Cargando…

FLT3 inhibitor design using molecular docking based virtual screening for acute myeloid leukemia

Acute Myeloid Leukaemia (AML) is a blood cancer, which affects the red blood cells in the bone marrow. Of the possible proteins that are affected in AML, fms-like tyrosine kinase 3 (FLT3) has long been recognized as a potential therapeutic target as it affects the other signaling pathways and leads...

Descripción completa

Detalles Bibliográficos
Autores principales: Gokhale, Padmini, Chauhan, Aashish Pratap Singh, Arora, Anushka, Khandekar, Natasha, Nayarisseri, Anuraj, Singh, Sanjeev Kumar
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Biomedical Informatics 2019
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6677903/
https://www.ncbi.nlm.nih.gov/pubmed/31435156
http://dx.doi.org/10.6026/97320630015104
_version_ 1783440978336546816
author Gokhale, Padmini
Chauhan, Aashish Pratap Singh
Arora, Anushka
Khandekar, Natasha
Nayarisseri, Anuraj
Singh, Sanjeev Kumar
author_facet Gokhale, Padmini
Chauhan, Aashish Pratap Singh
Arora, Anushka
Khandekar, Natasha
Nayarisseri, Anuraj
Singh, Sanjeev Kumar
author_sort Gokhale, Padmini
collection PubMed
description Acute Myeloid Leukaemia (AML) is a blood cancer, which affects the red blood cells in the bone marrow. Of the possible proteins that are affected in AML, fms-like tyrosine kinase 3 (FLT3) has long been recognized as a potential therapeutic target as it affects the other signaling pathways and leads to a cascade of events. First-generation inhibitors sorafenib and midostaurin, as well as secondgeneration agents such as quizartinib and crenolanib are known. It is of interest to identify new compounds against FLT3 with improved activity using molecular docking and virtual screening. Molecular docking of existing inhibitors selected a top scoring bestestablished candidate Quizartinib having PubChem CID: 24889392. Similarity searching resulted in compound XGIQBUNWFCCMASUHFFFAOYSA-NPubChemCID: 44598530 which shows higher affinity scores. A comparative study of both the compounds using a drug-drug comparison, ADMET studies, boiled egg plot and pharmacophore parameters and properties confirmed the result and predicted the ligand to be an efficient inhibitor of FLT3.
format Online
Article
Text
id pubmed-6677903
institution National Center for Biotechnology Information
language English
publishDate 2019
publisher Biomedical Informatics
record_format MEDLINE/PubMed
spelling pubmed-66779032019-08-21 FLT3 inhibitor design using molecular docking based virtual screening for acute myeloid leukemia Gokhale, Padmini Chauhan, Aashish Pratap Singh Arora, Anushka Khandekar, Natasha Nayarisseri, Anuraj Singh, Sanjeev Kumar Bioinformation Research Article Acute Myeloid Leukaemia (AML) is a blood cancer, which affects the red blood cells in the bone marrow. Of the possible proteins that are affected in AML, fms-like tyrosine kinase 3 (FLT3) has long been recognized as a potential therapeutic target as it affects the other signaling pathways and leads to a cascade of events. First-generation inhibitors sorafenib and midostaurin, as well as secondgeneration agents such as quizartinib and crenolanib are known. It is of interest to identify new compounds against FLT3 with improved activity using molecular docking and virtual screening. Molecular docking of existing inhibitors selected a top scoring bestestablished candidate Quizartinib having PubChem CID: 24889392. Similarity searching resulted in compound XGIQBUNWFCCMASUHFFFAOYSA-NPubChemCID: 44598530 which shows higher affinity scores. A comparative study of both the compounds using a drug-drug comparison, ADMET studies, boiled egg plot and pharmacophore parameters and properties confirmed the result and predicted the ligand to be an efficient inhibitor of FLT3. Biomedical Informatics 2019-02-28 /pmc/articles/PMC6677903/ /pubmed/31435156 http://dx.doi.org/10.6026/97320630015104 Text en © 2019 Biomedical Informatics http://creativecommons.org/licenses/by/3.0/ This is an Open Access article which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly credited. This is distributed under the terms of the Creative Commons Attribution License.
spellingShingle Research Article
Gokhale, Padmini
Chauhan, Aashish Pratap Singh
Arora, Anushka
Khandekar, Natasha
Nayarisseri, Anuraj
Singh, Sanjeev Kumar
FLT3 inhibitor design using molecular docking based virtual screening for acute myeloid leukemia
title FLT3 inhibitor design using molecular docking based virtual screening for acute myeloid leukemia
title_full FLT3 inhibitor design using molecular docking based virtual screening for acute myeloid leukemia
title_fullStr FLT3 inhibitor design using molecular docking based virtual screening for acute myeloid leukemia
title_full_unstemmed FLT3 inhibitor design using molecular docking based virtual screening for acute myeloid leukemia
title_short FLT3 inhibitor design using molecular docking based virtual screening for acute myeloid leukemia
title_sort flt3 inhibitor design using molecular docking based virtual screening for acute myeloid leukemia
topic Research Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6677903/
https://www.ncbi.nlm.nih.gov/pubmed/31435156
http://dx.doi.org/10.6026/97320630015104
work_keys_str_mv AT gokhalepadmini flt3inhibitordesignusingmoleculardockingbasedvirtualscreeningforacutemyeloidleukemia
AT chauhanaashishpratapsingh flt3inhibitordesignusingmoleculardockingbasedvirtualscreeningforacutemyeloidleukemia
AT aroraanushka flt3inhibitordesignusingmoleculardockingbasedvirtualscreeningforacutemyeloidleukemia
AT khandekarnatasha flt3inhibitordesignusingmoleculardockingbasedvirtualscreeningforacutemyeloidleukemia
AT nayarisserianuraj flt3inhibitordesignusingmoleculardockingbasedvirtualscreeningforacutemyeloidleukemia
AT singhsanjeevkumar flt3inhibitordesignusingmoleculardockingbasedvirtualscreeningforacutemyeloidleukemia