A Dual-gene Reporter-amplifier Architecture for Enhancing the Sensitivity of Molecular MRI by Water Exchange
Chembiochem. 2024 Mar 4:e202400087. doi: 10.1002/cbic.202400087. Online ahead of print.ABSTRACTThe development of genetic reporters for magnetic resonance imaging (MRI) is essential for investigating biological functions in vivo. However, current MRI reporters have low sensitivity, making it challenging to create significant contrast against the tissue background, especially when only a small fraction of cells express the reporter. To overcome this limitation, we developed an approach for amplifying the sensitivity of molecular MRI by combining a chemogenetic contrast mechanism with a biophysical approach to increase water...
Source: Chembiochem - March 5, 2024 Category: Biochemistry Authors: Yimeng Huang Xinyue Chen Ziyue Zhu Arnab Mukherjee Source Type: research
Conversion of β-1,6-glucans to gentiobiose using an endo-β-1,6-glucanase PsGly30A from Paenibacillus sp. GKG
Chembiochem. 2024 Mar 5:e202400010. doi: 10.1002/cbic.202400010. Online ahead of print.ABSTRACTA plethora of di- and oligosaccharides isolated from the natural sources are used in food and pharmaceutical industry. An enzymatic hydrolysis of fungal cell wall β-glucans is a good alternative to produce the desired oligosaccharides with different functionalities, such as the flavour enhancer gentiobiose. We have previously identified PsGly30A as a potential yeast cell wall degrading β-1,6-glycosidase. The aim of this study is to characterise the PsGly30A enzyme, a member of the GH30 family, and to evaluate its suitability fo...
Source: Chembiochem - March 5, 2024 Category: Biochemistry Authors: Gediminas Plakys Nina Urbelien ė Gintaras Urbelis Justas Vaitek ūnas Linas Labanauskas Edita Ma žonienė Rolandas Me škys Source Type: research
Preclinical Evaluation of the Reversible Monoacylglycerol Lipase PET Tracer (R)-[ < sup > 11 < /sup > C]YH132: Application in Drug Development and Neurodegenerative Diseases
Chembiochem. 2024 Mar 5:e202300819. doi: 10.1002/cbic.202300819. Online ahead of print.ABSTRACTMonoacylglycerol lipase (MAGL) plays a crucial role in the degradation of 2-arachidonoylglycerol (2-AG), one of the major endocannabinoids in the brain. Inhibiting MAGL could lead to increased levels of 2-AG, which showed beneficial effects on pain management, anxiety, inflammation, and neuroprotection. In the current study, we report the characterization of an enantiomerically pure (R)-[11 C]YH132 as a novel MAGL PET tracer. It demonstrates an improved pharmacokinetic profile compared to its racemate. High in vitro MAGL specific...
Source: Chembiochem - March 5, 2024 Category: Biochemistry Authors: Yingfang He Aro Delparente Caitlin V M L Jie Claudia Keller Roland Humm Dominik Heer Ludovic Collin Roger Schibli Luca Gobbi Uwe Grether Linjing Mu Source Type: research
Reversible Influence of Hemipiperazine Photochromism on the Early Development of Zebrafish Embryo
This study explores the potential of controlling organismal development with light by using reversible photomodulation of activity in bioactive compounds. Specifically, our research focuses on plinabulin 1, an inhibitor of tubulin dynamics that contains a photochromic motif called hemipiperazine. The two isomeric forms, Z-1 and E-1, can partially interconvert with light, yet show remarkable thermal stability in darkness. The Z-isomer exhibits higher cytotoxicity due to stronger binding to α-tubulin's colchicine site. The less toxic E-1 form, considered a "pro-drug", can be isolated in vitro and stored. Upon activation by ...
Source: Chembiochem - March 5, 2024 Category: Biochemistry Authors: Angelika Seliwjorstow Masanari Takamiya Sepand Rastegar Zbigniew Pianowski Source Type: research
Synthesis and Macrodomain Binding of Gln-carba-ADPr-peptide
Chembiochem. 2024 Mar 5:e202300865. doi: 10.1002/cbic.202300865. Online ahead of print.ABSTRACTMono-ADP-ribosylation is a dynamic post-translational modification (PTM) with important roles in cell signalling. This modification occurs on a wide variety of amino acids, and one of the canonical modification sites within proteins is the side chain of glutamic acid. Given the transient nature of this modification (acylal linkage) and the high sensitivity of ADP-ribosylated glutamic acid, stabilized isosteres are required for structural and biochemical studies. Here, we report the synthesis of a mimic of ADP-ribosylated peptide ...
