Zobrazeno 1 - 10
of 11
pro vyhledávání: '"Bryan Oates"'
Autor:
Gary Woodnutt, Shenping Liu, Wei Li, Jane M. Withka, Xidong Feng, Boris A. Chrunyk, Wood Lauren Diane, Xiayang Qiu, Suman Shanker, Mary Ellen Banker, Parag Sahasrabudhe, Abhijit Bhat, Ping Jin, Curt Bradshaw, Bryan Oates, Rodney W. Lappe, Xi Song, David Tumelty, Matt Griffor, Gang Chen, Judith Jimenez, Atli Thorarensen, Joel Desharnais
Publikováno v:
Scientific Reports
IL-17A is a pro-inflammatory cytokine that has been implicated in autoimmune and inflammatory diseases. Monoclonal antibodies inhibiting IL-17A signaling have demonstrated remarkable efficacy, but an oral therapy is still lacking. A high affinity IL-
Autor:
Joselyn Del Rosario, Michelle Parish, Bin Liu, Jie Huang, Ping Jin, Dingguo Liu, Marla J. Matin, Gary Woodnutt, Bryan Oates, Jing-Yu Lai, Nancy Levin, Rodney W. Lappe, Curt W. Bradshaw, Richard A. Lerner, Crystal Hagen, Abhijit Bhat, Robert E. Murphy, Zemeda W Ainekulu, Michael J. Shields, Venkata Doppalapudi, Lingna Li, Joel Desharnais
Publikováno v:
Proceedings of the National Academy of Sciences. 107:22611-22616
Bispecific antibodies (BsAbs) are regarded as promising therapeutic agents due to their ability to simultaneously bind two different antigens. Several bispecific modalities have been developed, but their utility is limited due to problems with stabil
Autor:
William A. Schleif, Karen Holmes, Julie A. DeMartino, Liping Wang, Anthony Carella, Gwen Carver, Lorraine Malkowitz, Malcolm MacCoss, Paul E. Finke, Bryan Oates, Janet Lineberger, Emilio A. Emini, Ping Chen, Renee Danzeisen, Joseph Kessler, Michael W. Miller, Martin S. Springer, Sandra L. Gould, Daria J. Hazuda, Sander G. Mills, Dooseop Kim, Charles G. Caldwell
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 11:3099-3102
A series of hydantoin derivatives has been discovered as highly potent nonpeptide antagonists for the human CCR5 receptor. The synthesis, SAR, and biological profiles of this class of antagonists are described.
Autor:
Janet Lineberger, Julie A. DeMartino, Salvatore J. Siciliano, Paul E. Finke, Richard J. Budhu, Gwen Carver, Malcolm MacCoss, Karen Holmes, Jeffrey J. Hale, Renee Danzeisen, Sandra L. Gould, Joseph Kessler, Bryan Oates, Edward Holson, William A. Schleif, Anthony Carella, Emilio A. Emini, Daria J. Hazuda, Sander G. Mills, Lorraine Malkowitz, Michael W. Miller, Martin S. Springer
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 11:2741-2745
Investigations of the structure-activity relationships of 1,3,4-trisubstituted pyrrolidine human CCR5 receptor antagonists afforded orally bioavailable compounds with the ability to inhibit HIV replication in vitro.
