Recent Progress in Prompt Molecular Detection of Exosomes Using CRISPR/Cas and Microfluidic-Assisted Approaches Toward Smart Cancer Diagnosis and Analysis
ChemMedChem. 2023 Nov 2:e202300359. doi: 10.1002/cmdc.202300359. Online ahead of print.ABSTRACTNano exosomes are essential indicators of molecular mechanisms involved in interacting with cancer cells and the tumor environment. The nano exosomes, as nanostructures based on lipids and nucleic acids, provide a communication pathway for information transfer by transporting biomolecules from the target cell to other cells. Importantly, these extracellular vesicles are released into the blood flow by the most invading cells, i.e., cancer cells; thereby, they could be considered a promising specific biomarker for cancer diagnosis...
Source: ChemMedChem - November 2, 2023 Category: Chemistry Authors: Seyyed Mojtaba Mousavi Seyyed Alireza Hashemi Masoomeh Yari Kalashgrani Vahid Rahmanian Mohsen Riazi Navid Omidifar Raed H Althomali Mohammed M Rahman Wei-Hung Chiang Ahmad Gholami Source Type: research

Kinetic Modeling of PROTAC-Induced Protein Degradation
ChemMedChem. 2023 Oct 31:e202300530. doi: 10.1002/cmdc.202300530. Online ahead of print.ABSTRACTKinetics of the PROTAC-induced protein degradation was modelled with the equilibrium approximation, accounting for the protein recovery rate with a time lag. The simulated kinetic curves resemble what is experimentally observed, and the physical formulas of the half-maximal degradation concentration (DC50) were derived from them. The equations reveal that DC50 is proportional to the dissociation constant of the ternary complex (Kd) and inversely proportional to the expression level of the E3 ligase and the effective ubiquitylati...
Source: ChemMedChem - October 31, 2023 Category: Chemistry Authors: Hongtao Zhao Frank Narjes Source Type: research

Kinetic Modeling of PROTAC-Induced Protein Degradation
ChemMedChem. 2023 Oct 31:e202300530. doi: 10.1002/cmdc.202300530. Online ahead of print.ABSTRACTKinetics of the PROTAC-induced protein degradation was modelled with the equilibrium approximation, accounting for the protein recovery rate with a time lag. The simulated kinetic curves resemble what is experimentally observed, and the physical formulas of the half-maximal degradation concentration (DC50) were derived from them. The equations reveal that DC50 is proportional to the dissociation constant of the ternary complex (Kd) and inversely proportional to the expression level of the E3 ligase and the effective ubiquitylati...
Source: ChemMedChem - October 31, 2023 Category: Chemistry Authors: Hongtao Zhao Frank Narjes Source Type: research

Terpene-functionalized Fluoroquinolones as Potential Antimicrobials: Synthesis and Properties
This study was the first to synthesize terpene-containing conjugates of fluoroquinolones, ciprofloxacin and norfloxacin, and to evaluate their antibacterial activity against gram-positive methicillin sensitive (MSSA) and methicillin resistant (MRSA) S. aureus, gram-negative P. aeruginosa as well as antifungal activity against C. albicans. The ability of obtained fluoroquinolones to inhibit S. aureus growth was found to depend upon the presence of a linker separating the bulky terpene and fluoroquinolone fragments, and this activity diminished with increasing its length. The highest activity against MSSA was demonstrated by...
Source: ChemMedChem - October 24, 2023 Category: Chemistry Authors: Evgeniy Sergeevich Izmest'ev Pestova V Svetlana Alena I Kolesnikova Diana R Baidamshina Airat R Kayumov Svetlana A Rubtsova Source Type: research

Synergistic and additive effects of menadione in combination with antibiotics on multidrug-resistant Staphylococcus aureus: Insights from structure-function analysis of NQs
ChemMedChem. 2023 Oct 24:e202300328. doi: 10.1002/cmdc.202300328. Online ahead of print.ABSTRACTAntimicrobial resistance (AMR) has interfered with effective treatment of microbial infection and increased the risk of microbial spread, illness, and deaths. The synergistic activities of combinations of antimicrobials offer satisfactory approaches to some extent. Structurally diverse naphthoquinones (NQs) including menadione (-CH3 at C-2) exhibit substantial antimicrobial activities against multidrug-resistant (MDR) pathogens. We explored the combinations of menadione with antibiotic ciprofloxacin or ampicillin against Staphyl...
Source: ChemMedChem - October 24, 2023 Category: Chemistry Authors: Nishigandha S Mone Sahil Syed Palanisamy Ravichandiran Ekta E Kamble Karishma R Pardesi Sunita Salunke-Gawali Mansi Rai Ajay Vikram Singh Sarada Prasad Dakua Byung-Hyun Park Dong Jin Yoo Surekha K Satpute Source Type: research

Terpene-functionalized Fluoroquinolones as Potential Antimicrobials: Synthesis and Properties
This study was the first to synthesize terpene-containing conjugates of fluoroquinolones, ciprofloxacin and norfloxacin, and to evaluate their antibacterial activity against gram-positive methicillin sensitive (MSSA) and methicillin resistant (MRSA) S. aureus, gram-negative P. aeruginosa as well as antifungal activity against C. albicans. The ability of obtained fluoroquinolones to inhibit S. aureus growth was found to depend upon the presence of a linker separating the bulky terpene and fluoroquinolone fragments, and this activity diminished with increasing its length. The highest activity against MSSA was demonstrated by...
Source: ChemMedChem - October 24, 2023 Category: Chemistry Authors: Evgeniy Sergeevich Izmest'ev Pestova V Svetlana Alena I Kolesnikova Diana R Baidamshina Airat R Kayumov Svetlana A Rubtsova Source Type: research

Synergistic and additive effects of menadione in combination with antibiotics on multidrug-resistant Staphylococcus aureus: Insights from structure-function analysis of NQs
ChemMedChem. 2023 Oct 24:e202300328. doi: 10.1002/cmdc.202300328. Online ahead of print.ABSTRACTAntimicrobial resistance (AMR) has interfered with effective treatment of microbial infection and increased the risk of microbial spread, illness, and deaths. The synergistic activities of combinations of antimicrobials offer satisfactory approaches to some extent. Structurally diverse naphthoquinones (NQs) including menadione (-CH3 at C-2) exhibit substantial antimicrobial activities against multidrug-resistant (MDR) pathogens. We explored the combinations of menadione with antibiotic ciprofloxacin or ampicillin against Staphyl...
Source: ChemMedChem - October 24, 2023 Category: Chemistry Authors: Nishigandha S Mone Sahil Syed Palanisamy Ravichandiran Ekta E Kamble Karishma R Pardesi Sunita Salunke-Gawali Mansi Rai Ajay Vikram Singh Sarada Prasad Dakua Byung-Hyun Park Dong Jin Yoo Surekha K Satpute Source Type: research

Terpene-functionalized Fluoroquinolones as Potential Antimicrobials: Synthesis and Properties
This study was the first to synthesize terpene-containing conjugates of fluoroquinolones, ciprofloxacin and norfloxacin, and to evaluate their antibacterial activity against gram-positive methicillin sensitive (MSSA) and methicillin resistant (MRSA) S. aureus, gram-negative P. aeruginosa as well as antifungal activity against C. albicans. The ability of obtained fluoroquinolones to inhibit S. aureus growth was found to depend upon the presence of a linker separating the bulky terpene and fluoroquinolone fragments, and this activity diminished with increasing its length. The highest activity against MSSA was demonstrated by...
Source: ChemMedChem - October 24, 2023 Category: Chemistry Authors: Evgeniy Sergeevich Izmest'ev Pestova V Svetlana Alena I Kolesnikova Diana R Baidamshina Airat R Kayumov Svetlana A Rubtsova Source Type: research

Synergistic and additive effects of menadione in combination with antibiotics on multidrug-resistant Staphylococcus aureus: Insights from structure-function analysis of NQs
ChemMedChem. 2023 Oct 24:e202300328. doi: 10.1002/cmdc.202300328. Online ahead of print.ABSTRACTAntimicrobial resistance (AMR) has interfered with effective treatment of microbial infection and increased the risk of microbial spread, illness, and deaths. The synergistic activities of combinations of antimicrobials offer satisfactory approaches to some extent. Structurally diverse naphthoquinones (NQs) including menadione (-CH3 at C-2) exhibit substantial antimicrobial activities against multidrug-resistant (MDR) pathogens. We explored the combinations of menadione with antibiotic ciprofloxacin or ampicillin against Staphyl...
Source: ChemMedChem - October 24, 2023 Category: Chemistry Authors: Nishigandha S Mone Sahil Syed Palanisamy Ravichandiran Ekta E Kamble Karishma R Pardesi Sunita Salunke-Gawali Mansi Rai Ajay Vikram Singh Sarada Prasad Dakua Byung-Hyun Park Dong Jin Yoo Surekha K Satpute Source Type: research

Terpene-functionalized Fluoroquinolones as Potential Antimicrobials: Synthesis and Properties
This study was the first to synthesize terpene-containing conjugates of fluoroquinolones, ciprofloxacin and norfloxacin, and to evaluate their antibacterial activity against gram-positive methicillin sensitive (MSSA) and methicillin resistant (MRSA) S. aureus, gram-negative P. aeruginosa as well as antifungal activity against C. albicans. The ability of obtained fluoroquinolones to inhibit S. aureus growth was found to depend upon the presence of a linker separating the bulky terpene and fluoroquinolone fragments, and this activity diminished with increasing its length. The highest activity against MSSA was demonstrated by...
Source: ChemMedChem - October 24, 2023 Category: Chemistry Authors: Evgeniy Sergeevich Izmest'ev Pestova V Svetlana Alena I Kolesnikova Diana R Baidamshina Airat R Kayumov Svetlana A Rubtsova Source Type: research

