New chemical adaptor unit designed to release a drug from a tumor targeting device by enzymatic triggering

Anna Gopin; Christoph Rader; Doron Shabat

doi:10.1016/j.bmc.2004.01.041

New chemical adaptor unit designed to release a drug from a tumor targeting device by enzymatic triggering

Anna Gopin
, Christoph Rader
, Doron Shabat^*

^*Corresponding author for this work

School of Chemistry

Research output: Contribution to journal › Article › peer-review

25 Scopus citations

Abstract

A new controlled drug delivery system for selective chemotherapy was developed. It is based on a chemical adaptor unit, that releases a drug by a spontaneous cyclization mechanism after cleavage of an enzymatic substrate. It also provides a generic linkage of a drug with a targeting device in a manner set to be triggered by defined enzymatic activity. The system is generic and allows using a variety of drugs, targeting devices, and enzymes by introducing the corresponding substrate as a trigger for drug release in the chemical adaptor.

Original language	English
Pages (from-to)	1853-1858
Number of pages	6
Journal	Bioorganic and Medicinal Chemistry
Volume	12
Issue number	8
DOIs	https://doi.org/10.1016/j.bmc.2004.01.041
State	Published - 15 Apr 2004

Keywords

1-[3-(dimethylamino)propyl]-3- ethylcarbodiimide
9-fluorenylmethoxycarbonyl
Boc-t-buthyl carbonate
DIPEA
DMAP
DMF
Diisopropyl ethyl amine
Dimethyl aminopyridine
Dimethyl formamide
EDC
EtN
EtOAc
Ethyl acetate
Fmoc
He
N-Hexane
Triethyl amine

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10.1016/j.bmc.2004.01.041

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title = "New chemical adaptor unit designed to release a drug from a tumor targeting device by enzymatic triggering",

abstract = "A new controlled drug delivery system for selective chemotherapy was developed. It is based on a chemical adaptor unit, that releases a drug by a spontaneous cyclization mechanism after cleavage of an enzymatic substrate. It also provides a generic linkage of a drug with a targeting device in a manner set to be triggered by defined enzymatic activity. The system is generic and allows using a variety of drugs, targeting devices, and enzymes by introducing the corresponding substrate as a trigger for drug release in the chemical adaptor.",

keywords = "1-[3-(dimethylamino)propyl]-3- ethylcarbodiimide, 9-fluorenylmethoxycarbonyl, Boc-t-buthyl carbonate, DIPEA, DMAP, DMF, Diisopropyl ethyl amine, Dimethyl aminopyridine, Dimethyl formamide, EDC, EtN, EtOAc, Ethyl acetate, Fmoc, He, N-Hexane, Triethyl amine",

author = "Anna Gopin and Christoph Rader and Doron Shabat",

year = "2004",

month = apr,

day = "15",

doi = "10.1016/j.bmc.2004.01.041",

language = "אנגלית",

volume = "12",

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journal = "Bioorganic and Medicinal Chemistry",

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T1 - New chemical adaptor unit designed to release a drug from a tumor targeting device by enzymatic triggering

AU - Gopin, Anna

AU - Rader, Christoph

AU - Shabat, Doron

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N2 - A new controlled drug delivery system for selective chemotherapy was developed. It is based on a chemical adaptor unit, that releases a drug by a spontaneous cyclization mechanism after cleavage of an enzymatic substrate. It also provides a generic linkage of a drug with a targeting device in a manner set to be triggered by defined enzymatic activity. The system is generic and allows using a variety of drugs, targeting devices, and enzymes by introducing the corresponding substrate as a trigger for drug release in the chemical adaptor.

AB - A new controlled drug delivery system for selective chemotherapy was developed. It is based on a chemical adaptor unit, that releases a drug by a spontaneous cyclization mechanism after cleavage of an enzymatic substrate. It also provides a generic linkage of a drug with a targeting device in a manner set to be triggered by defined enzymatic activity. The system is generic and allows using a variety of drugs, targeting devices, and enzymes by introducing the corresponding substrate as a trigger for drug release in the chemical adaptor.

KW - 1-[3-(dimethylamino)propyl]-3- ethylcarbodiimide

KW - 9-fluorenylmethoxycarbonyl

KW - Boc-t-buthyl carbonate

KW - DIPEA

KW - DMAP

KW - DMF

KW - Diisopropyl ethyl amine

KW - Dimethyl aminopyridine

KW - Dimethyl formamide

KW - EDC

KW - EtN

KW - EtOAc

KW - Ethyl acetate

KW - Fmoc

KW - He

KW - N-Hexane

KW - Triethyl amine

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U2 - 10.1016/j.bmc.2004.01.041

DO - 10.1016/j.bmc.2004.01.041

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AN - SCOPUS:1642543394

SN - 0968-0896

VL - 12

SP - 1853

EP - 1858

JO - Bioorganic and Medicinal Chemistry

JF - Bioorganic and Medicinal Chemistry

IS - 8

ER -

New chemical adaptor unit designed to release a drug from a tumor targeting device by enzymatic triggering

Abstract

Keywords

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