Methylsulfonyl Benzothiazole (MSBT): A Selective Protein Thiol Blocking Reagent

A new thiol blocking reagent, methylsulfonyl benzothiazole, was discovered. This reagent showed good selectivity and high reactivity for protein thiols

Light-Induced Hydrogen Sulfide Release from “Caged” <i>gem</i>-Dithiols

“Caged” <i>gem</i>-dithiol derivatives that release H₂S upon light stimulation have been developed. This new class of H₂S donors was proven, by various spectroscopic methods, to generate H₂S in an aqueous/organic medium as well as in cell culture

Controllable Hydrogen Sulfide Donors and Their Activity against Myocardial Ischemia-Reperfusion Injury

Hydrogen sulfide (H₂S), known as an important cellular signaling molecule, plays critical roles in many physiological and/or pathological processes. Modulation of H₂S levels could have tremendous therapeutic value. However, the study on H₂S has been hindered due to the lack of controllable H₂S releasing agents that could mimic the slow and moderate H₂S release <i>in vivo</i>. In this work we report the design, synthesis, and biological evaluation of a new class of controllable H₂S donors. Twenty-five donors were prepared and tested. Their structures were based on a perthiol template, which was suggested to be involved in H₂S biosynthesis. H₂S release mechanism from these donors was studied and proved to be thiol-dependent. We also developed a series of cell-based assays to access their H₂S-related activities. H9c2 cardiac myocytes were used in these experiments. We tested lead donors’ cytotoxicity and confirmed their H₂S production in cells. Finally we demonstrated that selected donors showed potent protective effects in an <i>in vivo</i> murine model of myocardial ischemia-reperfusion injury, through a H₂S-related mechanism

DataSheet_1_Redox integration of signaling and metabolism in a head and neck cancer model of radiation resistance using COSMRO.docx

Redox metabolism is increasingly investigated in cancer as driving regulator of tumor progression, response to therapies and long-term patients’ quality of life. Well-established cancer therapies, such as radiotherapy, either directly impact redox metabolism or have redox-dependent mechanisms of action defining their clinical efficacy. However, the ability to integrate redox information across signaling and metabolic networks to facilitate discovery and broader investigation of redox-regulated pathways in cancer remains a key unmet need limiting the advancement of new cancer therapies. To overcome this challenge, we developed a new constraint-based computational method (COSMro) and applied it to a Head and Neck Squamous Cell Cancer (HNSCC) model of radiation resistance. This novel integrative approach identified enhanced capacity for H2S production in radiation resistant cells and extracted a key relationship between intracellular redox state and cholesterol metabolism; experimental validation of this relationship highlights the importance of redox state in cellular metabolism and response to radiation.</p

DataSheet_2_Redox integration of signaling and metabolism in a head and neck cancer model of radiation resistance using COSMRO.xlsx

Redox metabolism is increasingly investigated in cancer as driving regulator of tumor progression, response to therapies and long-term patients’ quality of life. Well-established cancer therapies, such as radiotherapy, either directly impact redox metabolism or have redox-dependent mechanisms of action defining their clinical efficacy. However, the ability to integrate redox information across signaling and metabolic networks to facilitate discovery and broader investigation of redox-regulated pathways in cancer remains a key unmet need limiting the advancement of new cancer therapies. To overcome this challenge, we developed a new constraint-based computational method (COSMro) and applied it to a Head and Neck Squamous Cell Cancer (HNSCC) model of radiation resistance. This novel integrative approach identified enhanced capacity for H2S production in radiation resistant cells and extracted a key relationship between intracellular redox state and cholesterol metabolism; experimental validation of this relationship highlights the importance of redox state in cellular metabolism and response to radiation.</p