Zobrazeno 1 - 10
of 41
pro vyhledávání: '"Gretchen M, Schroeder"'
Autor:
Emily C. Cherney, Liping Zhang, Julian Lo, Tram Huynh, Donna Wei, Vijay Ahuja, Claude Quesnelle, Gary L. Schieven, Alan Futran, Gregory A. Locke, Zeyu Lin, Laura Monereau, Charu Chaudhry, Jordan Blum, Sha Li, Mark Fereshteh, Bifang Li-Wang, Sanjeev Gangwar, Chin Pan, Colin Chong, Xiao Zhu, Shana L. Posy, John S. Sack, Ping Zhang, Max Ruzanov, Mary Harner, Fahad Akhtar, Gretchen M. Schroeder, Gregory Vite, Brian Fink
Publikováno v:
Journal of Medicinal Chemistry. 65:3518-3538
Autor:
Edgars Jecs, Yesim A. Tahirovic, Robert J. Wilson, Eric J. Miller, Michelle Kim, Valarie Truax, Huy H. Nguyen, Nicholas S. Akins, Manohar Saindane, Tao Wang, Chi S. Sum, Mary E. Cvijic, Gretchen M. Schroeder, Samantha L. Burton, Cynthia A. Derdeyn, Lingjie Xu, Yi Jiang, Lawrence J. Wilson, Dennis C. Liotta
Publikováno v:
Journal of medicinal chemistry. 65(5)
Our first-generation CXCR4 antagonist TIQ15 was rationally modified to improve drug-like properties. Introducing a nitrogen atom into the aromatic portion of the tetrahydroisoquinoline ring led to several heterocyclic variants including the 5,6,7,8-t
Autor:
Chi S. Sum, Yi Jiang, Yesim Altas Tahirovic, Lingjie Xu, Dennis C. Liotta, Michelle B. Kim, Nicholas S. Akins, Lawrence J. Wilson, Huy Nguyen, Mary Ellen Cvijic, Gretchen M. Schroeder, Tao Wang, Valarie M. Truax, Robert Wilson, Eric J. Miller, Edgars Jecs
Publikováno v:
ACS Med Chem Lett
[Image: see text] This work surveys a variety of diamino-heterocycles as an isosteric replacement for the piperazine substructure of our previously disclosed piperarinyl-tetrahydroisoquinoline containing CXCR4 antagonists. A late-stage Buchwald coupl
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fd15efbdf4f13c7f5fae15f6ab98bdb6
https://europepmc.org/articles/PMC8521655/
https://europepmc.org/articles/PMC8521655/
Autor:
Chi S. Sum, Christopher J. Butch, Lawrence J. Wilson, Katie M. Kuo, Michelle B. Kim, Yesim Altas Tahirovic, Mary Ellen Cvijic, Huy Nguyen, Dennis C. Liotta, Tao Wang, Robert Wilson, Valarie M. Truax, Eric J. Miller, Gretchen M. Schroeder, Edgars Jecs
Publikováno v:
Journal of Medicinal Chemistry. 61:7168-7188
CXCR4 is a G-protein-coupled receptor that interacts with its cognate ligand, CXCL12, to synchronize many physiological responses and pathological processes. Disruption of the CXCL12-CXCR4 circuitry by small-molecule antagonists has emerged as a prom
Autor:
Mary Ellen Cvijic, Katie M. Kuo, Chi S. Sum, Lawrence J. Wilson, Tao Wang, Yesim Altas Tahirovic, Valarie M. Truax, Eric J. Miller, Michelle B. Kim, Robert Wilson, Dennis C. Liotta, Gretchen M. Schroeder, Edgars Jecs, Huy Nguyen
Publikováno v:
ACS Medicinal Chemistry Letters. 9:446-451
[Image: see text] A novel series of CXCR4 antagonists with piperidinyl and piperazinyl alkylamine side chains designed as butyl amine replacements are described. Several of these compounds showed similar activity to the parent compound TIQ-15 (5) in
Autor:
Chi S. Sum, Katie M. Kuo, Dennis C. Liotta, Tao Wang, Lawrence J. Wilson, Eric J. Miller, Brook M. Katzman, Gretchen M. Schroeder, Mary Ellen Cvijic, Edgars Jecs, Robert Wilson, Huy Nguyen, Valarie M. Truax, Michelle B. Kim, Yesim Altas Tahirovic
Publikováno v:
ACS Medicinal Chemistry Letters. 9:89-93
A structure–activity relationship study of potent TIQ15-derived CXCR4 antagonists is reported. In this investigation, the TIQ15 side-chain was constrained to improve its drug properties. The cyclohexylamino congener 15a was found to be a potent CXC
Autor:
Robert Wilson, Michelle B. Kim, Edgars Jecs, Katie M. Kuo, Anthony A. Paiva, Dennis C. Liotta, Yesim Altas Tahirovic, Tao Wang, Huy Nguyen, Lawrence J. Wilson, Valarie M. Truax, Gretchen M. Schroeder, Mary Ellen Cvijic, Eric J. Miller, Chi Shing Sum
Publikováno v:
ACS Medicinal Chemistry Letters. 9:17-22
CXCR4 is the most common chemokine receptor expressed on the surface of many cancer cell types. In comparison to normal cells, cancer cells overexpress CXCR4, which correlates with cancer cell metastasis, angiogenesis, and tumor growth. CXCR4 antagon
Autor:
Yong Zhang, Madeleine Héroux, Bryan Cox, Brooke M Katzman, Brigitte Murat, Lawrence J. Wilson, Anthony R. Prosser, Ana A. Alcaraz, Dennis C. Liotta, Andrew J. Tebben, Gretchen M. Schroeder, James P. Snyder
[Image: see text] The rationale for the structural and mechanistic basis of a tetrahydroisoquinoline (THIQ) based series of CXCR4 antagonists is presented. Using the previously reported crystal structures which reveal two distinct binding sites of CX
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ed94921ea08225465c7be2c6bdcf6758
https://europepmc.org/articles/PMC6331156/
https://europepmc.org/articles/PMC6331156/
Autor:
Edgars Jecs, Dennis C. Liotta, Eric J. Miller, Katie M. Kuo, Gretchen M. Schroeder, Manohar Saindane, Huy Nguyen, Huanyu Zhao, Robert Wilson, Mary Ellen Cvijic, Brooke M Katzman, Tao Wang, Lawrence J. Wilson, Chi S. Sum, Valarie M. Truax, Yesim Altas Tahirovic, Michelle B. Kim
Publikováno v:
Journal of medicinal chemistry. 61(3)
CXCR4 is a seven-transmembrane receptor expressed by hematopoietic stem cells and progeny, as well as by ≥48 different cancers types. CXCL12, the only chemokine ligand of CXCR4, is secreted within the tumor microenvironment, providing sanctuary for
Autor:
Hart Amy C, Javed Khan, Grebinski James W, James Kempson, Jonathan Lippy, Gretchen M. Schroeder, Theresa M. McDevitt, Ashok V. Purandare, Ragini Vuppugalla, John S. Tokarski, George L. Trainor, Junqing Guo, Jennifer Inghrim, Matthew V. Lorenzi, Dan You, Honghe Wan, John S. Sack, William J. Pitts, Yueping Zhang, Louis J. Lombardo
Publikováno v:
ACS Medicinal Chemistry Letters. 6:845-849
Early hit to lead work on a pyrrolopyridine chemotype provided access to compounds with biochemical and cellular potency against Janus kinase 2 (JAK2). Structure-based drug design along the extended hinge region of JAK2 led to the identification of a