Zobrazeno 1 - 10
of 18
pro vyhledávání: '"Ana S. Newton"'
Autor:
Sean P. Henry, Maria-Elena Liosi, Joseph A. Ippolito, Kara J. Cutrona, Stefan G. Krimmer, Ana S. Newton, Joseph Schlessinger, William L. Jorgensen
Publikováno v:
ACS Med Chem Lett
[Image: see text] The Janus kinase 2 (JAK2) pseudokinase domain (JH2) is an ATP-binding domain that regulates the activity of the catalytic tyrosine kinase domain (JH1). Dysregulation of JAK2 JH1 signaling caused by the V617F mutation in JH2 is impli
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a2a2477b4edebc570513fb94f2dc0c2c
https://doi.org/10.1021/acsmedchemlett.2c00051
https://doi.org/10.1021/acsmedchemlett.2c00051
Autor:
Sean P. Henry, Maria-Elena Liosi, Joseph A. Ippolito, Fabian Menges, Ana S. Newton, Joseph Schlessinger, William L. Jorgensen
Publikováno v:
ACS medicinal chemistry letters. 13(11)
Probe molecules that covalently modify the JAK2 pseudokinase domain (JH2) are reported. Selective targeting of JH2 domains over the kinase (JH1) domains is a necessary feature for ligands intended to evaluate JH2 domains as therapeutic targets. The J
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5511873d3b241a20174a4df6248fdcd7
https://pubmed.ncbi.nlm.nih.gov/36385940
https://pubmed.ncbi.nlm.nih.gov/36385940
Autor:
Maria-Elena Liosi, Joseph A. Ippolito, Sean P. Henry, Stefan G. Krimmer, Ana S. Newton, Kara J. Cutrona, Rene A. Olivarez, Jyotidarsini Mohanty, Joseph Schlessinger, William L. Jorgensen
Publikováno v:
J Med Chem
JAK2 is a non-receptor tyrosine kinase that regulates hematopoiesis through the JAK-STAT pathway. The pseudokinase domain (JH2) is an important regulator of the activity of the kinase domain (JH1). V617F mutation in JH2 has been associated with the p
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bcd684b9cfa095978eecbe7070dc39fa
https://europepmc.org/articles/PMC9939005/
https://europepmc.org/articles/PMC9939005/
Autor:
William L. Jorgensen, Karen S. Anderson, Marcus Bosenberg, Nicole Bertoletti, John C. Faver, Shalley N. Kudalkar, Ana S. Newton, Goran Micevic, Viswanathan Muthusamy
Publikováno v:
ACS Med Chem Lett
[Image: see text] Methyltransferase 3 beta (DNMT3B) inhibitors that interfere with cancer growth are emerging possibilities for treatment of melanoma. Herein we identify small molecule inhibitors of DNMT3B starting from a homology model based on a DN
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::91ff05797b4634806193edaab54c7bd6
https://doi.org/10.1021/acsmedchemlett.0c00011
https://doi.org/10.1021/acsmedchemlett.0c00011
Autor:
Patrick Fitzgerald, Jessica Freeze, Ana S. Newton, Dennis J. Jakiela, Jessica A. Martin, Clorice R. Reinhardt
Publikováno v:
Journal of Chemical Education
The New Haven Local Section of the American Chemical Society held a virtual version of its annual Student Research Symposium prompted by the COVID-19 pandemic. A combination of YouTube, Google Drive, Open Broadcaster Software, and Zoom was utilized t
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::477c1e7634889d71c352c8583399b287
Publikováno v:
J Chem Inf Model
With standard scoring methods, top-ranked compounds from virtual screening by docking often turn out to be inactive. For this reason, Metadynamics, a method used for sampling rare events, was studied to further evaluate docking poses with the aim of
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2abe23c995ba42ff2b8ec903632889a6
https://europepmc.org/articles/PMC7927942/
https://europepmc.org/articles/PMC7927942/
Autor:
Thomas K. Dawson, S.G. Krimmer, Maria-Elena Liosi, Kara J. Cutrona, Ana S. Newton, David E. Puleo, Joseph Schlessinger, Yoshihisa Suzuki, William L. Jorgensen
Publikováno v:
J Med Chem
Janus kinases (JAKs) are non-receptor tyrosine kinases that are essential components of the JAK-STAT signaling pathway. Associated aberrant signaling is responsible for many forms of cancer and disorders of the immune system. The present focus is on
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4147c54acb04879d3ac21b985bb19a75
https://europepmc.org/articles/PMC7949251/
https://europepmc.org/articles/PMC7949251/
Autor:
Sean P. Henry, Joseph Schlessinger, Ana S. Newton, Maria-Elena Liosi, John C. Faver, William L. Jorgensen, S.G. Krimmer, Luca Deiana, David E. Puleo
Publikováno v:
Tetrahedron Lett
Small molecules that selectively bind to the pseudokinase JH2 domain over the JH1 kinase domain of JAK2 kinase are sought. Virtual screening led to the purchase of 17 compounds among which 9 were found to bind to V617F JAK2 JH2 with affinities of 40
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e209b41f18875b8e5be9d836830e8c7b
https://doi.org/10.1016/j.tetlet.2021.153248
https://doi.org/10.1016/j.tetlet.2021.153248
Autor:
Henrik Hammaren, William L. Jorgensen, David E. Puleo, Daniela Ungureanu, Joseph Schlessinger, Olli Silvennoinen, Kaury Kucera, Ana S. Newton
Publikováno v:
ACS Medicinal Chemistry Letters. 8:618-621
Janus kinases (JAKs) regulate hematopoiesis via the cytokine-mediated JAK-STAT signaling pathway. JAKs contain tandem C-terminal pseudokinase (JH2) and tyrosine kinase (JH1) domains. The JAK2 pseudokinase domain adopts a protein kinase fold and, desp
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::928a2aa7e8b23aa679b5c49cb5f38e32
https://doi.org/10.1021/acsmedchemlett.7b00153
https://doi.org/10.1021/acsmedchemlett.7b00153
Autor:
José A. Cisneros, Joseph Schlessinger, Kara J. Cutrona, Luca Deiana, William L. Jorgensen, David E. Puleo, Ana S. Newton
Publikováno v:
ACS Medicinal Chemistry Letters. 8:614-617
A competitive fluorescence polarization (FP) assay is reported for determining binding affinities of probe molecules with the pseudokinase JAK2 JH2 allosteric site. The syntheses of the fluorescent 5 and 6 used in the assay are reported as well as Kd
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::90d96713a7e4bb7cc07181bcbe4e03b1
https://doi.org/10.1021/acsmedchemlett.7b00154
https://doi.org/10.1021/acsmedchemlett.7b00154