Autor:
Paul E. Finke, Emilio A. Emini, Sandra L. Gould, Michael W. Miller, Martin S. Springer, Lorraine Malkowitz, Anthony Carella, Karen Holmes, Julie A. DeMartino, Gwen Carver, Daria J. Hazuda, Sander G. Mills, Renee Danzeisen, Joseph Kessler, William A. Schleif, Malcolm MacCoss, Janet Lineberger, Bryan Oates
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 11:2475-2479
(2S)-2-(3-Chlorophenyl)-1-[N-(methyl)-N-(phenylsulfonyl)amino]-4-[spiro(2,3-dihydrobenzthiophene-3,4'-piperidin-1'-yl)]butane S-oxide (1b) has been identified as a potent CCR5 antagonist having an IC50=10 nM. Herein, structure-activity relationship s
Autor:
Karen Holmes, Michael W. Miller, Malcolm MacCoss, Lorraine Malkowitz, Renee Danzeisen, Gwen Carver, Salvatore J. Siciliano, Martin S. Springer, Joseph Kessler, Daria J. Hazuda, Sander G. Mills, Julie A. DeMartino, Bruce L. Daugherty, Janet Lineberger, William A. Schleif, Emilio A. Emini, Bryan Oates, Anthony Carella, Laura C. Meurer, Sandra L. Gould, Paul E. Finke
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 11:265-270
(2S)-2-(3,4-Dichlorophenyl)-1-[N-(methyl)-N-(phenylsulfonyl)amino]-4-[spiro(2,3-dihydrobenzthiophene-3,4'-piperidin-1'-yl)]butane S-oxide (3) has been identified as a potent CCR5 antagonist lead structure having an IC50 = 35 nM. Herein, we describe t
Autor:
Moorthy S. S. Palanki, Bin Liu, John Rizzo, Curt Bradshaw, Abhijit Bhat, Nebojsa Stankovic, Rodney W. Lappe, Bryan Oates
Publikováno v:
Bioorganicmedicinal chemistry letters. 22(13)
We have developed modified maleimide novel linkers with improved chemical stability that could potentially be used in conjugating various pharmacophores such as oligo nucleotides, peptides, and proteins to antibodies to afford novel biologics with we
Autor:
Kristen E Bower, Ryan Preston, Emily Corner, Robert E. Murphy, Arvind G. Kinhikar, Xia Cao, Zemeda W Ainekulu, Aakash B Datt, Steven Pirie-Shepherd, Lioudmila Campbell, Gang Chen, Venkata Doppalapudi, Joselyn Del Rosario, Hanhua Huang, Bryan Oates, Rodney W. Lappe, Son Lam, Trina Osothprarop, Nancy Levin, Curt Bradshaw, Gary Woodnutt, Julie A Hoye, Judith Jimenez
Publikováno v:
Journal of medicinal chemistry. 54(5)
Novel phage-derived peptides are the first reported molecules specifically targeting human placental growth factor 1 (PlGF-1). Phage data enabled peptide modifications that decreased IC(50) values in PlGF-1/VEGFR-1 competition ELISA from 100 to 1 μM
Autor:
Karen Holmes, Charles G. Caldwell, Salvatore J. Siciliano, Renee Danzeisen, Joseph Kessler, Julie A. DeMartino, Martin S. Springer, Ping Chen, William A. Schleif, Shrenik K. Shah, Michael D. Miller, Daria J. Hazuda, Sander G. Mills, Gwen Carver, Kothandaraman Shankaran, Malcolm MacCoss, Janet Lineberger, Lorraine Malkowitz, Karla L. Donnelly, Anthony Carella, Sandra L. Gould, Emilio A. Emini, Paul E. Finke, Gloria Kwei, Bryan Oates
Publikováno v:
Bioorganicmedicinal chemistry letters. 14(13)
Cellular proliferation of HIV-1 requires the cooperative assistance of both the CCR5 and CD4 receptors. Our medicinal chemistry efforts in this area have resulted in the identification of N-alkyl piperidine sulfones as CCR5 antagonists. These compoun
Autor:
Shrenik K. Shah, Julie A. DeMartino, Lorraine Malkowitz, Bryan Oates, Jennifer L. Loebach, Sandra L. Gould, Laura C. Meurer, Martin S. Springer, Malcolm MacCoss, Paul E. Finke, Laurie A. Castonguay, Sander G. Mills
Publikováno v:
Bioorganicmedicinal chemistry letters. 11(18)
Structure-activity relationship studies directed toward the optimization of (2S)-2-(3-chlorophenyl)-1-[N-(methyl)-N-(phenylsulfonyl)amino]-4-[4-(substituted)piperidin-1-yl]butanes as CCR5 antagonists resulted in the synthesis of the spiro-indanone de