Month: April 2024

Small molecule probes to quantify the functional fraction of a specific protein in a cell with minimal folding equilibrium shifts was written by Liu, Yu;Tan, Yun Lei;Zhang, Xin;Bhabha, Gira;Ekiert, Damian C.;Genereux, Joseph C.;Cho, Younhee;Kipnis, Yakov;Bjelic, Sinisa;Baker, David;Kelly, Jeffery W.. And the article was included in Proceedings of the National Academy of Sciences of the United States of America in 2014.Application In Synthesis of 2,5-Dioxopyrrolidin-1-yl 3′,6′-dihydroxy-3-oxo-3H-spiro[isobenzofuran-1,9′-xanthene]-5-carboxylate This article mentions the following:

Although much is known about protein folding in buffers, it remains unclear how the cellular protein homeostasis network functions as a system to partition client proteins between folded and functional, soluble and misfolded, and aggregated conformations. Herein, we develop small mol. folding probes that specifically react with the folded and functional fraction of the protein of interest, enabling fluorescence-based quantification of this fraction in cell lysate at a time point of interest. Importantly, these probes minimally perturb a protein’s folding equilibrium within cells during and after cell lysis, because sufficient cellular chaperone/chaperonin holdase activity is created by rapid ATP depletion during cell lysis. The folding probe strategy and the faithful quantification of a particular protein’s functional fraction are exemplified with retroaldolase, a de novo designed enzyme, and transthyretin, a nonenzyme protein. Our findings challenge the often invoked assumption that the soluble fraction of a client protein is fully folded in the cell. Moreover, our results reveal that the partitioning of destabilized retroaldolase and transthyretin mutants between the aforementioned conformational states is strongly influenced by cytosolic proteostasis network perturbations. Overall, our results suggest that applying a chem. folding probe strategy to other client proteins offers opportunities to reveal how the proteostasis network functions as a system to regulate the folding and function of individual client proteins in vivo. In the experiment, the researchers used many compounds, for example, 2,5-Dioxopyrrolidin-1-yl 3′,6′-dihydroxy-3-oxo-3H-spiro[isobenzofuran-1,9′-xanthene]-5-carboxylate (cas: 92557-80-7Application In Synthesis of 2,5-Dioxopyrrolidin-1-yl 3′,6′-dihydroxy-3-oxo-3H-spiro[isobenzofuran-1,9′-xanthene]-5-carboxylate).

2,5-Dioxopyrrolidin-1-yl 3′,6′-dihydroxy-3-oxo-3H-spiro[isobenzofuran-1,9′-xanthene]-5-carboxylate (cas: 92557-80-7) belongs to benzofurans derivatives. Benzofuran is a core structural unit found in many naturally occurring compounds with multidirectional biological activities. Substituted benzofurans find applications such as fluorescent sensors, oxidants, in drug discovery, and in another field of chemistry and agriculture.Application In Synthesis of 2,5-Dioxopyrrolidin-1-yl 3′,6′-dihydroxy-3-oxo-3H-spiro[isobenzofuran-1,9′-xanthene]-5-carboxylate

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Protein-responsive protein release of supramolecular/polymer hydrogel composite integrating enzyme activation systems was written by Shigemitsu, Hajime;Kubota, Ryou;Nakamura, Keisuke;Matsuzaki, Tomonobu;Minami, Saori;Aoyama, Takuma;Urayama, Kenji;Hamachi, Itaru. And the article was included in Nature Communications.Synthetic Route of C25H15NO9 This article mentions the following:

Non-enzymic proteins including antibodies function as biomarkers and are used as biopharmaceuticals in several diseases. Protein-responsive soft materials capable of the controlled release of drugs and proteins have potential for use in next-generation diagnosis and therapies. Here, we describe a supramol./agarose hydrogel composite that can release a protein in response to a non-enzymic protein. A non-enzymic protein-responsive system is developed by hybridization of an enzyme-sensitive supramol. hydrogel with a protein-triggered enzyme activation set. In situ imaging shows that the supramol./agarose hydrogel composite consists of orthogonal domains of supramol. fibers and agarose, which play distinct roles in protein entrapment and mech. stiffness, resp. Integrating the enzyme activation set with the composite allows for controlled release of the embedded RNase in response to an antibody. Such composite hydrogels would be promising as a matrix embedded in a body, which can autonomously release biopharmaceuticals by sensing biomarker proteins. In the experiment, the researchers used many compounds, for example, 2,5-Dioxopyrrolidin-1-yl 3′,6′-dihydroxy-3-oxo-3H-spiro[isobenzofuran-1,9′-xanthene]-5-carboxylate (cas: 92557-80-7Synthetic Route of C25H15NO9).