Source: Chembiochem - March 5, 2024 Category: Biochemistry Authors: Sande B Engelsma Aurelio Pio Nardozza Pieter de Saint Aulaire Herman S Overkleeft Gijsbert A van der Marel Andreas G Ladurner Dmitri Filippov Source Type: research
A Dual-gene Reporter-amplifier Architecture for Enhancing the Sensitivity of Molecular MRI by Water Exchange
Chembiochem. 2024 Mar 4:e202400087. doi: 10.1002/cbic.202400087. Online ahead of print.ABSTRACTThe development of genetic reporters for magnetic resonance imaging (MRI) is essential for investigating biological functions in vivo. However, current MRI reporters have low sensitivity, making it challenging to create significant contrast against the tissue background, especially when only a small fraction of cells express the reporter. To overcome this limitation, we developed an approach for amplifying the sensitivity of molecular MRI by combining a chemogenetic contrast mechanism with a biophysical approach to increase water...
Source: Chembiochem - March 5, 2024 Category: Biochemistry Authors: Yimeng Huang Xinyue Chen Ziyue Zhu Arnab Mukherjee Source Type: research
Conversion of β-1,6-glucans to gentiobiose using an endo-β-1,6-glucanase PsGly30A from Paenibacillus sp. GKG
Chembiochem. 2024 Mar 5:e202400010. doi: 10.1002/cbic.202400010. Online ahead of print.ABSTRACTA plethora of di- and oligosaccharides isolated from the natural sources are used in food and pharmaceutical industry. An enzymatic hydrolysis of fungal cell wall β-glucans is a good alternative to produce the desired oligosaccharides with different functionalities, such as the flavour enhancer gentiobiose. We have previously identified PsGly30A as a potential yeast cell wall degrading β-1,6-glycosidase. The aim of this study is to characterise the PsGly30A enzyme, a member of the GH30 family, and to evaluate its suitability fo...
Source: Chembiochem - March 5, 2024 Category: Biochemistry Authors: Gediminas Plakys Nina Urbelien ė Gintaras Urbelis Justas Vaitek ūnas Linas Labanauskas Edita Ma žonienė Rolandas Me škys Source Type: research
Preclinical Evaluation of the Reversible Monoacylglycerol Lipase PET Tracer (R)-[ < sup > 11 < /sup > C]YH132: Application in Drug Development and Neurodegenerative Diseases
Chembiochem. 2024 Mar 5:e202300819. doi: 10.1002/cbic.202300819. Online ahead of print.ABSTRACTMonoacylglycerol lipase (MAGL) plays a crucial role in the degradation of 2-arachidonoylglycerol (2-AG), one of the major endocannabinoids in the brain. Inhibiting MAGL could lead to increased levels of 2-AG, which showed beneficial effects on pain management, anxiety, inflammation, and neuroprotection. In the current study, we report the characterization of an enantiomerically pure (R)-[11 C]YH132 as a novel MAGL PET tracer. It demonstrates an improved pharmacokinetic profile compared to its racemate. High in vitro MAGL specific...
Source: Chembiochem - March 5, 2024 Category: Biochemistry Authors: Yingfang He Aro Delparente Caitlin V M L Jie Claudia Keller Roland Humm Dominik Heer Ludovic Collin Roger Schibli Luca Gobbi Uwe Grether Linjing Mu Source Type: research
Bifunctional Sildenafil Diazeniumdiolates Acting as Phosphodiesterase 5 Inhibitors and Nitric Oxide Donors ̶ Towards Wound Healing
This study explores hybrid compounds, combining NO-releasing diazeniumdiolates with a sildenafil-derived PDE5 inhibitor. One compound demonstrated a favorable NO-release profile, triggered by an esterase (prodrug), and displayed in vitro nanomolar inhibition potency against PDE5 and thrombin-induced platelet aggregation. Both factors are known to promote blood flow and oxygenation. Thus, our findings unveil promising prospects for effective wound healing treatments.PMID:38430555 | DOI:10.1002/cbic.202300801 (Source: Chembiochem)
Source: Chembiochem - March 2, 2024 Category: Biochemistry Authors: Josep Mas-Rosell ó Hermann Tenor Timea Szabo Reto Naef Simon Sieber Karl Gademann Source Type: research
Bifunctional Sildenafil Diazeniumdiolates Acting as Phosphodiesterase 5 Inhibitors and Nitric Oxide Donors ̶ Towards Wound Healing
This study explores hybrid compounds, combining NO-releasing diazeniumdiolates with a sildenafil-derived PDE5 inhibitor. One compound demonstrated a favorable NO-release profile, triggered by an esterase (prodrug), and displayed in vitro nanomolar inhibition potency against PDE5 and thrombin-induced platelet aggregation. Both factors are known to promote blood flow and oxygenation. Thus, our findings unveil promising prospects for effective wound healing treatments.PMID:38430555 | DOI:10.1002/cbic.202300801 (Source: Chembiochem)
Source: Chembiochem - March 2, 2024 Category: Biochemistry Authors: Josep Mas-Rosell ó Hermann Tenor Timea Szabo Reto Naef Simon Sieber Karl Gademann Source Type: research
O-nitrobenzyl Caged Molecule Enables Photo-controlled Release of Thiabendazole
Chembiochem. 2024 Mar 1:e202300742. doi: 10.1002/cbic.202300742. Online ahead of print.ABSTRACTPesticides are essential in agricultural development. Controlled-release pesticides have attracted great attentions. Base on a principle of spatiotemporal selectivity, we extended the photoremovable protective group (PRPG) into agrochemical agents to achieve controllable release of active ingredients. Herein, we obtained NP-TBZ by covalently linking o-nitrobenzyl (NP) with thiabendazole (TBZ). Compound NP-TBZ can be controlled to release TBZ in dependent to light. The irradiated and unirradiated NP-TBZ showed significant differen...
