Research ExplorerPublicationsFunctional non-nucleoside adenylyl cyclase inhibitors

Functional non-nucleoside adenylyl cyclase inhibitors

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Functional non-nucleoside adenylyl cyclase inhibitors. / Lelle, Marco; Hameed, Abdul; Ackermann, Lisa-Maria; Kaloyanova, Stefka; Wagner, Manfred; Berisha, Filip; Nikolaev, Viacheslav O; Peneva, Kalina.

In: CHEM BIOL DRUG DES, Vol. 85, No. 5, 05.2015, p. 633-637.

Research output: SCORING: Contribution to journal › Other (editorial matter etc.) › Research

Harvard

Lelle, M, Hameed, A, Ackermann, L-M, Kaloyanova, S, Wagner, M, Berisha, F, Nikolaev, VO & Peneva, K 2015, 'Functional non-nucleoside adenylyl cyclase inhibitors', CHEM BIOL DRUG DES, vol. 85, no. 5, pp. 633-637. https://doi.org/10.1111/cbdd.12452

APA

Lelle, M., Hameed, A., Ackermann, L-M., Kaloyanova, S., Wagner, M., Berisha, F., Nikolaev, V. O., & Peneva, K. (2015). Functional non-nucleoside adenylyl cyclase inhibitors. CHEM BIOL DRUG DES, 85(5), 633-637. https://doi.org/10.1111/cbdd.12452

Vancouver

Lelle M, Hameed A, Ackermann L-M, Kaloyanova S, Wagner M, Berisha F et al. Functional non-nucleoside adenylyl cyclase inhibitors. CHEM BIOL DRUG DES. 2015 May;85(5):633-637. https://doi.org/10.1111/cbdd.12452

Bibtex

@article{481ec02b8fb84d7cb3532ed3e731abc1,
title = "Functional non-nucleoside adenylyl cyclase inhibitors",
abstract = "In this study, we describe the synthesis of novel functional non-nucleoside adenylyl cyclase inhibitors, which can be easily modified with thiol containing biomolecules such as tumour targeting structures. The linkage between inhibitor and biomolecule contains cleavable bonds to enable efficient intracellular delivery in the reductive milieu of the cytosol as well as in the acidic environment within endosomes and lysosomes. The suitability of this synthetic approach was shown by the successful bioconjugation of a poor cell-permeable inhibitor with a cell-penetrating peptide. Additionally, we have demonstrated the excellent inhibitory effect of the compounds presented here in a live-cell F{\"o}rster resonance energy transfer-based assay in human embryonic kidney cells.",
keywords = "Adenylyl Cyclase Inhibitors, Adenylyl Cyclases, Biosensing Techniques, Cell-Penetrating Peptides, Cyclic AMP, Fluorescence Resonance Energy Transfer, HEK293 Cells, Humans, Isoproterenol",
author = "Marco Lelle and Abdul Hameed and Lisa-Maria Ackermann and Stefka Kaloyanova and Manfred Wagner and Filip Berisha and Nikolaev, {Viacheslav O} and Kalina Peneva",
note = "Letter",
year = "2015",
month = may,
doi = "10.1111/cbdd.12452",
language = "English",
volume = "85",
pages = "633--637",
journal = "CHEM BIOL DRUG DES",
issn = "1747-0277",
publisher = "Blackwell",
number = "5",

}

RIS

TY - JOUR

T1 - Functional non-nucleoside adenylyl cyclase inhibitors

AU - Lelle, Marco

AU - Hameed, Abdul

AU - Ackermann, Lisa-Maria

AU - Kaloyanova, Stefka

AU - Wagner, Manfred

AU - Berisha, Filip

AU - Nikolaev, Viacheslav O

AU - Peneva, Kalina

N1 - Letter

PY - 2015/5

Y1 - 2015/5

N2 - In this study, we describe the synthesis of novel functional non-nucleoside adenylyl cyclase inhibitors, which can be easily modified with thiol containing biomolecules such as tumour targeting structures. The linkage between inhibitor and biomolecule contains cleavable bonds to enable efficient intracellular delivery in the reductive milieu of the cytosol as well as in the acidic environment within endosomes and lysosomes. The suitability of this synthetic approach was shown by the successful bioconjugation of a poor cell-permeable inhibitor with a cell-penetrating peptide. Additionally, we have demonstrated the excellent inhibitory effect of the compounds presented here in a live-cell Förster resonance energy transfer-based assay in human embryonic kidney cells.

AB - In this study, we describe the synthesis of novel functional non-nucleoside adenylyl cyclase inhibitors, which can be easily modified with thiol containing biomolecules such as tumour targeting structures. The linkage between inhibitor and biomolecule contains cleavable bonds to enable efficient intracellular delivery in the reductive milieu of the cytosol as well as in the acidic environment within endosomes and lysosomes. The suitability of this synthetic approach was shown by the successful bioconjugation of a poor cell-permeable inhibitor with a cell-penetrating peptide. Additionally, we have demonstrated the excellent inhibitory effect of the compounds presented here in a live-cell Förster resonance energy transfer-based assay in human embryonic kidney cells.

KW - Adenylyl Cyclase Inhibitors

KW - Adenylyl Cyclases

KW - Biosensing Techniques

KW - Cell-Penetrating Peptides

KW - Cyclic AMP

KW - Fluorescence Resonance Energy Transfer

KW - HEK293 Cells

KW - Humans

KW - Isoproterenol

U2 - 10.1111/cbdd.12452

DO - 10.1111/cbdd.12452

M3 - Other (editorial matter etc.)

C2 - 25319071

VL - 85

SP - 633

EP - 637

JO - CHEM BIOL DRUG DES

JF - CHEM BIOL DRUG DES

SN - 1747-0277

IS - 5

ER -