TARGETID

T93105

FORMERID

TTDR00444

UNIPROID

PSN1_HUMAN

TARGNAME

Presenilin 1 (PSEN1)

GENENAME

PSEN1

TARGTYPE

Clinical trial target

SYNONYMS

S182 protein; Protein S182; Presenilin-1; PSNL1; PS1; PS-1; AD3

FUNCTION

Requires the presence of the other members of the gamma-secretase complex for protease activity. Plays a role in Notch and Wnt signaling cascades and regulation of downstream processes via its role in processing key regulatory proteins, and by regulating cytosolic CTNNB1 levels. Stimulates cell-cell adhesion via its interaction with CDH1; this stabilizes the complexes between CDH1 (E-cadherin) and its interaction partners CTNNB1 (beta-catenin), CTNND1 and JUP (gamma-catenin). Under conditions of apoptosis or calcium influx, cleaves CDH1. This promotes the disassembly of the complexes between CDH1 and CTNND1, JUP and CTNNB1, increases the pool of cytoplasmic CTNNB1, and thereby negatively regulates Wnt signaling. Required for normal embryonic brain and skeleton development, and for normal angiogenesis. Mediates the proteolytic cleavage of EphB2/CTF1 into EphB2/CTF2. The holoprotein functions as a calcium-leak channel that allows the passive movement of calcium from endoplasmic reticulum to cytosol and is therefore involved in calcium homeostasis. Involved in the regulation of neurite outgrowth. Is a regulator of presynaptic facilitation, spike transmission and synaptic vesicles replenishment in a process that depends on gamma-secretase activity. It acts through the control of SYT7 presynaptic expression. Catalytic subunit of the gamma-secretase complex, an endoprotease complex that catalyzes the intramembrane cleavage of integral membrane proteins such as Notch receptors and APP (amyloid-beta precursor protein).

PDBSTRUC

6IYC; 6IDF; 5FN5; 5FN4; 5FN3

BIOCLASS

Peptidase

ECNUMBER

EC 3.4.23.-

SEQUENCE

MTELPAPLSYFQNAQMSEDNHLSNTVRSQNDNRERQEHNDRRSLGHPEPLSNGRPQGNSRQVVEQDEEEDEELTLKYGAKHVIMLFVPVTLCMVVVVATIKSVSFYTRKDGQLIYTPFTEDTETVGQRALHSILNAAIMISVIVVMTILLVVLYKYRCYKVIHAWLIISSLLLLFFFSFIYLGEVFKTYNVAVDYITVALLIWNFGVVGMISIHWKGPLRLQQAYLIMISALMALVFIKYLPEWTAWLILAVISVYDLVAVLCPKGPLRMLVETAQERNETLFPALIYSSTMVWLVNMAEGDPEAQRRVSKNSKYNAESTERESQDTVAENDDGGFSEEWEAQRDSHLGPHRSTPESRAAVQELSSSILAGEDPEERGVKLGLGDFIFYSVLVGKASATASGDWNTTIACFVAILIGLCLTLLLLAIFKKALPALPISITFGLVFYFATDYLVQPFMDQLAFHQFYI

DRUGINFO

(S)-FLURBIPROFEN

DRUGINFO

R-flurbiprofen

DRUGINFO

(2S,3R)-2-(benzyloxy)-3-methoxycyclohexanone

DRUGINFO

(5R,6S)-5,6-bis(benzyloxy)cyclohex-2-enone

DRUGINFO

(5R,6S)-6-(benzyloxy)-5-methoxycyclohex-2-enone

DRUGINFO

1-benzoyl-2-benzyl-1,2-dihydropyridin-3(6H)-one

DRUGINFO

1-Chloro-4-(1-phenyl-cyclohexanesulfonyl)-benzene

DRUGINFO

Drug 311383