Synergistic inhibition of Aβ production by combinations of γ-secretase modulators

by Robertson, Alan S., Iben, Lawrence G., Wei, Cong, Meredith, Jere E., Drexler, Dieter M., Banks, Martyn, Vite, Gregory D., Olson, Richard E., Thompson, Lorin A., Albright, Charles F., Ahlijanian, Michael K., Toyn, Jeremy H.
Published in European journal of pharmacology

Discovery of furo[2,3-d][1,3]thiazinamines as beta amyloid cleaving enzyme-1 (BACE1) inhibitors

by Wu, Yong-Jin, Guernon, Jason, Rajamani, Ramkumar, Toyn, Jeremy H., Ahlijanian, Michael K., Albright, Charles F., Muckelbauer, Jodi, Chang, ChiehYing, Camac, Dan, Macor, John E., Thompson, Lorin A.
Published in Bioorganic & medicinal chemistry letters

Robust Translation of γ-Secretase Modulator Pharmacology across Preclinical Species and Human Subjects

by Toyn, Jeremy H, Boy, Kenneth M, Raybon, Joseph, Meredith, Jr, Jere E, Robertson, Alan S, Guss, Valerie, Hoque, Nina, Sweeney, Francis, Zhuo, Xiaoliang, Clarke, Wendy, Snow, Kimberly, Denton, R Rex, Zuev, Dmitry, Thompson, Lorin A, Morrison, John, Grace, James, Berisha, Flora, Furlong, Michael, Wang, Jun-Sheng, Lentz, Kimberly A, Padmanabha, Ramesh, Cook, Lynda, Wei, Cong, Drexler, Dieter M, Macor, John E, Albright, Charlie F, Gasior, Maciej, Olson, Richard E, Hong, Quan, Soares, Holly D, AbuTarif, Malaz, Ahlijanian, Michael K
Published in The Journal of pharmacology and experimental therapeutics

Discovery of morpholine-based aryl sulfonamides as Na v 1.7 inhibitors

by Wu, Yong-Jin, Guernon, Jason, McClure, Andrea, Venables, Brian, Rajamani, Ramkumar, Robbins, Kevin J, Knox, Ronald J, Matchett, Michele, Pieschl, Rick L, Herrington, James, Bristow, Linda J, Meanwell, Nicholas A, Olson, Richard, Thompson, Lorin A, Dzierba, Carolyn
Published in Bioorganic & medicinal chemistry letters

Design and optimization of tricyclic gamma-secretase modulators

by Shi, Jianliang, Zuev, Dmitry, Xu, Li, Lentz, Kimberley A., Grace, James E., Toyn, Jeremy H., Olson, Richard E., Macor, John E., Thompson, Lorin A.
Published in Bioorganic & medicinal chemistry letters

Targeting the BACE1 Active Site Flap Leads to a Potent Inhibitor That Elicits Robust Brain Aβ Reduction in Rodents

by Wu, Yong-Jin, Guernon, Jason, Yang, Fukang, Snyder, Lawrence, Shi, Jianliang, Mcclure, Andrea, Rajamani, Ramkumar, Park, Hyunsoo, Ng, Alicia, Lewis, Hal, Chang, ChiehYing, Camac, Dan, Toyn, Jeremy H, Ahlijanian, Michael K, Albright, Charles F, Macor, John E, Thompson, Lorin A
Published in ACS medicinal chemistry letters

Synthesis of β-disubstituted β-amino isoxazolyl ketones by addition of ketimines with isoxazolyl methyl ketone enolates

by Guernon, Jason, Marcin, Lawrence, Higgins, Mendi, Yang, Fukang, Shi, Jianliang, Snyder, Lawrence, Thompson, Lorin A., Wu, Yong-Jin
Published in Tetrahedron letters

Identification and Characterization of Presenilin-independent Notch Signaling

by Berechid, Bridget E., Kitzmann, Magali, Foltz, Daniel R., Roach, Arthur H., Seiffert, Dietmar, Thompson, Lorin A., Olson, Richard E., Bernstein, Alan, Donoviel, Dorit B., Nye, Jeffrey S.
Published in The Journal of biological chemistry

