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...
Autores principales: | , , , , , |
---|---|
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 |