Insight into oral amphiphilic cyclodextrin nanoparticles for colorectal cancer: comprehensive mathematical model of drug release kinetic studies and antitumoral efficacy in 3D spheroid colon tumors

• Sedat Ünal,
• Gamze Varan,
• Juan M. Benito,
• Yeşim Aktaş and
• Erem Bilensoy

Beilstein J. Org. Chem. 2023, 19, 139–157, doi:10.3762/bjoc.19.14

• extensively investigated in new drug and gene delivery studies, particularly in cancer therapy, for targeted drug delivery, extended/controlled release, and improving cellular interaction [25][26][27][28][29]. Within the scope of this study, advanced studies were carried out for the oral polycationic nanodrug

Design, synthesis and biological evaluation of immunostimulating mannosylated desmuramyl peptides

• Rosana Ribić,
• Ranko Stojković,
• Lidija Milković,
• Mariastefania Antica,
• Marko Cigler and
• Srđanka Tomić

Beilstein J. Org. Chem. 2019, 15, 1805–1814, doi:10.3762/bjoc.15.174

• most suitable position of adamantane in this class of compounds is at the peptide N-terminus. Adamantane can act as membrane anchor for mannose structures and thus be exposed on liposome surfaces and as such used in targeted drug delivery [37]. It can be also incorporated into a β-cyclodextrine cavity

• , a powerful supramolecular nanoparticle carrier for targeted drug delivery [38]. Previous research suggested a design of mannosylated desmuramyl peptides with adamantane at the C-terminus in order to facilitate the incorporation into the hydrophobic layer of the cavity because of the minor steric

Polyaminoazide mixtures for the synthesis of pH-responsive calixarene nanosponges

• Antonella Di Vincenzo,
• Antonio Palumbo Piccionello,
• Alberto Spinella,
• Delia Chillura Martino,
• Marco Russo and
• Paolo Lo Meo

Beilstein J. Org. Chem. 2019, 15, 633–641, doi:10.3762/bjoc.15.59

• external stimuli is a highly desirable property for tailored materials designed to accomplish particular functions, such as targeted drug delivery systems, as accounted for by the present burst in literature reports [1][2][3][4][5][6]. In this context, we have been recently interested in the synthesis of

Novel solid-phase strategy for the synthesis of ligand-targeted fluorescent-labelled chelating peptide conjugates as a theranostic tool for cancer

• Sagnik Sengupta,
• Mena Asha Krishnan,
• Premansh Dudhe,
• Ramesh B. Reddy,
• Bishnubasu Giri,
• Sudeshna Chattopadhyay and
• Venkatesh Chelvam

Beilstein J. Org. Chem. 2018, 14, 2665–2679, doi:10.3762/bjoc.14.244

• tag; Fmoc-Lys-(Tfa)-OH; prostate cancer and ovarian cancer; solid-phase peptide synthesis; Introduction The understanding of cell processes is indispensable to devise new strategies for diagnosis and treatment of cancer and inflammatory diseases through targeted drug delivery techniques [1]. The

• malignancy [23] and inflammatory diseases. They are also utilized for targeted drug delivery [24][25] of therapeutics to avoid any off-site toxicity to normal and healthy cells. Unfortunately, strategies to construct diagnostic and therapeutic chemical tools consisting of a polypeptidic spacer, a homing

• which express neither PSMA nor folate receptors [panels (iv) and (viii)]. The absence of any rhodamine B bioconjugates 13 and 17 uptake in the cytoplasm of negative cell line, PC-3 cells, show that the bioconjugates are very specific which is an important criterion in targeted drug delivery systems for

Synthesis and photophysical studies of a multivalent photoreactive Ru^II-calix[4]arene complex bearing RGD-containing cyclopentapeptides

• Sofia Kajouj,
• Lionel Marcelis,
• Alice Mattiuzzi,
• Adrien Grassin,
• Damien Dufour,
• Pierre Van Antwerpen,
• Didier Boturyn,
• Eric Defrancq,
• Mathieu Surin,
• Julien De Winter,
• Pascal Gerbaux,
• Ivan Jabin and
• Cécile Moucheron

Beilstein J. Org. Chem. 2018, 14, 1758–1768, doi:10.3762/bjoc.14.150

• its receptor [44][45][46], clustered RGD-containing compounds were developed and were shown to exhibit attractive biological properties for the imaging of tumors [47][48][49][50] and for the targeted drug delivery [51][52][53]. In the course of designing phototherapeutic agents that could specifically

