Blockade of Oncogenic NOTCH1 with the SERCA Inhibitor CAD204520 in T Cell Acute Lymphoblastic Leukemia.
Animals
Antineoplastic Agents
/ chemical synthesis
Cell Line, Tumor
Cell Proliferation
/ drug effects
Drug Screening Assays, Antitumor
Enzyme Inhibitors
/ chemical synthesis
Female
Humans
Male
Mice
Mice, Inbred BALB C
Mice, Inbred ICR
Mice, Inbred NOD
Mice, SCID
Molecular Structure
Mutation
Neoplasms, Experimental
/ drug therapy
Precursor T-Cell Lymphoblastic Leukemia-Lymphoma
/ drug therapy
Receptor, Notch1
/ antagonists & inhibitors
Signal Transduction
/ drug effects
CAD204520
NOTCH1
NOTCH1 mutation
P-type ATPases screening
PEST mutation
SERCA
T cell acute lymphoblastic leukemia (T-ALL)
crystal structure
mantle cell lymphoma (MCL)
thapsigargin
Journal
Cell chemical biology
ISSN: 2451-9448
Titre abrégé: Cell Chem Biol
Pays: United States
ID NLM: 101676030
Informations de publication
Date de publication:
18 06 2020
18 06 2020
Historique:
received:
04
07
2019
revised:
14
02
2020
accepted:
31
03
2020
pubmed:
11
5
2020
medline:
7
7
2021
entrez:
11
5
2020
Statut:
ppublish
Résumé
The identification of SERCA (sarco/endoplasmic reticulum calcium ATPase) as a target for modulating gain-of-function NOTCH1 mutations in Notch-dependent cancers has spurred the development of this compound class for cancer therapeutics. Despite the innate toxicity challenge associated with SERCA inhibition, we identified CAD204520, a small molecule with better drug-like properties and reduced off-target Ca
Identifiants
pubmed: 32386594
pii: S2451-9456(20)30116-1
doi: 10.1016/j.chembiol.2020.04.002
pmc: PMC7305996
mid: NIHMS1582168
pii:
doi:
Substances chimiques
Antineoplastic Agents
0
Enzyme Inhibitors
0
NOTCH1 protein, human
0
Receptor, Notch1
0
Types de publication
Journal Article
Research Support, N.I.H., Extramural
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
678-697.e13Subventions
Organisme : NCI NIH HHS
ID : R35 CA210030
Pays : United States
Informations de copyright
Copyright © 2020 Elsevier Ltd. All rights reserved.
Déclaration de conflit d'intérêts
Author Contributions Conceptualization and Design, M.M., A.G., W.D.-B., A.-M.L.W., M.B., and G.R.; Methodology, all authors; Resources, all authors; Investigation, all authors; Formal Analysis, all authors; Writing – Original Draft, W.D.-B., A.-M.L.W., M.M., M.B., and G.R.; Writing – Review & Editing, W.D.-B., A.-M.L.W., M.M., M.B., and G.R.; Data Curation, W.D.-B., A.-M.L.W., P.S., R.L.S., C.M., F.A., K.S., M.B., and G.R. Funding Acquisition, P.S., C.M., R.L.S., K.S., M.M., and G.R.; Project Administration, M.M. and G.R.; Supervision, G.R. Declaration of Interests W.D.-B. and A.-M.L.W. are CaDo Biotechnology IvS employees. The compounds studied are part of a patent application wholly owned by CaDo Biotechnology IvS, Denmark. K.S. has previously consulted for Novartis and Rigel Pharmaceuticals and currently receives grant funding from Novartis on topics unrelated to this manuscript.
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