Structural Insights into JAK2 Inhibition by Ruxolitinib, Fedratinib, and Derivatives Thereof-Reference-Cited by-同舟云学术

Structural Insights into JAK2 Inhibition by Ruxolitinib, Fedratinib, and Derivatives Thereof

Published:2021-02-11 Issue:4 Volume:64 Page:2228-2241
ISSN:0022-2623
Container-title:Journal of Medicinal Chemistry
language:en
Short-container-title:J. Med. Chem.

Author:

Davis Ryan R.¹,Li Baoli¹,Yun Sang Y.²,Chan Alice¹,Nareddy Pradeep¹,Gunawan Steven¹,Ayaz Muhammad²,Lawrence Harshani R.²^ORCID,Reuther Gary W.³,Lawrence Nicholas J.¹,Schönbrunn Ernst¹^ORCID

Affiliation:

1. Drug Discovery DepartmentMoffitt Cancer Center, Tampa, Florida 33612, United States

2. Chemical Biology Core, Moffitt Cancer Center, Tampa, Florida 33612, United States

3. Molecular Oncology Department, Moffitt Cancer Center, Tampa, Florida 33612, United States

Funder

National Cancer Institute

Bankhead-Coley Foundation

Leukemia and Lymphoma Society

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

Link

https://pubs.acs.org/doi/pdf/10.1021/acs.jmedchem.0c01952

Reference35 articles.

1. Cancer Genome Landscapes

2. Mechanistic Insights into Regulation of JAK2 Tyrosine Kinase

3. Targeting substrate-site in Jak2 kinase prevents emergence of genetic resistance

4. Heterodimeric JAK–STAT activation as a mechanism of persistence to JAK2 inhibitor therapy

5. Ruxolitinib Mediated Paradox JAK2 Hyperphosphorylation Is Due To The Protection Of Activation Loop Phosphotyrosines From Phosphatases

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