Zobrazeno 1 - 10
of 18
pro vyhledávání: '"Edgars Jecs"'
Autor:
Perry W. Bartsch, Julien Sourimant, Thalia Le, Edgars Jecs, Nicole Pribut, Richard K. Plemper, Stephen C. Pelly, Robert Wilson, Zackery W. Dentmon, Savita Sharma, Pieter B. Burger, Jeong-Joong Yoon, Dennis C. Liotta, Thomas M. Kaiser, Soyon S. Hwang
Publikováno v:
ACS Infect Dis
A series of five benzimidazole-based compounds were identified using a machine learning algorithm as potential inhibitors of the respiratory syncytial virus (RSV) fusion protein. These compounds were synthesized, and compound 2 in particular exhibite
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f4cce3380433cbafe8e4064585046da3
https://doi.org/10.1021/acsinfecdis.9b00524
https://doi.org/10.1021/acsinfecdis.9b00524
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b393ed15a5b53abcfd5ac6f12274c8e4
https://pubmed.ncbi.nlm.nih.gov/35179893
https://pubmed.ncbi.nlm.nih.gov/35179893
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:
Eric J. Miller, Carrie Q. Sun, Petra Gregorova, Edgars Jecs, Yesim Altas Tahirovic, Robert J. Wilson, Huy H. Nguyen, Savita K. Sharma, Perry Bartsch, Zachary Sticher, Levi Moellering, Priscilla Davidson, Ryan Jajosky, Michael D'Erasmo, Manohar Saindane, Zafer Sahin, Nicholas S. Akins, Alexander A. Kolykhalov, Lawrence Wilson, Rebecca S. Arnold, John A. Petros, Haydn Kissick, Lingjie Xu, Yi Jiang, Dennis C. Liotta
Publikováno v:
Cancer Research. 82:2649-2649
Purpose: Pro-angiogenic and immune cells expressing chemokine receptor CXCR4 traffic along concentration gradients of the chemokine ligand CXCL12, which disseminates from stromal niches. The CXCR4/CXCL12 axis is hijacked by various cancer types chara
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::1d27eabc5a921f9e628cb90e2d983ea4
https://doi.org/10.1158/1538-7445.am2022-2649
https://doi.org/10.1158/1538-7445.am2022-2649
Autor:
Edgars Jecs, Savita Sharma, Yesim Altas Tahirovic, Dennis C. Liotta, Sameshnee Pelly, Lawrence J. Wilson, Eric J. Miller
Publikováno v:
Expert opinion on therapeutic patents. 30(2)
Introduction: The chemokine receptor CXCR4 has been under intense study due to the central role it plays in immune system regulation and the pathology of many human diseases. The FDA approval of the first CXCR4 antagonist drug Plerixafor (i.e. AMD310
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d582df6a81801f39fd69e4f26b0955bc
https://pubmed.ncbi.nlm.nih.gov/31854208
https://pubmed.ncbi.nlm.nih.gov/31854208
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::79aa355fc7e64b8be28843fa21520a33
https://doi.org/10.1021/acs.jmedchem.8b00450
https://doi.org/10.1021/acs.jmedchem.8b00450
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e1fb137ea8c246121b4acf7a962577b6
https://doi.org/10.1021/acsmedchemlett.8b00030
https://doi.org/10.1021/acsmedchemlett.8b00030
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c37978d1c82bb13605d9185553329f15
https://doi.org/10.1021/acsmedchemlett.7b00406
https://doi.org/10.1021/acsmedchemlett.7b00406
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::96a63b4e56550407b42f2c8d00cabfb8
https://doi.org/10.1021/acsmedchemlett.7b00381
https://doi.org/10.1021/acsmedchemlett.7b00381
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e663423d25f58ab1e46b1fb7d16462bc
https://pubmed.ncbi.nlm.nih.gov/29350534
https://pubmed.ncbi.nlm.nih.gov/29350534