PMADS

Id:	acc0568
Group:	1sens
Protein:	DRP1
Gene Symbol:	DNM1L
Protein Id:	O00429
Protein Name:	DNM1L_HUMAN
PTM:	phosphorylation
Site:	Ser637
Site Sequence:	VPVPVARKLSAREQRDCEVIE
Disease Category:	Cancer
Disease:	Breast Cancer
Disease Subtype:
Disease Cellline:	MCF7
Disease Info:
Drug:	silibinin
Drug Info:	"Silibinin is a flavonoid compound derived from milk thistle, primarily used in the treatment of liver toxicity and liver diseases, such as drug-induced liver injury and chronic hepatitis with fatty liver."
Effect:	modulate
Effect Info:	Silibinin downregulates the expression of p-DRP1 and increases cell apoptosis.
Note:
Score:	4.0
Pubmed(PMID):	31085166
Sentence Index:	31085166_9
Sentence:	"In addition, silibinin treatment down-regulates ATP content as well as the levels of mitochondrial biogenesis-regulators including mitochondrial transcription factor A, peroxisome proliferator-activated receptor gamma coactivator 1 and nuclear respiratory factor 2. Moreover, treatments with DRP1 inhibitor, mdivi-1, or with DRP1-targetted siRNA efficiently prevent silibinin-induced apoptosis in the breast cancer cells, whereas inhibition of DRP1 phosphorylation with staurosporine increases apoptosis furthermore."

Sequence & Structure:

MEALIPVINKLQDVFNTVGADIIQLPQIVVVGTQSSGKSSVLESLVGRDLLPRGTGIVTRRPLILQLVHVSQEDKRKTTGEENGVEAEEWGKFLHTKNKLYTDFDEIRQEIENETERISGNNKGVSPEPIHLKIFSPNVVNLTLVDLPGMTKVPVGDQPKDIELQIRELILRFISNPNSIILAVTAANTDMATSEALKISREVDPDGRRTLAVITKLDLMDAGTDAMDVLMGRVIPVKLGIIGVVNRSQLDINNKKSVTDSIRDEYAFLQKKYPSLANRNGTKYLARTLNRLLMHHIRDCLPELKTRINVLAAQYQSLLNSYGEPVDDKSATLLQLITKFATEYCNTIEGTAKYIETSELCGGARICYIFHETFGRTLESVDPLGGLNTIDILTAIRNATGPRPALFVPEVSFELLVKRQIKRLEEPSLRCVELVHEEMQRIIQHCSNYSTQELLRFPKLHDAIVEVVTCLLRKRLPVTNEMVHNLVAIELAYINTKHPDFADACGLMNNNIEEQRRNRLARELPSAVSRDKSSKVPSALAPASQEPSPAASAEADGKLIQDSRRETKNVASGGGGVGDGVQEPTTGNWRGMLKTSKAEELLAEEKSKPIPIMPASPQKGHAVNLLDVPVPVARKLSAREQRDCEVIERLIKSYFLIVRKNIQDSVPKAVMHFLVNHVKDTLQSELVGQLYKSSLLDDLLTESEDMAQRRKEAADMLKALQGASQIIAEIRETHLW

Select PDB:

Known Drugs:

source: Multi-Sources

(see table)

No data.

Protein Tractability:

source: Open Targets

Small molecule

Antibody

PROTAC

Other modalities

Approved Drug

Advanced Clinical

Phase 1 Clinical

Structure with Ligand

High-Quality Ligand

High-Quality Pocket

Med-Quality Pocket

Druggable Family

Approved Drug

Advanced Clinical

Phase 1 Clinical

UniProt loc high conf

GO CC high conf

UniProt loc med conf

UniProt SigP or TMHMM

GO CC med conf

Human Protein Atlas loc

Approved Drug

Advanced Clinical

Phase 1 Clinical

Literature

UniProt Ubiquitination

Database Ubiquitination

Half-life Data

Small Molecule Binder

Approved Drug

Advanced Clinical

Phase 1 Clinical

PTM Intensity:

source: CPTAC

No intensity data of this site,
show all other sites!

DNM1L-Ser119
Cancer	Intensity
BRCA	-1.07
COAD
HGSC
ccRCC
GBM
HNSC
LUAD	0.158
LUSC	0.912
non_ccRCC
PDAC
UCEC

DNM1L-Ser529
Cancer	Intensity
BRCA	-0.744
COAD	-0.927
HGSC	0.877
ccRCC	-0.002
GBM
HNSC	-0.913
LUAD	-0.487
LUSC	-0.073
non_ccRCC	2.346
PDAC	-0.379
UCEC	0.302

DNM1L-Ser548
Cancer	Intensity
BRCA
COAD
HGSC
ccRCC	0.179
GBM
HNSC	0.838
LUAD	0.17
LUSC	0.339
non_ccRCC	-2.211
PDAC	0.333
UCEC	0.351

DNM1L-Ser561
Cancer	Intensity
BRCA
COAD
HGSC
ccRCC	-0.707
GBM	0.707
HNSC
LUAD
LUSC
non_ccRCC
PDAC
UCEC

DNM1L-Ser605
Cancer	Intensity
BRCA	-0.268
COAD	-0.646
HGSC	1.985
ccRCC	-0.267
GBM
HNSC	-0.535
LUAD	-0.334
LUSC	-0.929
non_ccRCC	1.431
PDAC	-0.436
UCEC

PTM-Disease Association:

source: PTMD

Residue	Position	State	Disease	Class	PMID
S	637	D	Nasopharyngeal carcinoma	Phosphorylation	32433544
S	637	U	Glioblastoma multiforme	Phosphorylation	35697672

State Note: Based on the distinct PTM states in diseases, PTMD classified all disease-associated PTMs into six classes, including whether the up-regulation (U) or down-regulation (D) of PTM levels, the absence (A) or presence (P) of PTMs, and the creation (C) or disruption (N) of PTM sites are associated with diseases.

PTM-Drug Perturbation Response:

source: DecryptM

No data.

Function score:

source: funscoR

No data.

Cross Links:

CTD
DMRdb