Source: Chembiochem - March 1, 2024 Category: Biochemistry Authors: Wen Fu Zhongli Shao Zhiping Xu Zhong Li Xusheng Shao Source Type: research
O-nitrobenzyl Caged Molecule Enables Photo-controlled Release of Thiabendazole
Chembiochem. 2024 Mar 1:e202300742. doi: 10.1002/cbic.202300742. Online ahead of print.ABSTRACTPesticides are essential in agricultural development. Controlled-release pesticides have attracted great attentions. Base on a principle of spatiotemporal selectivity, we extended the photoremovable protective group (PRPG) into agrochemical agents to achieve controllable release of active ingredients. Herein, we obtained NP-TBZ by covalently linking o-nitrobenzyl (NP) with thiabendazole (TBZ). Compound NP-TBZ can be controlled to release TBZ in dependent to light. The irradiated and unirradiated NP-TBZ showed significant differen...
Source: Chembiochem - March 1, 2024 Category: Biochemistry Authors: Wen Fu Zhongli Shao Zhiping Xu Zhong Li Xusheng Shao Source Type: research
Amine-Carbamate Self-Immolative Spacers Counterintuitively Release 3 ° Alcohol at Much Faster Rates than 1° Alcohol Payloads
Chembiochem. 2024 Feb 28:e202400174. doi: 10.1002/cbic.202400174. Online ahead of print.ABSTRACTSelf-immolative (SI) spacers are degradable chemical connectors widely used in prodrugs and drug conjugates to release pharmaceutical ingredients in response to specific stimuli. Amine-carbamate SI spacers are particularly versatile, as they have been used to release different hydroxy cargos, ranging from 2° and 3° alcohols to phenols and oximes. In this work, we describe the ability of three amine-carbamate SI spacers to release three structurally similar imidazoquinoline payloads, bearing either a 1°, a 2° or a 3° alcohol...
Source: Chembiochem - February 28, 2024 Category: Biochemistry Authors: Mattia Mason Lydia Bisbal Lopez Fazel Bashiri Aur élie Herrero Aur élien Baron Raffaella Bucci Luca Pignataro Cesare Gennari Alberto Dal Corso Source Type: research
The Biocatalytic Potential of Aromatic Ammonia-Lyase from Loktanella atrilutea
Chembiochem. 2024 Feb 28:e202400011. doi: 10.1002/cbic.202400011. Online ahead of print.ABSTRACTCharacterization of the aromatic ammonia-lyase from Loktanella atrilutea (LaAAL) revealed reduced activity towards canonical AAL substrates: L-Phe, L-Tyr, and L-His, contrasted by its pronounced efficiency towards 3,4-dimethoxy-L-phenylalanine. Assessing optimal conditions, LaAAL exhibited maximal activity at pH 9.5 in the ammonia elimination reaction route, distinct from the typical pH ranges of most PALs and TALs. Within the exploration of the ammonia source for the opposite, synthetically valuable ammonia addition reaction, t...
Source: Chembiochem - February 28, 2024 Category: Biochemistry Authors: Raluca Bianca Tomoaiaga Gyoparka Agoston Krisztina Boros Levente Csaba Nagy Monica Ioana Tosa Csaba Paizs Laszlo Csaba Bencze Source Type: research
Ether Bond Cleavage of a Phenylcoumaran β-5 Lignin Model Compound and Polymeric Lignin Catalysed by a LigE-type Etherase from Agrobacterium sp
Chembiochem. 2024 Feb 28:e202400132. doi: 10.1002/cbic.202400132. Online ahead of print.ABSTRACTA LigE-type beta-etherase enzyme from lignin-degrading Agrobacterium sp. has been identified, which assists degradation of polymeric lignins. Testing against lignin dimer model compounds revealed that it does not catalyse the previously reported reaction of Sphingobium SYK-6 LigE, but instead shows activity for a β-5 phenylcoumaran lignin dimer. The reaction products did not contain glutathione, indicating a catalytic role for reduced glutathione in this enzyme. Three reaction products were identified: the major product was a c...
Source: Chembiochem - February 28, 2024 Category: Biochemistry Authors: Goran M M Rashid Guillaume Rivi ère Betty Cottyn-Boitte Amel Majira Laurent C ézard Victoria Sodr é Richard Lam Julia A Fairbairn St éphanie Baumberger Timothy David Bugg Source Type: research