Development of New Benzenesulfonamides As Potent and Selective Na v 1.7 Inhibitors for the Treatment of Pain

by Wu, Yong-Jin, Guernon, Jason, Shi, Jianliang, Ditta, Jonathan, Robbins, Kevin J, Rajamani, Ramkumar, Easton, Amy, Newton, Amy, Bourin, Clotilde, Mosure, Kathleen, Soars, Matthew G, Knox, Ronald J, Matchett, Michele, Pieschl, Rick L, Post-Munson, Debra J, Wang, Shuya, Herrington, James, Graef, John, Newberry, Kimberly, Bristow, Linda J, Meanwell, Nicholas A, Olson, Richard, Thompson, Lorin A, Dzierba, Carolyn
Published in Journal of medicinal chemistry

Identification and Preclinical Evaluation of the Bicyclic Pyrimidine γ‑Secretase Modulator BMS-932481

by Boy, Kenneth M, Guernon, Jason M, Zuev, Dmitry S, Xu, Li, Zhang, Yunhui, Shi, Jianliang, Marcin, Lawrence R, Higgins, Mendi A, Wu, Yong-Jin, Krishnananthan, Subramaniam, Li, Jianqing, Trehan, Ashok, Smith, Daniel, Toyn, Jeremy H, Meredith, Jere E, Burton, Catherine R, Kimura, S. Roy, Zvyaga, Tatyana, Zhuo, Xiaoliang, Lentz, Kimberley A, Grace, James E, Denton, Rex, Morrison, John S, Mathur, Arvind, Albright, Charles F, Ahlijanian, Michael K, Olson, Richard E, Thompson, Lorin A, Macor, John E
Published in ACS medicinal chemistry letters

BMS-986163, a Negative Allosteric Modulator of GluN2B with Potential Utility in Major Depressive Disorder

by Marcin, Lawrence R, Warrier, Jayakumar, Thangathirupathy, Srinivasan, Shi, Jianliang, Karageorge, George N, Pearce, Bradley C, Ng, Alicia, Park, Hyunsoo, Kempson, James, Li, Jianqing, Zhang, Huiping, Mathur, Arvind, Reddy, Aliphedi B, Nagaraju, G, Tonukunuru, Gopikishan, Gupta, Grandhi V. R. K. M, Kamble, Manjunatha, Mannoori, Raju, Cheruku, Srinivas, Jogi, Srinivas, Gulia, Jyoti, Bastia, Tanmaya, Sanmathi, Charulatha, Aher, Jayant, Kallem, Rajareddy, Srikumar, Bettadapura N, Vijaya, Kumar Kuchibhotla, Naidu, Pattipati S, Paschapur, Mahesh, Kalidindi, Narasimharaju, Vikramadithyan, Reeba, Ramarao, Manjunath, Denton, Rex, Molski, Thaddeus, Shields, Eric, Subramanian, Murali, Zhuo, Xiaoliang, Nophsker, Michelle, Simmermacher, Jean, Sinz, Michael, Albright, Charlie, Bristow, Linda J, Islam, Imadul, Bronson, Joanne J, Olson, Richard E, King, Dalton, Thompson, Lorin A, Macor, John E
Published in ACS medicinal chemistry letters

P-glycoprotein efflux and other factors limit brain amyloid beta reduction by beta-site amyloid precursor protein-cleaving enzyme 1 inhibitors in mice

by Meredith, Jr, Jere E, Thompson, Lorin A, Toyn, Jeremy H, Marcin, Lawrence, Barten, Donna M, Marcinkeviciene, Jovita, Kopcho, Lisa, Kim, Young, Lin, Alan, Guss, Valerie, Burton, Catherine, Iben, Lawrence, Polson, Craig, Cantone, Joe, Ford, Michael, Drexler, Dieter, Fiedler, Tracey, Lentz, Kimberley A, Grace, Jr, James E, Kolb, Janet, Corsa, Jason, Pierdomenico, Maria, Jones, Kelli, Olson, Richard E, Macor, John E, Albright, Charles F
Published in The Journal of pharmacology and experimental therapeutics

