Delving into the Latest Updates on SEN-177 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target

QPCT x QPCTL

Mechanism

Glutaminyl-peptide cyclotransferase inhibitors, QPCTL inhibitors(glutaminyl-peptide cyclotransferase like inhibitors)

Therapeutic Areas

Nervous System DiseasesCongenital DisordersOther Diseases

Active Indication

Huntington Disease

Inactive Indication

Neoplasms

Originator Organization

Netherlands Cancer Insitute

Active Organization

Siena Biotech SpA

University of Cambridge

Cenix BioScience GmbH

Inactive Organization

Netherlands Cancer Insitute

Drug Highest PhasePreclinical

First Approval Date-

Regulation-

Recent evidence links the role of human glutaminyl cyclase (hQC) to the amyloidogenic process involved in Alzheimer's disease (AD). hQC is a zinc enzyme present in neuronal tissue and its activity is responsible for the cyclization of N-terminal Gln or Glu β-amyloid peptides, leading to N-pyroglutamic acid peptides (pE-Aβ) that is probably a crucial event in the initiation and progress of the disease. Indeed, pE-containing peptides exhibit an elevated neurotoxicity and a tendency to aggregate. These observations render hQC inhibition an attractive strategy for developing new molecules active against AD. We present here the crystal structure of hQC in complex with SEN177, a newly designed molecule. The SEN177-binding mode to hQC differs from that of the known hQC inhibitors. SEN177 K_i on hQC is 20 nM, comparable or better than that of the most potent known hQC inhibitors PBD150 and PQ912. In addition, SEN177 already demonstrated relevant pharmacological properties in in vivo models of Huntington's disease. All these properties make SEN177 an important scaffold for developing molecules acting on AD and related diseases.

100 Deals associated with SEN-177

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R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Huntington Disease	Preclinical	GB	University of Cambridge	06 Apr 2015
Huntington Disease	Preclinical	IT	Siena Biotech SpA	06 Apr 2015
Huntington Disease	Preclinical	DE	Cenix BioScience GmbH	06 Apr 2015
Neoplasms	Discovery	NL	Netherlands Cancer Insitute	31 Mar 2019