2,5-Dioxopyrrolidin-1-yl 3′,6′-dihydroxy-3-oxo-3H-spiro[isobenzofuran-1,9′-xanthene]-5-carboxylate (cas: 92557-80-7) belongs to benzofurans derivatives. Benzofurans are only weakly aromatic in nature and they are cleaved by many oxidative and reductive conditions. Benzofurans have also made significant and distinctive contributions to biology. They exhibit several biological activities that range from antioxidant, antitubercular, antiplasmodial, insecticidal.Synthetic Route of C25H15NO9

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

A simple open source bioinformatic methodology for initial exploration of GPCR ligands′ agonistic/antagonistic properties was written by Panagiotopoulos, Athanasios A.;Papachristofi, Christina;Kalyvianaki, Konstantina;Malamos, Panagiotis;Theodoropoulos, Panayiotis A.;Notas, George;Calogeropoulou, Theodora;Castanas, Elias;Kampa, Marilena. And the article was included in Pharmacology Research & Perspectives in 2020.Quality Control of 4-Amino-5-chloro-N-(1-(3-methoxypropyl)piperidin-4-yl)-2,3-dihydrobenzofuran-7-carboxamide This article mentions the following:

Drug development is an arduous procedure, necessitating testing the interaction of a large number of potential candidates with potential interacting (macro)mols. Therefore, any method which could provide an initial screening of potential candidate drugs might be of interest for the acceleration of the procedure, by highlighting interesting compounds, prior to in vitro and in vivo validation. In this line, we present a method which may identify potential hits, with agonistic and/or antagonistic properties on GPCR receptors, integrating the knowledge on signaling events triggered by receptor activation (GPCRs binding to Gα,β,γ proteins, and activating Gα, exchanging GDP for GTP, leading to a decreased affinity of the Gα for the GPCR). We show that, by integrating GPCR-ligand and Gα-GDP or -GTP binding in docking simulation, which correctly predicts crystallog. data, we can discriminate agonists, partial agonists, and antagonists, through a linear function, based on the ΔG (Gibbs-free energy) of liganded-GPCR/Gα-GDP. We built our model using two Gαs (β2-adrenergic and prostaglandin-D2), four Gαi (μ-opioid, dopamine-D3, adenosine-A1, rhodopsin), and one Gαo (serotonin) receptors and validated it with a series of ligands on a recently deorphanized Gαi receptor (OXER1). This approach could be a valuable tool for initial in silico validation and design of GPRC-interacting ligands. In the experiment, the researchers used many compounds, for example, 4-Amino-5-chloro-N-(1-(3-methoxypropyl)piperidin-4-yl)-2,3-dihydrobenzofuran-7-carboxamide (cas: 179474-81-8Quality Control of 4-Amino-5-chloro-N-(1-(3-methoxypropyl)piperidin-4-yl)-2,3-dihydrobenzofuran-7-carboxamide).

4-Amino-5-chloro-N-(1-(3-methoxypropyl)piperidin-4-yl)-2,3-dihydrobenzofuran-7-carboxamide (cas: 179474-81-8) belongs to benzofurans derivatives. Benzofurans are only weakly aromatic in nature and they are cleaved by many oxidative and reductive conditions. Introduction of benzofurans in organic synthesis, particularly drug synthesis, involves generally the use of their metalated species as nucleophiles in addition reactions or in metal-catalysed cross-coupling reactions.Quality Control of 4-Amino-5-chloro-N-(1-(3-methoxypropyl)piperidin-4-yl)-2,3-dihydrobenzofuran-7-carboxamide

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Development and characterization of layer-by-layer coated liposomes with poly(L-lysine) and poly(L-glutamic acid) to increase their resistance in biological media was written by Hermal, Florence;Frisch, Benoit;Specht, Alexandre;Bourel-Bonnet, Line;Heurtault, Beatrice. And the article was included in International Journal of Pharmaceutics (Amsterdam, Netherlands) in 2020.SDS of cas: 3326-34-9 This article mentions the following:

Multilayered coated liposomes were prepared using the layer-by-layer (LbL) technique in an effort to improve their stability in biol. media. The formulation strategy was based on the alternate deposition of two biocompatible and biodegradable polyelectrolytes – poly(L-lysine) (PLL) and poly(L-glutamic acid) (PGA) – on neg. charged small unilamellar vesicles (SUVs). Some parameters of the formulation process were optimized such as the polyelectrolyte concentration and the purification procedure. This optimized procedure has allowed the development of very homogeneous formulations of liposomes coated with up to 6 layers of polymers (so-called layersomes). The coating was characterized by dynamic light scattering (DLS), zeta potential measurements and Forster resonance energy transfer (FRET) between two fluorescently labeled polyelectrolytes. Studies on the stability of the formulations at 4°C in a buffered solution have shown that most structures are stable over 1 mo without impacting their encapsulation capacity. In addition, fluorophore release experiments have demonstrated a better resistance of the layersomes in the presence of a non-ionic detergent (Triton X-100) as well as in the presence of phospholipase A₂ and human plasma. In conclusion, new multilayered liposomes have been developed to increase the stability of conventional liposomes in biol. environments. In the experiment, the researchers used many compounds, for example, 5-Amino-3′,6′-dihydroxy-3H-spiro[isobenzofuran-1,9′-xanthen]-3-one (cas: 3326-34-9SDS of cas: 3326-34-9).

5-Amino-3′,6′-dihydroxy-3H-spiro[isobenzofuran-1,9′-xanthen]-3-one (cas: 3326-34-9) belongs to benzofurans derivatives. Many natural or synthetic compounds containing benzofuran skeletons have been found to possess remarkable activity as agrochemicals and pharmaceuticals. In nature, benzofurans have occupied an important role among the plant phenols & several pharmacologically active compounds.SDS of cas: 3326-34-9

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Nickel-catalyzed intramolecular C-H arylation using aryl pivalates as electrophiles was written by Wang, Jiayi;Ferguson, Devin M.;Kalyani, Dipannita. And the article was included in Tetrahedron in 2013.Safety of Naphtho[2,1-b]benzofuran This article mentions the following:

This paper describes a method for nickel catalyzed intramol. C-H arylation using aryl pivalates as electrophiles. The transformation is efficient for the synthesis of diverse electronically and sterically differentiated dibenzofurans. Addnl., the method could be expanded toward the synthesis of carbazoles. Preliminary mechanistic studies of the transformation are also described. In the experiment, the researchers used many compounds, for example, Naphtho[2,1-b]benzofuran (cas: 205-39-0Safety of Naphtho[2,1-b]benzofuran).

Naphtho[2,1-b]benzofuran (cas: 205-39-0) belongs to benzofurans derivatives. Benzofurans are only weakly aromatic in nature and they are cleaved by many oxidative and reductive conditions. Benzofurans are stable towards alkali and readily polymerize on treatment with sulfuric acid, due to which they are useful for the preparation of low cost chemically relatively inert resins.Safety of Naphtho[2,1-b]benzofuran

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Development and evaluation of a multi-class analytical method based on solid-phase extraction combined with liquid chromatography-tandem mass spectrometry for the analysis of pharmaceuticals and personal care products in urban wastewater samples was written by Konda, Satyanand;Asati, Ankita;Williams, Mike;Mudiam, Mohana Krishna Reddy. And the article was included in Separation Science plus in 2022.HPLC of Formula: 80621-81-4 This article mentions the following:

An anal. method has been developed for the quant. evaluation of 64 pharmaceuticals and personal care products in urban wastewater using solid-phase extraction coupled with liquid chromatog.-tandem mass spectrometry. Design of experiments approach was used in the multiparametric optimization of solid-phase extraction method for the anal. of pharmaceuticals and personal care products. The method was found to be linear within the range of 0.01-1 μg/L with coefficient of determination (R²) ranging from 0.990 to 0.999. The limit of detection and limit of quantification were found to be in the range of 0.002-0.028 and 0.007-0.091 μg/L, resp. The accuracy was calculated with respect to percent recovery, and it was found to be in the range of 70.0-129% for all the analytes. The intra- and interday precisions were found to be less than 15% relative standard deviation for all the analytes. The developed anal. method was applied to real samples collected from four different sampling sites of Musi River in Hyderabad to evaluate its performance. The method found a wide application for the anal. of urban wastewater samples. In the experiment, the researchers used many compounds, for example, (2S,16Z,18E,20S,21S,22R,23R,24R,25S,26R,27S,28E)-25-(Acetyloxy)-5,6,21,23-tetrahydroxy-27-methoxy-2,4,11,16,20,22,24,26-octamethyl-2,7-(epoxypentadeca[1,11,13]trienimino)benzofuro[4,5-e]pyrido[1,2-a]benzimidazole-1,15(2H)-dione (cas: 80621-81-4HPLC of Formula: 80621-81-4).

