178685-33-1Relevant articles and documents
Targeted Delivery of a Mannose-Conjugated BODIPY Photosensitizer by Nanomicelles for Photodynamic Breast Cancer Therapy
Zhang, Quan,Cai, Ying,Li, Qiu-Yan,Hao, Lin-Na,Ma, Zheng,Wang, Xiao-Jun,Yin, Jian
, p. 14307 - 14315 (2017)
The targeted delivery of a photosensitizer (PS) with appropriate carriers represents an attractive means of selectively delivering cargo to target tissues or subcellular compartments for photodynamic therapy (PDT). Herein, a three-arm distyryl BODIPY derivative conjugated with mannose units (denoted by BTM) that can co-assemble with Tween 80 to form nanomicelles (BTM-NMs) for targeted PDT is reported. MDA-MB-231 breast cancer cells recognized and specifically internalized BTM-NMs via mannose-receptor-mediated endocytosis with preferential accumulation in the lysosomes. These NMs could disassemble in cell lysosomes and subsequently induce highly efficient singlet oxygen (1O2) generation upon light irradiation. 1O2 disrupted the lysosomal membrane and promoted the escape of BTM from the lysosome into the cytoplasm, thereby resulting in the efficient and selective killing of cancer cells through PDT. This study may provide a new strategy for designing targeted PDT systems to fight cancer.
Novel unit B cryptophycin analogues as payloads for targeted therapy
Figueras, Eduard,Borbély, Adina,Ismail, Mohamed,Frese, Marcel,Sewald, Norbert
, p. 1281 - 1286 (2018)
Cryptophycins are naturally occurring cytotoxins with great potential for chemotherapy. Since targeted therapy provides new perspectives for treatment of cancer, new potent analogues of cytotoxic agents containing functional groups for conjugation to homing devices are required. We describe the design, synthesis and biological evaluation of three new unit B cryptophycin analogues. The O-methyl group of the unit B D-tyrosine analogue was replaced by an O-(allyloxyethyl) moiety, an O-(hydroxyethyl) group, or an O-(((azidoethoxy)ethoxy)ethoyxethyl) substituent. While the former two maintain cytotoxicity in the subnanomolar range, the attachment of the triethylene glycol spacer with a terminal azide results in a complete loss of activity. Docking studies of the novel cryptophycin analogues to β-tubulin provided a rationale for the observed cytotoxicities.
Synthesis and preliminary evaluation of a 18F-labeled ethisterone derivative [18F]EAEF for progesterone receptor targeting
Wu, Xiaowei,You, Linyi,Zhang, Deliang,Gao, Mengna,Li, Zijing,Xu, Duo,Zhang, Pu,Huang, Lumei,Zhuang, Rongqiang,Wu, Hua,Zhang, Xianzhong
, p. 559 - 565 (2017)
To develop a novel progesterone receptor-targeting probe for positron emission tomography imaging, an ethisterone derivative [18F]EAEF was designed and prepared in high decay-corrected radiochemical yield (30–35%) with good radiochemical purity (>98%). [18F]EAEF is a lipophilic tracer (logP?=?0.53?±?0.06) with very good stability in saline and serum. In the biodistribution study, high radioactivity accumulation of [18F]EAEF were found in uterus (5.73?±?1.83% ID/g) and ovary (4.05?±?0.73% ID/g) at 2?hr postinjection (p.i.), which have high progesterone receptor expression after treated with estradiol, while the muscle background has very low uptake (0.50?±?0.17% ID/g). For positron emission tomography imaging, [18F]EAEF showed high uptake in progesterone receptor-positive MCF-7 tumor (3.15?±?0.07% ID/g at 2?hr p.i.) with good tumor to muscle ratio (2.90), and obvious lower tumor uptakes were observed in MCF-7 with EAEF blocking (1.84?±?0.05% ID/g at 2?hr p.i.) or in progesterone receptor-negative MDA-MB-231 tumor (1.80?±?0.03% ID/g at 2?hr p.i.). Based on the good stability and specificity of [18F]EAEF, it may be a good candidate for imaging progesterone receptor and worth further investigation.
Carbonic Anhydrase Inhibitors Featuring a Porphyrin Scaffold: Synthesis, Optical and Biological Properties
Clément, Sébastien,Gary-Bobo, Magali,Gerbier, Philippe,Merabti, Amina,Nguyen, Christophe,Nocentini, Alessio,Richeter, Sébastien,Roger, Maxime,Supuran, Claudiu T.,Winum, Jean-Yves
, (2022/02/19)
The synthesis, characterization and study of optical properties of innovative tetrafunctionalized zinc(II) porphyrins with carbonic anhydrase (CA) inhibitors in sulfonamide and coumarin series are described. The synthetic methodology relies on the prepara
CELL SURFACE RECEPTOR BINDING COMPOUNDS AND CONJUGATES
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Paragraph 001166-001168, (2021/07/17)
The present disclosure provides a class of compounds including a ligand moiety that specifically binds to a cell surface receptor, such as a mannose-6-phosphate receptor (M6PR) or a cell surface asialoglycoprotein receptor (ASGPR). The cell surface M6PR or ASGPR binding compounds can trigger the receptor to internalize into the cell a bound compound. The ligand moieties of this disclosure can be linked to a variety of moieties of interest without impacting the specific binding to, and function of, the cell surface receptor, e.g., M6PR or ASGPR. Also provided are compounds that are conjugates of the ligand moieties linked to a biomolecule, such as an antibody, which conjugates can harness cellular pathways to remove specific proteins of interest from the cell surface or from the extracellular milieu. Also provided are methods of using the conjugates to target a polypeptide of interest for sequestration and/or lysosomal degradation.
Compound for degrading TGF-beta1 through targeted ubiquitination, and preparation method and application thereof
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Paragraph 0053-0059, (2020/09/20)
The invention discloses a compound (I) for targeted ubiquitination degradation of TGF-beta1. The compound (I) for degradation of TGF-beta1 through targeted ubiquitination is formed by connecting a TGF-beta1 micromolecular ligand and an E3 ubiquitin ligase
