L-735,524: An Orally Bioavailable Human Immunodeficiency Virus Type 1 Protease Inhibitor
Vacca, J. P., Dorsey, B. D., Schleif, W. A., Levin, R. B., McDaniel, S. L., Darke, P. L., Zugay, J., Quintero, J. C., Blahy, O. M., Roth, E., Sardana, V. V., Schlabach, A. J., Graham, P. I., Condra, J. H., Gotlib, L., Holloway, M. K., Lin, J., I.-W. Chen, Vastag, K., Ostovic, D., Anderson, P. S., Emini, E. A., Huff, J. R.
Published in Proceedings of the National Academy of Sciences - PNAS (26.04.1994)
Published in Proceedings of the National Academy of Sciences - PNAS (26.04.1994)
Get full text
Journal Article
L-735,524 - THE DESIGN OF A POTENT AND ORALLY BIOAVAILABLE HIV PROTEASE INHIBITOR
DORSEY, BD, LEVIN, RB, MCDANIEL, SL, VACCA, JP, GUARE, JP, DARKE, PL, ZUGAY, JA, EMINI, EA, SCHLEIF, WA, QUINTERO, JC, LIN, JH, CHEN, IW, HOLLOWAY, MK, FITZGERALD, PMD, AXEL, MG, OSTOVIC, D, ANDERSON, PS, HUFF
Published in Journal of medicinal chemistry (14.10.1994)
Published in Journal of medicinal chemistry (14.10.1994)
Get full text
Journal Article
P450 interaction with HIV protease inhibitors : Relationship between metabolic stability, inhibitory potency, and P450 binding spectra
CHIBA, Masato, LIXIA JIN, NEWAY, William, VACCA, Joseph P, TATA, James R, CHAPMAN, Kevin, LIN, Jiunn H
Published in Drug metabolism and disposition (2001)
Get full text
Published in Drug metabolism and disposition (2001)
Journal Article
Design of Novel, Potent, Noncovalent Inhibitors of Thrombin with Nonbasic P-1 Substructures: Rapid Structure−Activity Studies by Solid-Phase Synthesis
Lumma, William C, Witherup, Keith M, Tucker, Thomas J, Brady, Steven F, Sisko, John T, Naylor-Olsen, Adel M, Lewis, S. Dale, Lucas, Bobby J, Vacca, Joseph P
Published in Journal of medicinal chemistry (26.03.1998)
Published in Journal of medicinal chemistry (26.03.1998)
Get full text
Journal Article
Discovery and Development of the Novel Potent Orally Active Thrombin Inhibitor N-(9-Hydroxy-9-fluorenecarboxy)prolyl trans-4-Aminocyclohexylmethyl Amide (L-372,460): Coapplication of Structure-Based Design and Rapid Multiple Analogue Synthesis on Solid Support
Brady, Stephen F, Stauffer, Kenneth J, Lumma, William C, Smith, Graham M, Ramjit, Harri G, Lewis, S. Dale, Lucas, Bobby J, Gardell, Steven J, Lyle, Elizabeth A, Appleby, Sandra D, Cook, Jacquelynn J, Holahan, Marie A, Stranieri, Maria T, Lynch, Joseph J, Lin, Jiunn H, Chen, I.-Wu, Vastag, Kari, Naylor-Olsen, Adel M, Vacca, Joseph P
Published in Journal of medicinal chemistry (29.01.1998)
Published in Journal of medicinal chemistry (29.01.1998)
Get full text
Journal Article
Highly diastereoselective alkylations of chiral amide enolates: new routes to hydroxyethylene dipeptide isostere inhibitors of HIV-1 protease
Askin, D, Wallace, M. A, Vacca, J. P, Reamer, R. A, Volante, R. P, Shinkai, I
Published in Journal of organic chemistry (01.05.1992)
Published in Journal of organic chemistry (01.05.1992)
Get full text
Journal Article
Potent Noncovalent Thrombin Inhibitors That Utilize the Unique Amino Acid d-Dicyclohexylalanine in the P3 Position. Implications on Oral Bioavailability and Antithrombotic Efficacy
Tucker, Thomas J, Lumma, William C, Lewis, S. Dale, Gardell, Stephen J, Lucas, Bobby J, Baskin, Elizabeth P, Woltmann, Richard, Lynch, Joseph J, Lyle, Elizabeth A, Appleby, Sandra D, Chen, I-Wu, Dancheck, Kimberley B, Vacca, Joseph P
Published in Journal of medicinal chemistry (23.05.1997)
Published in Journal of medicinal chemistry (23.05.1997)
Get full text
Journal Article
L-374,087, an efficacious, orally bioavailable, pyridinone acetamide thrombin inhibitor
Sanderson, Philip E.J., Cutrona, Kellie J., Dorsey, Bruce D., Dyer, Dona L., McDonough, Colleen M., Naylor-Olsen, Adel M., Chen, I-Wu, Chen, Zhongguo, Cook, Jacquelynn J., Gardell, Stephen J., Krueger, Julie A., Lewis, S.Dale, Lin, Jiunn H., Lucas, Bobby J., Lyle, Elizabeth A., Lynch, Joseph J., Stranieri, Maria T., Vastag, Kari, Shafer, Jules A., Vacca, Joseph P.
