Next-Generation JAK2 Inhibitors for the Treatment of Myeloproliferative Neoplasms: Lessons from Structure-Based Drug Discovery Approaches
DC Element | Wert | Sprache |
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dc.contributor.author | Nair, Pramod C. | |
dc.contributor.author | Piehler, Jacob | |
dc.contributor.author | Tvorogov, Denis | |
dc.contributor.author | Ross, David M. | |
dc.contributor.author | Lopez, Angel F. | |
dc.contributor.author | Gotlib, Jason | |
dc.contributor.author | Thomas, Daniel | |
dc.date.accessioned | 2024-01-04T10:28:45Z | - |
dc.date.available | 2024-01-04T10:28:45Z | - |
dc.date.issued | 2023 | |
dc.identifier.issn | 2643-3230 | |
dc.identifier.uri | http://osnascholar.ub.uni-osnabrueck.de/handle/unios/72895 | - |
dc.description | Cited by: 0; All Open Access, Green Open Access | |
dc.description.abstract | Selective inhibitors of Janus kinase (JAK) 2 have been in demand since the discovery of the JAK2 V617F mutation present in patients with myeloproliferative neoplasms (MPN); however, the structural basis of V617F oncogenicity has only recently been elucidated. New structural studies reveal a role for other JAK2 domains, beyond the kinase domain, that contribute to pathogenic signaling. Here we evaluate the structure-based approaches that led to recently-approved type I JAK2 inhibitors (fedratinib and pacritinib), as well as type II (BBT594 and CHZ868) and pseudokinase inhibitors under development (JNJ7706621). With full-length JAK homodimeric structures now available, superior selective and mutation-specific JAK2 inhibitors are foreseeable. © 2023 American Association for Cancer Research. | |
dc.language.iso | en | |
dc.publisher | American Association for Cancer Research Inc. | |
dc.relation.ispartof | Blood Cancer Discovery | |
dc.subject | Drug Discovery | |
dc.subject | Humans | |
dc.subject | Janus Kinase 2 | |
dc.subject | Janus Kinase Inhibitors | |
dc.subject | Mutation | |
dc.subject | Myeloproliferative Disorders | |
dc.subject | Neoplasms | |
dc.subject | deucravacitinib | |
dc.subject | fedratinib | |
dc.subject | Janus kinase 2 inhibitor | |
dc.subject | pacritinib | |
dc.subject | ruxolitinib | |
dc.subject | JAK2 protein, human | |
dc.subject | Janus kinase 2 | |
dc.subject | Janus kinase inhibitor | |
dc.subject | antineoplastic activity | |
dc.subject | drug design | |
dc.subject | drug structure | |
dc.subject | high throughput screening | |
dc.subject | human | |
dc.subject | JAK-STAT signaling | |
dc.subject | kinase assay | |
dc.subject | myeloproliferative neoplasm | |
dc.subject | Review | |
dc.subject | drug development | |
dc.subject | genetics | |
dc.subject | mutation | |
dc.subject | myeloproliferative disorder | |
dc.subject | neoplasm | |
dc.title | Next-Generation JAK2 Inhibitors for the Treatment of Myeloproliferative Neoplasms: Lessons from Structure-Based Drug Discovery Approaches | |
dc.type | review | |
dc.identifier.doi | 10.1158/2643-3230.BCD-22-0189 | |
dc.identifier.scopus | 2-s2.0-85169502726 | |
dc.identifier.url | https://www.scopus.com/inward/record.uri?eid=2-s2.0-85169502726&doi=10.1158%2f2643-3230.BCD-22-0189&partnerID=40&md5=c3722184c96209b22a04f33ef60b0dec | |
dc.description.volume | 4 | |
dc.description.issue | 5 | |
dc.description.startpage | 352 – 364 | |
dcterms.isPartOf.abbreviation | Blood Cancer Discov. | |
local.import.remains | affiliations : Cancer Program, South Australian Health and Medical Research Institute (SAHMRI), University of Adelaide, Adelaide, Australia; Discipline of Medicine, Adelaide Medical School, The University of Adelaide, Adelaide, Australia; Discipline of Clinical Pharmacology, Flinders Health and Medical Research Institute (FHMRI) Cancer Program, College of Medicine and Public Health, Flinders University, Adelaide, Australia; Department of Biology, Center of Cellular Nanoanalytics, University of Osnabrück, Osnabrück, Germany; Centre for Cancer Biology, University of South Australia, SA Pathology, Adelaide, Australia; Department of Hematology and Bone Marrow Transplantation, Royal Adelaide Hospital, Adelaide, SA, Australia; Stanford Cancer Institute, Stanford University, School of Medicine, Stanford, CA, United States | |
local.import.remains | correspondence_address : D. Thomas; Cancer Program, Precision Medicine Theme, South Australian Health and Medical Research Institute (SAHMRI), University of Adelaide, Adelaide, Australia; email: daniel.thomas@adelaide.edu.au; P.C. Nair; Discipline of Clinical Pharmacology, Flinders Medical Centre, College of Medicine, Public Health Flinders University, Adelaide, Australia; email: pramod.nair@flinders.edu.au | |
local.import.remains | pmid : 37498362 | |
local.import.remains | publication_stage : Final | |
crisitem.author.dept | FB 05 - Biologie/Chemie | - |
crisitem.author.deptid | fb05 | - |
crisitem.author.orcid | 0000-0002-2143-2270 | - |
crisitem.author.parentorg | Universität Osnabrück | - |
crisitem.author.netid | PiJa938 | - |
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geprüft am 18.05.2024