Id: acc2420
Group: 2sens
Protein: RIPK1
Gene Symbol: RIPK1
Protein Id: Q13546
Protein Name: RIPK1_HUMAN
PTM: ubiquitination
Site: unclear
Site Sequence:
Disease Category: Cancer
Disease: Leukemia
Disease Subtype: Adult T-cell leukemia/lymphoma
Disease Cellline: MT4
Disease Info:
Drug: MRT67307
Drug Info: "MRT67307 is a dual inhibitor of IKKepsilon and TBK-1 with IC50 values of 160 nM and 19 nM, respectively, in vitro (at 0.1 mM ATP), and also effectively inhibits ULK1 and ULK2 with IC50 values of 45 nM and 38 nM."
Effect: modulate
Effect Info: "SMAC mimetics or IKK inhibitors also disrupt the phosphorylation of CYLD and lead to the death of ATLL cells by reducing the ubiquitination of RIPK1, which is dependent on CYLD."
Note:
Score: 4.0
Pubmed(PMID): 32024820
Sentence Index:
Sentence:

Sequence & Structure:

MQPDMSLNVIKMKSSDFLESAELDSGGFGKVSLCFHRTQGLMIMKTVYKGPNCIEHNEALLEEAKMMNRLRHSRVVKLLGVIIEEGKYSLVMEYMEKGNLMHVLKAEMSTPLSVKGRIILEIIEGMCYLHGKGVIHKDLKPENILVDNDFHIKIADLGLASFKMWSKLNNEEHNELREVDGTAKKNGGTLYYMAPEHLNDVNAKPTEKSDVYSFAVVLWAIFANKEPYENAICEQQLIMCIKSGNRPDVDDITEYCPREIISLMKLCWEANPEARPTFPGIEEKFRPFYLSQLEESVEEDVKSLKKEYSNENAVVKRMQSLQLDCVAVPSSRSNSATEQPGSLHSSQGLGMGPVEESWFAPSLEHPQEENEPSLQSKLQDEANYHLYGSRMDRQTKQQPRQNVAYNREEERRRRVSHDPFAQQRPYENFQNTEGKGTAYSSAASHGNAVHQPSGLTSQPQVLYQNNGLYSSHGFGTRPLDPGTAGPRVWYRPIPSHMPSLHNIPVPETNYLGNTPTMPFSSLPPTDESIKYTIYNSTGIQIGAYNYMEIGGTSSSLLDSTNTNFKEEPAAKYQAIFDNTTSLTDKHLDPIRENLGKHWKNCARKLGFTQSQIDEIDHDYERDGLKEKVYQMLQKWVMREGIKGATVGKLAQALHQCSRIDLLSSLIYVSQN

Select PDB:

Known Drugs:

source: Multi-Sources

(see table)

Target Drug name MOA Phase Status Disease Source
RIPK1 GSK2982772 Receptor-interacting serine/threonine-protein kinase 1 inhibitor 2 Completed psoriasis ClinicalTrials
RIPK1 GSK2982772 Receptor-interacting serine/threonine-protein kinase 1 inhibitor 2 Completed rheumatoid arthritis ClinicalTrials
RIPK1 GSK2982772 Receptor-interacting serine/threonine-protein kinase 1 inhibitor 2 Completed ulcerative colitis ClinicalTrials
RIPK1 GSK2982772 Receptor-interacting serine/threonine-protein kinase 1 inhibitor 1 Completed immune system disease ClinicalTrials
ClinicalTrials
ClinicalTrials
ClinicalTrials
RIPK1 GSK2982772 Receptor-interacting serine/threonine-protein kinase 1 inhibitor 1 Completed psoriasis ClinicalTrials
RIPK1 GSK2982772 Receptor-interacting serine/threonine-protein kinase 1 inhibitor 1 Completed inflammatory bowel disease ClinicalTrials

Note: Only show clinically investigational or approved drugs with protein targets.

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 data.

PTM-Disease Association:

source: PTMD
Residue Position State Disease Class PMID
- - D Colon cancer Phosphorylation 35022391
- - U Glioblastoma Ubiquitination 22585859
- - U Breast cancer/tumor/carcinoma Ubiquitination 18570872
- - U Ovarian cancer/carcinoma Ubiquitination 18570872

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: