Irreversible Inhibitors
Irreversible Inhibitors - Related Videos
03:50
Irreversible Electroporation: A Technique for Ablating Pancreatic Tumor in Mouse
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2023
This video describes the procedure for performing irreversible electroporation (IRE) for non-thermal ablation of pancreatic tumors in mice. Both subcutaneous (SQ) and orthotopic tumors can be successfully treated with IRE in a highly controlled setting, facilitating various studies post-procedure.
14:05
A Murine Model of Irreversible and Reversible Unilateral Ureteric Obstruction
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Cited by 47 •
2014
The murine model of irreversible unilateral ureteric obstruction (UUO) is presented together with the model of reversible UUO in which the ureteric obstruction is relieved by anastomosis of the severed ureter into the bladder. These models enable the study of renal inflammation and scarring as well as tissue remodeling.
01:14
Reversible and Irreversible Processes
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2023
The thermodynamic processes can be classified into reversible and irreversible processes. The processes that can be restored to their initial state are called reversible processes. It is only possible if the process is in quasi-static equilibrium, i.e., it takes place in infinitesimally small steps, and the system remains at equilibrium However, these are ideal processes and do not occur naturally. An ideal system undergoing a reversible process is always in thermodynamic equilibrium within...
01:52
Eukaryotic Transcription Inhibitors
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2020
Certain biochemical processes, such as embryonic development and cell growth regulation, depend on the repression of specific genes. DNA binding proteins known as eukaryotic transcription inhibitors regulate the repression of gene expression in eukaryotes. The presence of these inhibitors at the required location and time in the cell is triggered by the presence of hormones and additional signals from other cells. Eukaryotic transcription inhibitors usually contain two distinct domains, a DNA...
06:17
Covalent Fragment Screening Using the Quantitative Irreversible Tethering Assay
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2025
The quantitative irreversible tethering (qIT) assay is a fluorescence-based method of identifying covalent fragments that selectively engage with a target protein. Here, a detailed protocol is outlined to describe the qIT assay, with example results included.
FAQs
Persistence results from covalent modification of a critical amino acid at the target protein’s active site. Once that bond prevents catalysis, removing unbound compound does not restore the already modified protein. Functional recovery therefore depends on production of new target protein by the cell, creating a longer-lasting effect than simple removal of free inhibitor would provide.
Selectivity depends on whether the compound forms its covalent bond with the intended amino acid at the target’s active site rather than affecting other proteins. Precise targeting can support useful suppression of a chosen function, whereas inadequate selectivity may complicate pharmacological effects and safety assessment. This makes target recognition central to irreversible inhibitor design.
Dose is important because the compound can produce effects that outlast its presence in the surrounding system. The duration of suppression also depends on how quickly cells synthesize new target protein, since recovery requires replacement of the inactivated protein. Consequently, both exposure level and the timing of protein renewal must be considered when interpreting pharmacological outcomes.
A practical comparison is to measure target activity during inhibitor exposure and again after unbound inhibitor has been removed. If catalysis remains blocked after removal, the result supports persistent inactivation rather than an effect that depends only on continued compound availability. Observing later recovery can further indicate that newly synthesized protein has restored activity.
They may be useful when prolonged suppression of a target is desirable, because their effects can continue after the inhibitor is no longer freely present. This property can help researchers investigate how sustained target inactivation changes drug action and can inform development of therapies intended to maintain pharmacological effects over an extended period.
Selectivity, dose, and the possibility of prolonged toxicity require careful evaluation. A compound that remains functionally important after unbound drug is removed may be difficult to reverse immediately if its target is suppressed excessively or if selectivity is insufficient. These considerations are relevant both to drug-development decisions and to clinical assessment of sustained pharmacological effects.