Synergistic and additive effects of menadione in combination with antibiotics on multidrug-resistant Staphylococcus aureus: Insights from structure-function analysis of NQs
ChemMedChem. 2023 Oct 24:e202300328. doi: 10.1002/cmdc.202300328. Online ahead of print.ABSTRACTAntimicrobial resistance (AMR) has interfered with effective treatment of microbial infection and increased the risk of microbial spread, illness, and deaths. The synergistic activities of combinations of antimicrobials offer satisfactory approaches to some extent. Structurally diverse naphthoquinones (NQs) including menadione (-CH3 at C-2) exhibit substantial antimicrobial activities against multidrug-resistant (MDR) pathogens. We explored the combinations of menadione with antibiotic ciprofloxacin or ampicillin against Staphyl...
Source: ChemMedChem - October 24, 2023 Category: Chemistry Authors: Nishigandha S Mone Sahil Syed Palanisamy Ravichandiran Ekta E Kamble Karishma R Pardesi Sunita Salunke-Gawali Mansi Rai Ajay Vikram Singh Sarada Prasad Dakua Byung-Hyun Park Dong Jin Yoo Surekha K Satpute Source Type: research

Terpene-functionalized Fluoroquinolones as Potential Antimicrobials: Synthesis and Properties
This study was the first to synthesize terpene-containing conjugates of fluoroquinolones, ciprofloxacin and norfloxacin, and to evaluate their antibacterial activity against gram-positive methicillin sensitive (MSSA) and methicillin resistant (MRSA) S. aureus, gram-negative P. aeruginosa as well as antifungal activity against C. albicans. The ability of obtained fluoroquinolones to inhibit S. aureus growth was found to depend upon the presence of a linker separating the bulky terpene and fluoroquinolone fragments, and this activity diminished with increasing its length. The highest activity against MSSA was demonstrated by...
Source: ChemMedChem - October 24, 2023 Category: Chemistry Authors: Evgeniy Sergeevich Izmest'ev Pestova V Svetlana Alena I Kolesnikova Diana R Baidamshina Airat R Kayumov Svetlana A Rubtsova Source Type: research

Synergistic and additive effects of menadione in combination with antibiotics on multidrug-resistant Staphylococcus aureus: Insights from structure-function analysis of NQs
ChemMedChem. 2023 Oct 24:e202300328. doi: 10.1002/cmdc.202300328. Online ahead of print.ABSTRACTAntimicrobial resistance (AMR) has interfered with effective treatment of microbial infection and increased the risk of microbial spread, illness, and deaths. The synergistic activities of combinations of antimicrobials offer satisfactory approaches to some extent. Structurally diverse naphthoquinones (NQs) including menadione (-CH3 at C-2) exhibit substantial antimicrobial activities against multidrug-resistant (MDR) pathogens. We explored the combinations of menadione with antibiotic ciprofloxacin or ampicillin against Staphyl...
Source: ChemMedChem - October 24, 2023 Category: Chemistry Authors: Nishigandha S Mone Sahil Syed Palanisamy Ravichandiran Ekta E Kamble Karishma R Pardesi Sunita Salunke-Gawali Mansi Rai Ajay Vikram Singh Sarada Prasad Dakua Byung-Hyun Park Dong Jin Yoo Surekha K Satpute Source Type: research

Terpene-functionalized Fluoroquinolones as Potential Antimicrobials: Synthesis and Properties
This study was the first to synthesize terpene-containing conjugates of fluoroquinolones, ciprofloxacin and norfloxacin, and to evaluate their antibacterial activity against gram-positive methicillin sensitive (MSSA) and methicillin resistant (MRSA) S. aureus, gram-negative P. aeruginosa as well as antifungal activity against C. albicans. The ability of obtained fluoroquinolones to inhibit S. aureus growth was found to depend upon the presence of a linker separating the bulky terpene and fluoroquinolone fragments, and this activity diminished with increasing its length. The highest activity against MSSA was demonstrated by...
Source: ChemMedChem - October 24, 2023 Category: Chemistry Authors: Evgeniy Sergeevich Izmest'ev Pestova V Svetlana Alena I Kolesnikova Diana R Baidamshina Airat R Kayumov Svetlana A Rubtsova Source Type: research

Synergistic and additive effects of menadione in combination with antibiotics on multidrug-resistant Staphylococcus aureus: Insights from structure-function analysis of NQs
ChemMedChem. 2023 Oct 24:e202300328. doi: 10.1002/cmdc.202300328. Online ahead of print.ABSTRACTAntimicrobial resistance (AMR) has interfered with effective treatment of microbial infection and increased the risk of microbial spread, illness, and deaths. The synergistic activities of combinations of antimicrobials offer satisfactory approaches to some extent. Structurally diverse naphthoquinones (NQs) including menadione (-CH3 at C-2) exhibit substantial antimicrobial activities against multidrug-resistant (MDR) pathogens. We explored the combinations of menadione with antibiotic ciprofloxacin or ampicillin against Staphyl...
Source: ChemMedChem - October 24, 2023 Category: Chemistry Authors: Nishigandha S Mone Sahil Syed Palanisamy Ravichandiran Ekta E Kamble Karishma R Pardesi Sunita Salunke-Gawali Mansi Rai Ajay Vikram Singh Sarada Prasad Dakua Byung-Hyun Park Dong Jin Yoo Surekha K Satpute Source Type: research