Asceneuron SA nhasi inozivisa kuburitswa kwedata rakaongororwa nevezera mujenari ACS Chemical Neuroscience maererano neASN90, O-GlcNAcase (OGA) inhibitor, uye mumwe wevanotungamira mukuvandudza kwekiriniki yekurapa neurodegenerative proteinopathies.
Neurodegenerative proteinopathies yakadai seAlzheimer's neParkinson's disease inoratidzirwa nekuumbwa kwe intracellular muuropi yekusanyungudika uye huturu hweprotein aggregates, senge microtubule-inosanganiswa neprotein tau uye α-synuclein zvichiteerana, iyo yakanyatsobatanidzwa nekufambira mberi kwechirwere. OGA ndiyo iri kubuda mishonga inonangwa mukati metsinga tsinga kugadzirwa kwezvinodhaka sezvo kushomeka kweglycosylation yeaya mapuroteni emukati memasero kwave kwakabatana neuronal dysfunction. OGA inhibitors inodzivirira kubviswa kwe intracellular protein glycosylation, zvichizomisa kudzikira kwehutano-nyika mazinga eiyi post-translation shanduko uye kudzivirira kuumbwa kwechepfu maprotein aggregates.
Mune iri richangoburwa, bepa rakatariswa nevezera, Asceneuron inoshuma kuwanikwa kwekutanga uye kuvandudzwa kweinoveli diki molecule OGA inhibitor ASN90 (yaimbozivikanwa seASN120290/ASN561), iyo yakatopedza kuyedza muzvikamu zvitatu zveChikamu I mune vane hutano vadiki uye vakura zvidzidzo. . Iyo preclinical data inoratidza kuti zuva nezuva kutonga kwemuromo kweASN90 kwakadzivirira kuvandudzwa kwetau tangle pathology, pamwe nekushomeka kwekuita muhunhu hwemotokari uye kufema, uye kuwedzera kupona. Chimwe chinhu chakakosha kuwana; novel yekirasi iyi yemamorekuru; ndeyekuti ASN90 yakadzora kufambira mberi kwekukanganiswa kwemota uye kuderedza astrogliosis mune inowanzo shandiswa, preclinical modhi yechirwere cheParkinson.
Asceneuron parizvino ine yakavhurika yekuferefeta mushonga mutsva (IND) application neUS Food and Drug Association (FDA) yeChidzidzo cheChikamu 2/3 chekuongorora ASN90 muprogressive supranuclear palsy (PSP), chiratidzo chenherera. PSP chinhu chisingawanzoitiki chetsinga chinokonzera matambudziko akakomba nekufamba, kuenzanisa, kutaura, kumedza uye kuona semugumisiro wekuunganidzwa kwezvibatanidzwa zvetau protein muuropi. Chirwere ichi chiri kuramba chichiwedzera, vanhu vachiremara zvakaipisisa mukati memakore matatu kusvika mashanu kubva pakatanga. Zvinonzi vanhu vatatu kusvika vatanhatu pa100,000 XNUMX vachabatwa nePSP uye parizvino hapana mushonga wekurapa chirwere ichi.
Dirk Beher, Chief Executive Officer, Co-Muvambi weAsceneuron uye munyori mukuru wechidzidzo ichi, akati: "Tinofara zvikuru kuburitsa kiyi iyi inokurudzira data yepreclinical paASN90 uye OGA maitiro ekuita. Izvi zvakawanikwa zvinopa chikonzero chakasimba chekugadzirwa kweOGA inhibitors sevanogadzirisa zvirwere mune zvose tauopathies uye α-synucleinopathies yakadai seAlzheimer's, PSP, uye Parkinson's disease. Sezvo tau uye α-synuclein pathologies ichiwanzovapo muzvirwere zveurourodegenerative, OGA inhibitors inomiririra yakasarudzika, multimodal zvinodhaka vamiriri kune akawanda zviratidzo. Isu tinoenderera mberi nekufambira mberi kwekiriniki yedu neazvino kamwe pazuva OGA inhibitor, ASN51, iyo ichapihwa muvarwere veAlzheimer's disease mumwedzi iri kuuya. "
ZVOKUBVA MUNYAYA INO:
- Neurodegenerative proteinopathies such as Alzheimer’s and Parkinson’s disease are characterized by the intracellular formation in the brain of insoluble and toxic protein aggregates, such as the microtubule-associated protein tau and α-synuclein respectively, that are closely linked to disease progression.
- PSP is a rare neurological condition that causes severe problems with walking, balance, speech, swallowing and vision as a result of the accumulation of aggregates of the tau protein in the brain.
- In this recently published, peer-reviewed paper, Asceneuron reports the preclinical discovery and development of the novel small molecule OGA inhibitor ASN90 (formerly known as ASN120290/ASN561), which has already completed testing in three Phase I studies in healthy young and elderly subjects.
