TY  - JOUR
AU  - Albert, Lea
AU  - Nagpal, Jatin
AU  - Steinchen, Wieland
AU  - Zhang, Lei
AU  - Werel, Laura
AU  - Đoković, Nemanja
AU  - Ružić, Dušan
AU  - Hoffarth, Malte
AU  - Xu, Jing
AU  - Kaspareit, Johanna
AU  - Abendroth, Frank
AU  - Royant, Antoine
AU  - Bange, Gert
AU  - Nikolić, Katarina
AU  - Ryu, Soojin
AU  - Dou, Yali
AU  - Essen, Lars-Oliver
AU  - Vázquez, Olalla
PY  - 2022
UR  - https://farfar.pharmacy.bg.ac.rs/handle/123456789/4904
AB  - Optical control has enabled functional modulation
in cell culture with unparalleled spatiotemporal resolution.
However, current tools for in vivo manipulation are scarce. Here,
we design and implement a genuine on−of f optochemical probe
capable of achieving hematopoietic control in zebrafish. Our
photopharmacological approach first developed conformationally
strained visible light photoswitches (CS-VIPs) as inhibitors of the
histone methyltransferase MLL1 (KMT2A). In blood homeostasis
MLL1 plays a crucial yet controversial role. CS-VIP 8 optimally
fulfils the requirements of a true bistable functional system in vivo under visible-light irradiation, and with unprecedented stability.
These properties are exemplified via hematopoiesis photoinhibition with a single isomer in zebrafish. The present interdisciplinary
study uncovers the mechanism of action of CS-VIPs. Upon WDR5 binding, CS-VIP 8 causes MLL1 release with concomitant
allosteric rearrangements in the WDR5/RbBP5 interface. Since our tool provides on-demand reversible control without genetic
intervention or continuous irradiation, it will foster hematopathology and epigenetic investigations. Furthermore, our workflow will
enable exquisite photocontrol over other targets inhibited by macrocycles.
PB  - American Chemical Society
T2  - ACS Central Science
T1  - Bistable Photoswitch Allows in Vivo Control of Hematopoiesis
VL  - 8
IS  - 1
SP  - 57
EP  - 66
DO  - 10.1021/acscentsci.1c00434
ER  - 

@article{
author = "Albert, Lea and Nagpal, Jatin and Steinchen, Wieland and Zhang, Lei and Werel, Laura and Đoković, Nemanja and Ružić, Dušan and Hoffarth, Malte and Xu, Jing and Kaspareit, Johanna and Abendroth, Frank and Royant, Antoine and Bange, Gert and Nikolić, Katarina and Ryu, Soojin and Dou, Yali and Essen, Lars-Oliver and Vázquez, Olalla",
year = "2022",
abstract = "Optical control has enabled functional modulation
in cell culture with unparalleled spatiotemporal resolution.
However, current tools for in vivo manipulation are scarce. Here,
we design and implement a genuine on−of f optochemical probe
capable of achieving hematopoietic control in zebrafish. Our
photopharmacological approach first developed conformationally
strained visible light photoswitches (CS-VIPs) as inhibitors of the
histone methyltransferase MLL1 (KMT2A). In blood homeostasis
MLL1 plays a crucial yet controversial role. CS-VIP 8 optimally
fulfils the requirements of a true bistable functional system in vivo under visible-light irradiation, and with unprecedented stability.
These properties are exemplified via hematopoiesis photoinhibition with a single isomer in zebrafish. The present interdisciplinary
study uncovers the mechanism of action of CS-VIPs. Upon WDR5 binding, CS-VIP 8 causes MLL1 release with concomitant
allosteric rearrangements in the WDR5/RbBP5 interface. Since our tool provides on-demand reversible control without genetic
intervention or continuous irradiation, it will foster hematopathology and epigenetic investigations. Furthermore, our workflow will
enable exquisite photocontrol over other targets inhibited by macrocycles.",
publisher = "American Chemical Society",
journal = "ACS Central Science",
title = "Bistable Photoswitch Allows in Vivo Control of Hematopoiesis",
volume = "8",
number = "1",
pages = "57-66",
doi = "10.1021/acscentsci.1c00434"
}

Albert, L., Nagpal, J., Steinchen, W., Zhang, L., Werel, L., Đoković, N., Ružić, D., Hoffarth, M., Xu, J., Kaspareit, J., Abendroth, F., Royant, A., Bange, G., Nikolić, K., Ryu, S., Dou, Y., Essen, L.,& Vázquez, O.. (2022). Bistable Photoswitch Allows in Vivo Control of Hematopoiesis. in ACS Central Science
American Chemical Society., 8(1), 57-66.
https://doi.org/10.1021/acscentsci.1c00434

Albert L, Nagpal J, Steinchen W, Zhang L, Werel L, Đoković N, Ružić D, Hoffarth M, Xu J, Kaspareit J, Abendroth F, Royant A, Bange G, Nikolić K, Ryu S, Dou Y, Essen L, Vázquez O. Bistable Photoswitch Allows in Vivo Control of Hematopoiesis. in ACS Central Science. 2022;8(1):57-66.
doi:10.1021/acscentsci.1c00434 .

