Proceeding of the 4
th
International Conference on Bioscience and Biotechnology, Vol. 4, 2019, pp. 11-15
Copyright © 2019 TIIKM
ISSN 2513-2695 online
DOI: https://doi.org/10.17501/25132695.2019.4102
Corresponding Author Email: *mfbhatti@asab.nust.edu.pk
STRUCTURAL CHARACTERIZATION OF NPAS4-ARNT
DIMERIZATION THROUGH COMPUTATIONAL
SIMULATION
Ammad Fahim
1
, Zaira Rehman
1
, Muhammad Faraz Bhatti*
1
, Nasar Virk
1
, Rehan
Zafar Paracha
2
1
Atta-ur-Rahman School of Applied Biosciences (ASAB), National University of Sciences & Technology
(NUST), Islamabad, Pakistan
2
Research Centre of Modeling and Simulation (RCMS), National University of Sciences & Technology (NUST),
Islamabad, Pakistan
Abstract: Neuronal PAS Domain Protein 4 (Npas4) is an activity dependent transcription factor
harboring basic helix-loop-helix (bHLH)-PAS domain, mediating the expression of target genes
involved in neuro-transmission. NPAS4 crucially regulates response to various excitatory stimuli and
has a role in GABAergic neuronal synapse development. Functionally, NPAS4 as a transcription
factor dimerizes with the ARNT protein to serve as complete transcription factor and start the
transcription of downstream genes. However, NPAS4 dimerization characteristics with ARNT has
not been studied so far. Hence the current study aimed to identify the interaction pattern of NPAS4-
ARNT complex through computational docking via HADDOCK. The interaction pattern were
determined through pdbSum. The electrostatic surface calculations were performed through APBS
plugins in PyMOL. The results indicated that PASB domain of NPAS4 is involved in interactions
with the PAS B domain of ARNT. A toll of 136 structures generated by HADDOCK were further
grouped into 14 clusters. The cluster with the minimum energy value of -82.6 KJ/mol was then
further selected for interaction analysis. The results showed that there is one salt bridge, 12 H-
bonding interactions and 156 non-bonded contacts between two proteins. The important interactions
among two proteins are Asp224:NPAS4 and Gln421:ARNT, Asp229:NPAS4 and Ser442:ARNT,
Glu232:NPAS4 and Thr361:ARNT, Phe240, Glu241:NPAS4, and Arg440:ARNT. The electrostatic
potential of these two proteins revealed the binding interface of NPAS4 and ARNT to be neutral
hence favoring hydrophobic interactions. The findings can help elucidate Npas4 role in interacting
with other neuronal proteins involved in neuronal signaling. Moreover, the interaction findings
provide useful comparative insight with other bHLH proteins.
Keywords: NPAS4, bHLH proteins, dimerization, neurotransmission, molecular simulation
Introduction
NPAS4 is an immediate-early gene (IEG) which encodes a transcription factor specific to neurons. This
transcription factor is involved in regulation of expression of a large number of genes that mediate diverse
effects on synapses. It plays an important role as an early transcription factor which induces late response gene
expression in both excitatory and inhibitory neurons. Structurally, NPAS4 belongs to basic Helix-Loop-Helix
(HLH) PAS protein family. This protein is specific to, and is highly expressed in brain in response to excitatory
activity in the synapse [1]. NPAS4 protein expression is partially induced by calcium influx in neurons. This
protein is particularly important in development and repair of inhibitory synapses where it regulates the
expression of genes depending on the activity of neuron. These activity-dependent genes are involved in
controlling the number of GABA-releasing synapses formed on excitatory neurons. Inhibitory pathways require
a balance between neuronal excitation and inhibition [2]. NPAS4 transcription factor regulate the expression of
genes which participate in maintaining this balance. NPAS4 regulates and balances the modification of synapses
formed on excitatory and inhibitory neurons according to their function within the neuronal circuit. In excitatory
neurons NPAS4 promotes BDNF gene expression which controls GABA releasing synapses and increases
number of inhibitory synapse formed on excitatory neurons. In inhibitory neurons NPAS4 promotes expression
of genes which increase feedback inhibition thereby increasing excitatory input in inhibitory neurons [3]. This