(2S,16Z,18E,20S,21S,22R,23R,24R,25S,26R,27S,28E)-25-(Acetyloxy)-5,6,21,23-tetrahydroxy-27-methoxy-2,4,11,16,20,22,24,26-octamethyl-2,7-(epoxypentadeca[1,11,13]trienimino)benzofuro[4,5-e]pyrido[1,2-a]benzimidazole-1,15(2H)-dione (cas: 80621-81-4) belongs to benzofurans derivatives. Many natural or synthetic compounds containing benzofuran skeletons have been found to possess remarkable activity as agrochemicals and pharmaceuticals. As benzofurans are prone to undergo ring opening of the heterocycle, examples of reduction of this type of aromatics by using dissolving metals are rather scarce.HPLC of Formula: 80621-81-4

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

The role of ROS generation from magnetic nanoparticles in an alternating magnetic field on cytotoxicity was written by Wydra, Robert J.;Rychahou, Piotr G.;Evers, B. Mark;Anderson, Kimberly W.;Dziubla, Thomas D.;Hilt, J. Zach. And the article was included in Acta Biomaterialia in 2015.Name: 5-Amino-3′,6′-dihydroxy-3H-spiro[isobenzofuran-1,9′-xanthen]-3-one This article mentions the following:

Monosaccharide coated iron oxide nanoparticles were developed to selectively target colon cancer cell lines for magnetically mediated energy delivery therapy. The nanoparticles were prepared using a coupling reaction to attach the glucose functional group to the iron oxide core, and functionality was confirmed with physicochem. characterization techniques. The targeted nanoparticles were internalized into CT26 cells at a greater extent than non-targeted nanoparticles, and the nanoparticles were shown to be localized within lysosomes. Cells with internalized nanoparticles were exposed to an AMF to determine the potential to delivery therapy. Cellular ROS generation and apoptotic cell death was enhanced with field exposure. The nanoparticle coatings inhibit the Fenton-like surface generation of ROS suggesting a thermal or mech. effect is more likely the source of the intracellular effect, unless the nanoparticle coating is unstable in the cellular environment. This is the first study to assess glucose coated MNPs for the delivery of MagMED therapy. With exposure of an AMF, the glucose-coated nanoparticles displayed a significant increase in cellular ROS and apoptotic cell death with no measurable increase in media temperature To determine the mechanism of toxicity, we investigated the surface generation of ROS through Fenton-like chem. The coated systems displayed negligible ROS generation compared to uncoated nanoparticles. These observations suggest the cellular ROS measured is attributed to a thermal or mech. effect of the internalized nanoparticles. In summary, this manuscript reports on some new insights as to the mechanism of MagMED therapies, which are of high interest to the biomaterials and cancer nanomedicine fields. In the experiment, the researchers used many compounds, for example, 5-Amino-3′,6′-dihydroxy-3H-spiro[isobenzofuran-1,9′-xanthen]-3-one (cas: 3326-34-9Name: 5-Amino-3′,6′-dihydroxy-3H-spiro[isobenzofuran-1,9′-xanthen]-3-one).

5-Amino-3′,6′-dihydroxy-3H-spiro[isobenzofuran-1,9′-xanthen]-3-one (cas: 3326-34-9) belongs to benzofurans derivatives. Benzofuran is a core structural unit found in many naturally occurring compounds with multidirectional biological activities. Benzofurans have also made significant and distinctive contributions to biology. They exhibit several biological activities that range from antiviral, antimicrobial, antitumor, anti-inflammatory.Name: 5-Amino-3′,6′-dihydroxy-3H-spiro[isobenzofuran-1,9′-xanthen]-3-one

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Impact of Steroid Only Induction on Rejection in Simultaneous Liver-Kidney Transplantation. was written by Ruiz, Irene;Sparkes, Tracy;Masters, Brian;Barth, Rolf;Maluf, Daniel;Freedman, Sari. And the article was included in Progress in transplantation (Aliso Viejo, Calif.) in 2022.Reference of 24280-93-1 This article mentions the following:

Introduction: The occurrence of simultaneous liver kidney transplantation has greatly increased; however, the ideal induction and maintenance immunosuppression remains unknown. Question: This evaluation aimed to determine if corticosteroid only induction in simultaneous liver kidney transplant recipients provided adequate prophylaxis against rejection when compared to basiliximab. Design: This was a single center, retrospective, cohort study of adult simultaneous liver kidney transplant recipients from June 2010 to June 2019 receiving corticosteroid only (N = 41) or basiliximab (N = 42) induction. Results: Liver or kidney biopsy proven acute rejection at 3 months was comparable between the corticosteroid only and basiliximab groups (10% vs 7%, P = .67), which persisted through 12 months posttransplant (15% vs 21%, P = .42). The occurrence of any infection at 3 months was increased in the corticosteroid only group relative to the basiliximab group (41% vs 21%, P = .049). Graft and patient survival at 12 months were similar between groups. Maintenance immunosuppression was overall minimized with a tacrolimus goal of 6-8 ng/mL, mycophenolate mofetil dose reduction to 1000 mg/day by 3 months, and early steroid withdrawal in both groups. Conclusion: Our findings suggested that corticosteroid only induction was an effective strategy for preventing rejection in simultaneous liver kidney transplant recipients, even in combination with reduced maintenance immunosuppression. In the experiment, the researchers used many compounds, for example, (E)-6-(4-Hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydroisobenzofuran-5-yl)-4-methylhex-4-enoic acid (cas: 24280-93-1Reference of 24280-93-1).

(E)-6-(4-Hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydroisobenzofuran-5-yl)-4-methylhex-4-enoic acid (cas: 24280-93-1) belongs to benzofurans derivatives. Many natural or synthetic compounds containing benzofuran skeletons have been found to possess remarkable activity as agrochemicals and pharmaceuticals. As benzofurans are prone to undergo ring opening of the heterocycle, examples of reduction of this type of aromatics by using dissolving metals are rather scarce.Reference of 24280-93-1

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Mucormycosis as SARS-CoV2 sequelae in kidney transplant recipients: a single-center experience from India was written by Meshram, Hari Shankar;Kute, Vivek B.;Chauhan, Sanshriti;Dave, Ruchir;Patel, Himanshu;Banerjee, Subho;Desai, Sudeep;Kumar, Deepak;Navadiya, Vijay;Mishra, Vineet. And the article was included in International Urology and Nephrology in 2022.Electric Literature of C17H20O6 This article mentions the following:

Coronavirus disease (COVID-19) sequelae in the transplant population are scarcely reported. Post-COVID-19 mucormycosis is one of such sequelae, which is a dreadful and rare entity. The purpose of this report was to study the full spectrum of this dual infection in kidney transplant recipients (KTR). We did a comprehensive anal. of 11 mucormycosis cases in KTR who recovered from COVID-19 in IKDRC, Ahmedabad, Gujarat, India during the study period from Nov 2020 to May 2021. We also looked for the risk factors for mucormycosis with a historical cohort of 157 KTR who did not develop mucormycosis. The median age (interquartile range, range) of the cohort was 42 (33.5-50, 26-60) years with 54.5% diabetes. COVID-19 severity ranged from mild (n = 10) to severe cases (n = 1). The duration from COVID-19 recovery to presentation was 7 (7-7, 4-14) days. Ten cases were Rhino-orbital-cerebral-mucormycosis (ROCM) and one had pulmonary mucormycosis. Functional endoscopic sinus surgery (FESS) was performed in all cases of ROCM. The duration of antifungal therapy was 28 (24-30, 21-62) days. The mortality rate reported was 27%. The risk factors for post-transplant mucormycosis were diabetes (18% vs 54.5%; p-value = 0.01), lymphopenia [12 (10-18) vs 20 (12-26) %; p-value = 0.15] and a higher neutrophil-lymphocyte ratio [7 (4.6-8.3) vs 3.85 (3.3-5.8); p-value = 0.5]. Conclusion: The morbidity and mortality with post-COVID-19 mucormycosis are high. Post-transplant patients with diabetes are more prone to this dual infection. Preparedness and early identification is the key to improve the outcomes. In the experiment, the researchers used many compounds, for example, (E)-6-(4-Hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydroisobenzofuran-5-yl)-4-methylhex-4-enoic acid (cas: 24280-93-1Electric Literature of C17H20O6).

(E)-6-(4-Hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydroisobenzofuran-5-yl)-4-methylhex-4-enoic acid (cas: 24280-93-1) belongs to benzofurans derivatives. Benzofuran is the “”parent”” of many related compounds with more complex structures. For example, psoralen is a benzofuran derivative that occurs in several plants. Introduction of benzofurans in organic synthesis, particularly drug synthesis, involves generally the use of their metalated species as nucleophiles in addition reactions or in metal-catalysed cross-coupling reactions.Electric Literature of C17H20O6

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem