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1. WO2022005179 - BLOOD-BRAIN BARRIER PENETRATING APTAMER, AND USE THEREOF

Publication Number WO/2022/005179
Publication Date 06.01.2022
International Application No. PCT/KR2021/008212
International Filing Date 29.06.2021
IPC
C12N 15/115 2010.1
CCHEMISTRY; METALLURGY
12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
NMICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
15Mutation or genetic engineering; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification; Use of hosts therefor
09Recombinant DNA-technology
11DNA or RNA fragments; Modified forms thereof
115Aptamers, i.e. nucleic acids binding a target molecule specifically and with high affinity without hybridising therewith
A61K 47/18 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
16containing nitrogen
18Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
Applicants
  • 주식회사 압타머사이언스 APTAMER SCIENCES INC. [KR]/[KR]
Inventors
  • 김윤동 KIM, Youndong
  • 이다솜 LEE, Da Som
  • 김소연 KIM, Soyeon
  • 임소령 LIM, So Ryong
  • 신의수 SHIN, Euisu
  • 강나예 KANG, Naye
  • 한동일 HAN, Dongil
Agents
  • 특허법인한얼 HANOL INTELLECTUAL PROPERTY AND LAW
Priority Data
10-2020-007949529.06.2020KR
10-2021-008237424.06.2021KR
Publication Language Korean (ko)
Filing Language Korean (KO)
Designated States
Title
(EN) BLOOD-BRAIN BARRIER PENETRATING APTAMER, AND USE THEREOF
(FR) APTAMÈRE PÉNÉTRANT DANS LA BARRIÈRE HÉMATO-ENCÉPHALIQUE, ET SON UTILISATION
(KO) 혈액-뇌 장벽 침투 압타머 및 이의 이용
Abstract
(EN) The present invention relates to an aptamer penetrating the blood-brain barrier (BBB) to enable receptor-mediated transcytosis, and a use thereof. The aptamer of the present invention selectively targets transferrin receptor proteins only, rapidly passes through BBB by means of receptor-mediated transcytosis, can effectively transport and deliver various therapeutic agents such as proteins, antibodies, nucleic acids and low molecular weight compounds through simple chemical bonds, exhibits interspecific cross-reactivity in transferrin receptors, and is easily chemically modified, and thus is applicable as a drug carrier for nervous system diseases, especially brain and central nervous system diseases.
(FR) La présente invention concerne un aptamère pénétrant dans la barrière hémato-encéphalique (BHE) pour permettre une transcytose médiée par un récepteur, et son utilisation. L'aptamère selon la présente invention cible sélectivement les protéines du récepteur de la transferrine uniquement, traverse rapidement la BHE au moyen d'une transcytose médiée par un récepteur, peut transporter et administrer efficacement divers agents thérapeutiques tels que des protéines, des anticorps, des acides nucléiques et des composés de faible poids moléculaire via des liaisons chimiques simples, présente une réactivité croisée interspécifique dans les récepteurs de la transferrine, et est facilement modifié chimiquement, et peut donc être utilisé comme véhicule pour médicament pour des maladies du système nerveux, en particulier des maladies du cerveau et du système nerveux central.
(KO) 본 발명은 혈액-뇌 장벽(Blood-brain barrier, BBB)에 침투하여 수용체 매개성 내재화(receptor-mediated transcytosis)가 가능한 압타머 및 이의 이용에 관한 것이다. 본 발명의 압타머는 트랜스페린 수용체(Transferrin receptor) 단백질만을 선택적으로 타겟팅하고, 수용체 매개 세포 내재화를 통해 BBB를 빠르게 통과하고, 단순한 화학적 결합을 통해 단백질, 항체, 핵산 및 저분자 화합물 등 다양한 치료제를 효율적으로 수송 및 전달할 수 있으며, 종 간 트랜스페린 수용체에서 교차 반응을 나타내며, 화학적 변형이 쉬운 바, 신경계 질환, 특히 뇌 및 중추 신경계 질환에서 약물 전달체로 적용할 수 있다.
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