Novel Crizotinib-GnRH Conjugates Revealed the Significance of Lysosomal Trapping in GnRH-Based Drug Delivery Systems.
Carcinoma, Non-Small-Cell Lung
/ metabolism
Cell Line, Tumor
Cell Membrane Permeability
/ drug effects
Cell Survival
Crizotinib
/ chemical synthesis
Drug Delivery Systems
Drug Design
Fibroblasts
/ metabolism
Galectins
/ metabolism
Gonadotropin-Releasing Hormone
/ chemical synthesis
Humans
Hydrogen-Ion Concentration
Lung Neoplasms
/ metabolism
Lysosomes
/ metabolism
Models, Biological
Proto-Oncogene Mas
Proto-Oncogene Proteins c-met
/ antagonists & inhibitors
Receptors, LHRH
/ metabolism
Skin
/ cytology
GnRH 2
GnRHR 3
NSCLC 7
c-Met 8
conjugate 6
crizotinib 5
endocytosis 9
galectin 10
lysosome 3
permeability 4
targeted drug delivery 1
Journal
International journal of molecular sciences
ISSN: 1422-0067
Titre abrégé: Int J Mol Sci
Pays: Switzerland
ID NLM: 101092791
Informations de publication
Date de publication:
08 Nov 2019
08 Nov 2019
Historique:
received:
30
09
2019
accepted:
06
11
2019
entrez:
14
11
2019
pubmed:
14
11
2019
medline:
14
4
2020
Statut:
epublish
Résumé
Several promising anti-cancer drug-GnRH (gonadotropin-releasing hormone) conjugates have been developed in the last two decades, although none of them have been approved for clinical use yet. Crizotinib is an effective multi-target kinase inhibitor, approved against anaplastic lymphoma kinase (ALK)- or ROS proto-oncogene 1 (ROS-1)-positive non-small cell lung carcinoma (NSCLC); however, its application is accompanied by serious side effects. In order to deliver crizotinib selectively into the tumor cells, we synthesized novel crizotinib analogues and conjugated them to a [d-Lys
Identifiants
pubmed: 31717403
pii: ijms20225590
doi: 10.3390/ijms20225590
pmc: PMC6888004
pii:
doi:
Substances chimiques
Galectins
0
MAS1 protein, human
0
Proto-Oncogene Mas
0
Receptors, LHRH
0
Gonadotropin-Releasing Hormone
33515-09-2
Crizotinib
53AH36668S
Proto-Oncogene Proteins c-met
EC 2.7.10.1
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Subventions
Organisme : Nemzeti Kutatási, Fejlesztési és Innovaciós Alap
ID : NVKP_16-1-2016-0005
Organisme : Nemzeti Kutatási, Fejlesztési és Innovaciós Alap
ID : "K-124813
Organisme : Nemzeti Kutatási, Fejlesztési és Innovaciós Alap
ID : K-128785
Organisme : Nemzeti Kutatási, Fejlesztési és Innovaciós Alap
ID : GINOP-2.3.2-15-2016-00043
Organisme : Emberi Eroforrások Minisztériuma
ID : 20428-3/2018/FEKUTSTRAT
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