Albert, Lea, Nagpal, Jatin, Steinchen, Wieland, Zhang, Lei, Werel, Laura, Đoković, Nemanja, Ružić, Dušan, Hoffarth, Malte, Xu, Jing, Kaspareit, Johanna, Abendroth, Frank, Royant, Antoine, Bange, Gert, Nikolić, Katarina, Ryu, Soojin, Dou, Yali, Essen, Lars-Oliver, Vázquez, Olalla, "Bistable Photoswitch Allows in Vivo Control of Hematopoiesis" in ACS Central Science, 8, no. 1 (2022):57-66,
https://doi.org/10.1021/acscentsci.1c00434 . .

TY  - JOUR
AU  - Albert, Lea
AU  - Penalver, Alberto
AU  - Đoković, Nemanja
AU  - Werel, Laura
AU  - Hoffarth, Malte
AU  - Ružić, Dušan
AU  - Xu, Jing
AU  - Essen, Lars-Oliver
AU  - Nikolić, Katarina
AU  - Dou, Yali
AU  - Vazquez, Olalla
PY  - 2019
UR  - https://farfar.pharmacy.bg.ac.rs/handle/123456789/3258
AB  - Life relies on a myriad of carefully orchestrated processes, in which proteins and their direct interplay ultimately determine cellular function and disease. Modulation of this complex crosstalk has recently attracted attention, even as a novel therapeutic strategy. Herein, we describe the synthesis and characterization of two visible-light-responsive peptide backbone photoswitches based on azobenzene derivatives, to exert optical control over protein-protein interactions (PPI). The novel peptidomimetics undergo fast and reversible isomerization with low photochemical fatigue under alternatively blue-/green-light irradiation cycles. Both bind in the nanomolar range to the protein of interest. Importantly, the best peptidomimetic displays a clear difference between isomers in its protein-binding capacity and, in turn, in its potential to inhibit enzymatic activity through PPI disruption. In addition, crystal structure determination, docking and molecular dynamics calculations allow a molecular interpretation and open up new avenues in the design and synthesis of future photoswitchable PPI modulators.
PB  - Wiley-VCH Verlag GMBH, Weinheim
T2  - Chembiochem
T1  - Modulating Protein-Protein Interactions with Visible-Light-Responsive Peptide Backbone Photoswitches
VL  - 20
IS  - 11
SP  - 1417
EP  - 1429
DO  - 10.1002/cbic.201800737
ER  - 

@article{
author = "Albert, Lea and Penalver, Alberto and Đoković, Nemanja and Werel, Laura and Hoffarth, Malte and Ružić, Dušan and Xu, Jing and Essen, Lars-Oliver and Nikolić, Katarina and Dou, Yali and Vazquez, Olalla",
year = "2019",
abstract = "Life relies on a myriad of carefully orchestrated processes, in which proteins and their direct interplay ultimately determine cellular function and disease. Modulation of this complex crosstalk has recently attracted attention, even as a novel therapeutic strategy. Herein, we describe the synthesis and characterization of two visible-light-responsive peptide backbone photoswitches based on azobenzene derivatives, to exert optical control over protein-protein interactions (PPI). The novel peptidomimetics undergo fast and reversible isomerization with low photochemical fatigue under alternatively blue-/green-light irradiation cycles. Both bind in the nanomolar range to the protein of interest. Importantly, the best peptidomimetic displays a clear difference between isomers in its protein-binding capacity and, in turn, in its potential to inhibit enzymatic activity through PPI disruption. In addition, crystal structure determination, docking and molecular dynamics calculations allow a molecular interpretation and open up new avenues in the design and synthesis of future photoswitchable PPI modulators.",
publisher = "Wiley-VCH Verlag GMBH, Weinheim",
journal = "Chembiochem",
title = "Modulating Protein-Protein Interactions with Visible-Light-Responsive Peptide Backbone Photoswitches",
volume = "20",
number = "11",
pages = "1417-1429",
doi = "10.1002/cbic.201800737"
}

Albert, L., Penalver, A., Đoković, N., Werel, L., Hoffarth, M., Ružić, D., Xu, J., Essen, L., Nikolić, K., Dou, Y.,& Vazquez, O.. (2019). Modulating Protein-Protein Interactions with Visible-Light-Responsive Peptide Backbone Photoswitches. in Chembiochem
Wiley-VCH Verlag GMBH, Weinheim., 20(11), 1417-1429.
https://doi.org/10.1002/cbic.201800737

Albert L, Penalver A, Đoković N, Werel L, Hoffarth M, Ružić D, Xu J, Essen L, Nikolić K, Dou Y, Vazquez O. Modulating Protein-Protein Interactions with Visible-Light-Responsive Peptide Backbone Photoswitches. in Chembiochem. 2019;20(11):1417-1429.
doi:10.1002/cbic.201800737 .

Albert, Lea, Penalver, Alberto, Đoković, Nemanja, Werel, Laura, Hoffarth, Malte, Ružić, Dušan, Xu, Jing, Essen, Lars-Oliver, Nikolić, Katarina, Dou, Yali, Vazquez, Olalla, "Modulating Protein-Protein Interactions with Visible-Light-Responsive Peptide Backbone Photoswitches" in Chembiochem, 20, no. 11 (2019):1417-1429,
https://doi.org/10.1002/cbic.201800737 . .