo, R., Wang, X., Wityak, J., Karanewsky, D.S., Tuntland,T., Nguyeñ-Tran, V.T., Cuc, C., Huang, D., Saez, E., Spalding, T., Gerken, A., Iskandar, M., Seidel, HM. and S.S. Tian. Novel Bisaryl Substituted Thiazoles and Oxazoles as Highly Potent and Selective Peroxisome Proliferator-Activated Receptor δ Agonists. Journal of Medicinal Chemistry 2010 53:77-105.

Jain, T. and E. Saez. Highly parallel introduction of nucleic acids into mammalian cells grown in microwell arrays. Lab Chip 2009. 9: 3557-3566.

Zhu, J., Mounzih, K., Chehab, E.C., Mitro, N., Saez, E. and F.F. Chehab. Effects of FoxO4 overexpression on cholesterol biosynthesis, triacylglycerols accumulation and glucose uptake. Journal of Lipid Research 2009. Dec 25. [Epub ahead of print]

Sironi, L., Mitro, M., Cimino, M., Gelosa, P., Guerrini, U., Tremoli, E., and Saez, E. Treatment with LXR agonists after focal cerebral ischemia prevents brain damage. FEBS letters 2008, 582(23-24):3396-400.

Wu, C., Delano, D.L., Mitro, N., Su, S.V., Janes, J., McClurg, P., Batalov, S., Welch, G.L., Zhang, J., Orth, A.P., Walker, J.R., Glynne, R.J., Cooke, M.P., Takahashi, J.S., Shimomura, K., Kohsaka, A., Bass, J., Saez, E., Wiltshire, T., Su, AI. Gene set enrichment in eQTL data identifies novel annotations and pathway regulators. PLoS Genet 2008, 4(5):e1000070.

Commerford, S.R., Vargas, L., Dorfman, S.E., Mak, P.A., Mitro, N., Rocheford, E.C., Li, X., Kennedy, P., Mullarkey, T.L., and Saez, E. Dissection of the anti-diabetic effect of liver X receptor ligands. Molecular Endocrinology 2007, 21(12):3002-1.

Molteni, V., Li, X., Nabakka, J., Liang, F., Wityak, J., Koder, A., Vargas, L., Romeo, R., Mitro, N., Mak, P.A., Seidel, H.M., Haslam, J.A., Tuntland, T., Spalding, T.A., Brock, A., Bradley, M., Castrillo, A., Tontonoz, P. and Saez, E. N-Acylthiadiazolines, a new class of liver X receptor agonists with selectivity for LXRβ. The Journal of Medicinal Chemistry 2007 50(17):4255-9.

Waki, H., Park, K.W., Mitro, N., Pei, L., Damoiseaux, R., Wilpitz, D.C., Reue, K., Saez, E. and P. Tontonoz. The Small Molecule Harmine Is an Antidiabetic Cell-Type-Specific Regulator of PPARγ Expression. Cell Metabolism 2007, 5: 357-70.

Mitro, N., Vargas, L., Romeo, R., Koder, A., and Saez, E. T0901317 is a potent PXR ligand: Implications for the biology ascribed to LXR. FEBS Lett. 2007, 581: 1721-6.

Mitro, N., Mak, P., Vargas, L., Godio, C., Hampton, E., Molteni, V., Kresuch, A. and Saez, E. 2006. The nuclear receptor LXR is a glucose sensor. Nature 2007, 445: 219-23.

Epple, R., Russo, R., Azimioara, M., Cow, C., Xie, Y., Wang, X., Wityak, J., Karanewsky, D., Gerken, A., Iskandar, M., Saez, E., Seidel, M. H. and S.S. Tian. 3,4,5-Trisubstituted isoxazoles as novel PPARδ agonists: Part 2. Bioorg Med Chem Lett 2006, 16: 5488-92.

Cho, C.Y., Koo, S-H., Wang, Y., Callaway, S., Hedrick, S., Mak, P.A., Orth, A.P., Peters, E.C., Saez, E., Montminy, M., Schultz, P.G. and S.K. Chanda. Identification of the tyrosine phosphatase PTP-MEG2 as an antagonist of hepatic insulin signaling. Cell Metabolism 2006, 3: 367-378.

