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Record W2771770874 · doi:10.1109/bibm.2017.8217665

Retrieval of promiscuous natural compounds using multiple targets docking strategy: A case study on kinase polypharmacology

2017· article· en· W2771770874 on OpenAlexaff
Chirag Patel, Siva Kumar Prasanth Kumar, Himanshu Pandya, Krunal Modi, Daxesh P. Patel, Frank J. Gonzalez

Bibliographic record

Venuenot available
Typearticle
Languageen
FieldChemistry
TopicQuinazolinone synthesis and applications
Canadian institutionsImpact
FundersUniversity Grants Commission
KeywordsProtein Data Bank (RCSB PDB)Docking (animal)ImatinibVirtual screeningTyrosine kinaseProtein Data BankIn silicoChemistryProtein kinase AComputational biologyImatinib mesylateDrug discoveryKinaseBiochemistryBiologyProtein structureCancer researchSignal transductionMedicine

Abstract

fetched live from OpenAlex

Cancer is a class of diseases characterized by out-of-control cell growth, which are the building blocks of the body. Imatinib, known by its brand-Gleevec, is a type of biological therapy called tyrosine kinase inhibitor (TKI) which, a chemical messenger, is protein that cells use to signal each other to grow and thus pro-motes cancer. Structure-based method includes inverse docking was used to anticipate of most probable protein targets of Imatinib from tyrosine kinase protein using in silico approaches. Seven tyrosine kinase proteins have been preferred for the docking evaluation. In which, re-docking was performed to evaluate the docking validation. Among them, Crystal structure of native c-Kit kinase in an auto inhibited conformation (PDB: 1T46), LCK bound to imatinib (PDB: 2PL0), P38 in complex with Imatinib/Transferase (PDB: 3HEC), and ABL kinase in complex with Imatinib and a fragment (FRAG1) in the myristate pocket (PDB: 3MS9) and were most potential protein targets for the Imatinib ligand which computed by both of these schemes. These validated proteins have been selected for the virtual library screening of 1500 natural compounds from NPACT database. Luxenchalcone, Schweinfurthin and Sanggenon M were the best docked ligands and have chosen for the understanding the plausible mechanism at molecular level by implying the molecular dynamics simulations to determine the conformational changes and stabilization which reveals the potency of these ligands towards the treatment of cancer treatment.

Fetched live from OpenAlex and de-inverted. Abstracts are not stored in this database: the inverted indexes are 8.6 GB of the frame’s 9.3 GB of text, and the host has 13 GB free.

How this classification was reachedexpand

Full frame distilled prediction

Teacher imitation

Not calibrated prevalence, not ground truth. Human validation pending. Learned from the 10,348 direct Codex labels and 10,348 direct Gemma labels. Candidate is the union of thresholded teacher heads; consensus is their intersection. These outputs are machine_predicted_unvalidated and are not human labels or direct frontier model labels.

metaresearch head score (Codex)0.000
metaresearch head score (Gemma)0.000
Version: codex-gemma-dda1882f352aValidation status: machine_predicted_unvalidated
Candidate categoriesnone
Consensus categoriesnone
DomainCandidate signal: none · Consensus signal: none
Study designCandidate signal: Bench or experimental · Consensus signal: Bench or experimental
GenreCandidate signal: Empirical · Consensus signal: Empirical
Teacher disagreement score0.019
Threshold uncertainty score0.654

Codex and Gemma teacher scores by category

CategoryCodexGemma
Metaresearch0.0000.000
Meta-epidemiology (narrow)0.0000.000
Meta-epidemiology (broad)0.0000.000
Bibliometrics0.0000.000
Science and technology studies0.0010.000
Scholarly communication0.0000.000
Open science0.0000.000
Research integrity0.0000.000
Insufficient payload (model declined to judge)0.0000.000

Machine scores (provisional)

The two teacher heads of the student model, read on this work. A score orders the frame for review; it never asserts a category, and the validation status ships verbatim with every row.

Baseline scores from an immature model (maturity gate not passed, 7 training rounds). Scores rank; they never assert a category.

Opus teacher head0.066
GPT teacher head0.361
Teacher spread0.296 · how far apart the two teachers sit on this one work
Validation statusscore_only:v0-immature-baseline · verbatim from the scoring run: score_only means the number may rank works, and no category label ships from it

Classification

machine, unvalidated

Machine predicted; a candidate call from one teacher head, not a consensus.

The models applied no category: nothing in the taxonomy fit this work.
Study designBench or experimental
Domainnot available
GenreEmpirical

How this classification was reached, model by model and score by score, is at the end of the page under "How this classification was reached".

Quick stats

Citations7
Published2017
Admission routes1
Has abstractyes

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