Published in Bioorganic & medicinal chemistry letters (07.04.1998)
Published in Bioorganic & medicinal chemistry letters (07.04.1998)
Get full text
Journal Article
Design and Synthesis of 8-Hydroxy-[1,6]Naphthyridines as Novel Inhibitors of HIV-1 Integrase in Vitro and in Infected Cells
Zhuang, Linghang, Wai, John S, Embrey, Mark W, Fisher, Thorsten E, Egbertson, Melissa S, Payne, Linda S, Guare, James P, Vacca, Joseph P, Hazuda, Daria J, Felock, Peter J, Wolfe, Abigail L, Stillmock, Kara A, Witmer, Marc V, Moyer, Gregory, Schleif, William A, Gabryelski, Lori J, Leonard, Yvonne M, Lynch, Joseph J, Michelson, Stuart R, Young, Steven D
Published in Journal of medicinal chemistry (13.02.2003)
Published in Journal of medicinal chemistry (13.02.2003)
Get full text
Journal Article
Metabolism of synthetic inositol trisphosphate analogs
Polokoff, M A, Bencen, G H, Vacca, J P, deSolms, S J, Young, S D, Huff, J R
Published in The Journal of biological chemistry (25.08.1988)
Published in The Journal of biological chemistry (25.08.1988)
Get full text
Journal Article
L-687,908, a potent hydroxyethylene containing HIV protease inhibitor
Vacca, Joseph P, Guare, J. P, DeSolms, S. J, Sanders, W. M, Giuliani, E. A, Young, S. D, Darke, P. L, Sigal, I. S, Schleif, W. A
Published in Journal of medicinal chemistry (01.03.1991)
Published in Journal of medicinal chemistry (01.03.1991)
Get full text
Journal Article
Discovery of a Novel, Selective, and Orally Bioavailable Class of Thrombin Inhibitors Incorporating Aminopyridyl Moieties at the P1 Position
Feng, Dong-Mei, Gardell, Stephen J, Lewis, S. Dale, Bock, Mark G, Chen, Zhongguo, Freidinger, Roger M, Naylor-Olsen, Adel M, Ramjit, Harri G, Woltmann, Richard, Baskin, Elizabeth P, Lynch, Joseph J, Lucas, Robert, Shafer, Jules A, Dancheck, Kimberley B, Chen, I-Wu, Mao, Shi-Shan, Krueger, Julie A, Hare, Timothy R, Mulichak, Anne M, Vacca, Joseph P
Published in Journal of medicinal chemistry (07.11.1997)
Published in Journal of medicinal chemistry (07.11.1997)
Get full text
Journal Article
C6 Modification of the pyridinone core of thrombin inhibitor L-374,087 as a means of enhancing its oral absorption
Isaacs, Richard C.A., Cutrona, Kellie J., Newton, Christina L., Sanderson, Philip E.J., Solinsky, Mark G., Baskin, Elizabeth P., Chen, I-Wu, Cooper, Carolyn M., Cook, Jacquelynn J., Gardell, Stephen J., Lewis, S.Dale, Lucas, Robert J., Lyle, Elizabeth A., Lynch, Joseph J., Naylor-Olsen, Adel M., Stranieri, Maria T., Vastag, Kari, Vacca, Joseph P.