Drug targeting to decrease cardiotoxicity – determination of the cytotoxic effect of GnRH-based conjugates containing doxorubicin, daunorubicin and methotrexate on human cardiomyocytes and endothelial cells

• Livia Polgár,
• Eszter Lajkó,
• Pál Soós,
• Orsolya Láng,
• Marilena Manea,
• Béla Merkely,
• Gábor Mező and
• László Kőhidai

Beilstein J. Org. Chem. 2018, 14, 1583–1594, doi:10.3762/bjoc.14.136

• ]. However, it exerted a significantly lower endocrine effect in mammals than the human GnRH (GnRH-I: Glp-His-Trp-Ser-Tyr-Gly-Leu-Arg-Pro-Gly-NH2) and other GnRH analogues [9]. This low hormonal effect might provide an advantage in the treatment of hormone-independent tumors [10]. Targeted drug delivery is a

• clinical trial, which was discontinued for all indications under development in May 2017 [12]. GnRH-III-based conjugates have been investigated in our laboratory as promising candidates for targeted drug delivery with positive results in human tumor cell lines, both related (e.g., MCF-7) and unrelated (e.g

On the design principles of peptide–drug conjugates for targeted drug delivery to the malignant tumor site

• Eirinaios I. Vrettos,
• Gábor Mező and
• Andreas G. Tzakos

Beilstein J. Org. Chem. 2018, 14, 930–954, doi:10.3762/bjoc.14.80

• to bind the EGFR with high affinity and selectivity through screening phage display libraries and have been used like a viable approach for targeted drug delivery: YHWYGYTPQNVI [73], CMYIEALDKYAC [74], LTVSPWY [75], YWPSVTL [76]. Angiopep-2: A peptide that has recently attracted attention is a 19-mer

Development of novel cyclic NGR peptide–daunomycin conjugates with dual targeting property

• Andrea Angelo Pierluigi Tripodi,
• Szilárd Tóth,
• Kata Nóra Enyedi,
• Gitta Schlosser,
• Gergely Szakács and
• Gábor Mező

Beilstein J. Org. Chem. 2018, 14, 911–918, doi:10.3762/bjoc.14.78

• release; NGR peptides; oxime-linkage; targeted drug delivery; Introduction Targeted chemotherapy is one of the most promising approaches for selective cancer treatment that may decrease the toxic side effects of anticancer drugs. This therapeutic approach is based on the fact that tumor specific

Synthesis and in vitro biochemical evaluation of oxime bond-linked daunorubicin–GnRH-III conjugates developed for targeted drug delivery

• Sabine Schuster,
• Beáta Biri-Kovács,
• Bálint Szeder,
• Viktor Farkas,
• László Buday,
• Zsuzsanna Szabó,
• Gábor Halmos and
• Gábor Mező

Beilstein J. Org. Chem. 2018, 14, 756–771, doi:10.3762/bjoc.14.64

Preparation and evaluation of cyclodextrin polypseudorotaxane with PEGylated liposome as a sustained release drug carrier

• Kayoko Hayashida,
• Taishi Higashi,
• Daichi Kono,
• Keiichi Motoyama,
• Koki Wada and
• Hidetoshi Arima

Beilstein J. Org. Chem. 2014, 10, 2756–2764, doi:10.3762/bjoc.10.292

• and forms a hydrophilic layer on the surface of LPs [28]. It is not recognized by RES, which leads to a prolonged retention in circulation (stealth characteristics), and shows the enhanced permeability retention (EPR) effect [36]. PEG-LP is widely used as a drug carrier to realize the targeted drug

• delivery of anticancer drugs [28]. PEG-LP encapsulating DOX is commercially available as DOXIL/CAELYX® [28]. In addition, PEG-LPs are also utilized as long-circulating drug carriers for protein drugs and nucleic acids [37][38]. Thus, PEG-LPs are representative drug carriers and CD PPRXs of PEG-LPs could be

Towards the sequence-specific multivalent molecular recognition of cyclodextrin oligomers

• Michael Kurlemann and
• Bart Jan Ravoo

Beilstein J. Org. Chem. 2014, 10, 2428–2440, doi:10.3762/bjoc.10.253

• toxins or viruses and for imaging and targeted drug delivery [3]. Hydrogels which are built up by multivalent host–guest interactions and vesicles of amphiphilic host molecules have been intensively studied for their ability to function as drug delivery systems as well [4][5][6][7][8][9]. Additionally