Galimi*, F., Saez*, E., Gall, J.G., Hoong, N., Cho, G., Evans, R.M., and I.M. Verma. Development of ecdysone-regulated lentiviral vectors. Molecular Therapy 2005, 11: 142-148. *Joint first authors

Joseph, S.B., Bradley, M., Castrillo, A., Bruhn, K., Mak, P., Pei, L. Hogenesch, J., Oï¿½Connell, R.M., Cheng, G., Saez, E., Miller, J. and P. Tontonoz. LXR-dependent gene expression is important for macrophage survival and the innate immune response to bacterial pathogens. Cell 2004, 119: 299-309.

Saez, E., Rosenfeld, J.R., Livolsi, A., Olson, P., Lombardo, E., Nelson, M.C., Banayo, E., Cardiff, R.D., Izpisua/Belmonte, J.C. and R.M. Evans. PPARγ signaling exarcebates mammary gland tumor development. Genes and Development 2004, 18: 528-540.

Saez, E., Olson, P. and R.M. Evans. Genetic deficiency in PPARg does not alter development of experimental prostate cancer. Nature Medicine 2003, 9: 5419-5424.

Laffitte, B.A., Chao, L.C., Li, J., Walczak, R., Hummasti, S., Joseph, S.B., Castrillo, A., Wilpitz, D.C., Mangelsdorf, D.J., Collins, J.L., Saez, E. and P. Tontonoz. Activation of liver X receptor improves glucose tolerance through coordinate regulation of glucose metabolism in liver and adipose tissue. PNAS 2003, 100: 5419-5424.

Saez, E., Nelson, M.C., Eshelman, B., Banayo, E., Koder, A., Cho, G.J., and R.M. Evans. Identification of ligands and coligands for the ecdysone-regulated gene switch. PNAS 2000, 97: 14512-14517.

Chawla, A., Saez, E., and R.M. Evans. "Don't know much bile-ology". Cell 2000, 103: 1-4.

Saez, E., Tontonoz, P., Nelson, M.C., Alvarez, J.G., U, T-M., Baird, S.M., Thomazy, V.A., and R.M. Evans. Activators of the nuclear receptor PPARγ enhance colon polyp formation. Nature Medicine 1998, 4:1058-1061.

Serova, L., Saez, E., Spiegelman, B.M., and E.L. Sabban. c-Fos deficiency inhibits induction of mRNA for some, but not all, neurotransmitter biosynthetic enzymes by immobilization stress. Journal of Neurochemistry 1998, 70: 1935-1940.

Saez, E., No, D., West, A., and R.M. Evans. Inducible gene expression in mammalian cells and transgenic mice. Current Opinion in Biotechnology 1997, 8:608-616.

Rutberg, S.E., Saez, E., Lo, S., Jang, S.-I., Markova, N., Spiegelman, B.M. and S.H. Yuspa. Opposing activities of c-Fos and Fra-2 on AP-1 regulated transcriptional activity in mouse keratinocytes induced to differentiate by calcium and phorbol esters. Oncogene 1997, 15: 1337-1346.

Holmes, S.G., Rose, A.B., Steuerle, K., Saez, E., Sayegh, S., Lee, Y.M. and J.R. Broach. Hyperactivation of the silencing proteins Sir2p and Sir3p, causes chromosome loss. Genetics 1997, 145:605-614.

Rutberg, S.E., Saez, E., Glick, A., Dlugosz, A.A., Spiegelman, B.M. and S.H. Yuspa. Differentiation of mouse keratinocytes is accompanied by PKC-dependent changes in AP-1 proteins. Oncogene 1996, 13: 167-176.

Saez, E., Oppenheim, H., Van Etten, R.E. and B.M. Spiegelman. C-fos is not essential for v-abl-induced lymphomagenesis. Cancer Research 1995, 55: 6196-6199.

Saez, E., Rutberg, S.E., Mueller, E., Oppenheim, H., Smoluk, J., Yuspa, S. H. and B.M. Spiegelman. C-fos is required for malignant progression of skin tumors. Cell 1995, 82: 721-732.