Synthesis and SAR of indole-and 7-azaindole-1,3-dicarboxamide hydroxyethylamine inhibitors of BACE-1

by Marcin, Lawrence R., Higgins, Mendi A., Zusi, F. Christopher, Zhang, Yunhui, Dee, Michael F., Parker, Michael F., Muckelbauer, Jodi K., Camac, Daniel M., Morin, Paul E., Ramamurthy, Vidhyashankar, Tebben, Andrew J., Lentz, Kimberley A., Grace, James E., Marcinkeviciene, Jovita A., Kopcho, Lisa M., Burton, Catherine R., Barten, Donna M., Toyn, Jeremy H., Meredith, Jere E., Albright, Charles F., Bronson, Joanne J., Macor, John E., Thompson, Lorin A.
Published in Bioorganic & medicinal chemistry letters

The structure of human tau-tubulin kinase 1 both in the apo form and in complex with an inhibitor

by Kiefer, Susan E., Chang, ChiehYing J., Kimura, S. Roy, Gao, Mian, Xie, Dianlin, Zhang, Yaqun, Zhang, Guifen, Gill, Martin B., Mastalerz, Harold, Thompson, Lorin A., Cacace, Angela M., Sheriff, Steven
Published in Acta crystallographica. Section F, Structural biology communications

Synthesis and in vivo evaluation of cyclic diaminopropane BACE-1 inhibitors

by Thompson, Lorin A., Shi, Jianliang, Decicco, Carl P., Tebben, Andrew J., Olson, Richard E., Boy, Kenneth M., Guernon, Jason M., Good, Andrew C., Liauw, Ann, Zheng, Changsheng, Copeland, Robert A., Combs, Andrew P., Trainor, George L., Camac, Daniel M., Muckelbauer, Jodi K., Lentz, Kimberley A., Grace, James E., Burton, Catherine R., Toyn, Jeremy H., Barten, Donna M., Marcinkeviciene, Jovita, Meredith, Jere E., Albright, Charles F., Macor, John E.
Published in Bioorganic & medicinal chemistry letters

Photochemically Enhanced Binding of Small Molecules to the Tumor Necrosis Factor Receptor-1 Inhibits the Binding of TNF-α

by Carter, Percy H., Scherle, Peggy A., Muckelbauer, Jodi A., Voss, Matthew E., Liu, Rui-Qin, Thompson, Lorin A., Tebben, Andrew J., Solomon, Kimberly A., Lo, Yvonne C., Li, Zhong, Strzemienski, Paul, Yang, Gengjie, Falahatpisheh, Nikoo, Xu, Meizhong, Wu, Zhongren, Farrow, Neil A., Ramnarayan, Kal, Wang, Jing, Rideout, Darryl, Yalamoori, Venkatachalapathi, Domaille, Peter, Underwood, Dennis J., Trzaskos, James M., Friedman, Steven M., Newton, Robert C., Decicco, Carl P.
Published in Proceedings of the National Academy of Sciences - PNAS

Synthesis and SAR of hydroxyethylamine based phenylcarboxyamides as inhibitors of BACE

by Wu, Yong-Jin, Zhang, Yunhui, Good, Andrew C., Burton, Catherine R., Toyn, Jeremy H., Albright, Charles F., Macor, John E., Thompson, Lorin A.
Published in Bioorganic & medicinal chemistry letters

[ 3H]BMS-599240 — A novel tritiated ligand for the characterization of BACE1 inhibitors

by Iben, Lawrence G., Kopcho, Lisa, Marcinkeviciene, Jovita, Zheng, Changsheng, Thompson, Lorin A., Albright, Charles F., Toyn, Jeremy H.
Published in European journal of pharmacology

Straightforward and general method for coupling alcohols to solid supports

by Thompson, Lorin A., Ellman, Jonathan A.
Published in Tetrahedron letters

Both 5-arylidene-2-thioxodihydropyrimidine-4,6(1H, 5H)-diones and 3-thioxo-2,3-dihydro-1H-imidazo[1,5-a]indol-1-ones are light-dependent tumor necrosis factor-α antagonists

by VOSS, Matthew E, CARTER, Percy H, STRZEMIENSKI, Paul, EVERLOF, J. Gerry, TRZASKOS, James M, DECICCO, Carl P, TEBBEN, Andrew J, SCHERLE, Peggy A, BROWN, Gregory D, THOMPSON, Lorin A, MEIZHONG XU, LO, Yvonne C, YANG, Gengjie, LIU, Rui-Qin
Published in Bioorganic & medicinal chemistry letters