Published in Bioorganic & medicinal chemistry letters (07.07.1998)
Published in Bioorganic & medicinal chemistry letters (07.07.1998)
Get full text
Journal Article
New advances in the discovery of thrombin and factor Xa inhibitors
Get full text
Book Review
Journal Article
Design and Synthesis of Potent, Selective, and Orally Bioavailable Tetrasubstituted Imidazole Inhibitors of p38 Mitogen-Activated Protein Kinase
Liverton, Nigel J, Butcher, John W, Claiborne, Christopher F, Claremon, David A, Libby, Brian E, Nguyen, Kevin T, Pitzenberger, Steven M, Selnick, Harold G, Smith, Garry R, Tebben, Andrew, Vacca, Joseph P, Varga, Sandor L, Agarwal, Lily, Dancheck, Kim, Forsyth, Amy J, Fletcher, Daniel S, Frantz, Betsy, Hanlon, William A, Harper, Coral F, Hofsess, Scott J, Kostura, Matthew, Lin, Jiunn, Luell, Sylvie, O'Neill, Edward A, Orevillo, Chad J, Pang, Margaret, Parsons, Janey, Rolando, Anna, Sahly, Yousif, Visco, Denise M, O'Keefe, Stephen J
Published in Journal of medicinal chemistry (17.06.1999)
Published in Journal of medicinal chemistry (17.06.1999)
Get full text
Journal Article
Metabolite–P450 Complex Formation by Methylenedioxyphenyl HIV Protease Inhibitors in Rat and Human Liver Microsomes
Chiba, Masato, Nishime, Joy A, Chen, I-Wu, Vastag, Kari J, Sahly, Yousif S, Kim, Byeong Moon, Dorsey, Bruce D, Vacca, Joseph P, Lin, Jiunn H
Published in Biochemical pharmacology (15.07.1998)
Published in Biochemical pharmacology (15.07.1998)
Get full text
Journal Article
Identification and SAR for a selective, nonpeptidyl thrombin inhibitor
Naylor-Olsen, Adel M., Ponticello, Gerald S., Lewis, S.Dale, Mulichak, Anne M., Chen, Zhonguo, Habecker, Charles N., Phillips, Brian T., Sanders, William M., Tucker, Thomas J., Shafer, Jules A., Vacca, Joseph P.
Published in Bioorganic & medicinal chemistry letters (07.07.1998)
Published in Bioorganic & medicinal chemistry letters (07.07.1998)
Get full text
Journal Article
Biochemical and cell-based assays for characterization of BACE-1 inhibitors
Pietrak, Beth L., Crouthamel, Ming-Chih, Tugusheva, Katherine, Lineberger, Janet E., Xu, Min, DiMuzio, Jillian M., Steele, Thomas, Espeseth, Amy S., Stachel, Shawn J., Coburn, Craig A., Graham, Samuel L., Vacca, Joseph P., Shi, Xiao-Ping, Simon, Adam J., Hazuda, Daria J., Lai, Ming-Tain
Published in Analytical biochemistry (01.07.2005)
Published in Analytical biochemistry (01.07.2005)
Get full text
Journal Article
Design and synthesis of HIV protease inhibitors. Variations of the carboxy terminus of the HIV protease inhibitor L-682,679
DESOLMS, S. J, GIULIANI, E. A, EMINI, E. A, SCHLEIF, W. A, QUINTERO, J. C, ANDERSON, P. S, HUFF, J. R, GUARE, J. P, VACCA, J. P, SANDERS, W. M, GRAHAM, S. L, WIGGINS, J. M, DARKE, P. L, SIGAL, I. S, ZUGAY, J. A
Published in Journal of medicinal chemistry (01.09.1991)
Published in Journal of medicinal chemistry (01.09.1991)
Get full text
Journal Article