Id: acc2422
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: TPCA
Drug Info: "TPCA-1 is a potent and selective inhibitor of IKK-2 (IC50 = 17.9 nM) that also suppresses STAT3 phosphorylation, DNA binding, and transactivation, demonstrating antitumor and anti-inflammatory effects in preclinical models."
Effect: modulate
Effect Info: "SMAC mimetics or IKK inhibitors can also disrupt the phosphorylation of CYLD and lead to the death of ATLL cells by reducing the ubiquitination of RIPK1, which is CYLD - dependent."
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: