Covalent Modifiers

FEBRUARY 25, 2025

4c15843 Peptide macrocycles are promising therapeutics for a variety of disease indications due to their overall metabolic stability and potential to make highly selective binding interactions with targets. Boyd, Lei Wang, Ralf Bartenschlager, and Matthew Bogyo Journal of the American Chemical Society 2025 DOI: 10.1021/jacs.4c15843

Metabolic Stability 100

Metabolic Stability Virus Disease Drugs 100

ASPET

MAY 22, 2024

This study highlights these PK parameters and the importance of using pharmacologically relevant pre-clinical doses to study pharmacodynamics (PD) in stroke and related neurodegenerative diseases. In vitro assays examined brain tissue binding and metabolic stability.

Pharmacokinetics 100

Pharmacokinetics Metabolic Stability Clinical Pharmacology Disease 100

Chemical Biology and Drug Design

OCTOBER 5, 2023

Abstract Sickle cell disease (SCD) is the most common genetic disorder, affecting millions of people worldwide. However, the aldehyde functional group metabolic instability has severly hampered their development, except for voxelotor, which was approved in 2019 for SCD treatment.

Metabolic Stability 100

Metabolic Stability Treatment Disease Research 100

DrugBank

OCTOBER 17, 2024

For instance, Insilico Medicine , an AI-driven drug discovery company, has leveraged generative models to design novel molecules with desired properties, such as improved solubility and metabolic stability.    Moreover, data science designs novel drugs, such as antibody-drug conjugates (ADC) and bispecific antibodies.

Drug Development 98

Drug Development Metabolic Stability Clinical Trials Drugs 98

Metabolite Tales Blog

AUGUST 2, 2023

To curb O -glucuronidation at that position, a gem-dimethyl group was incorporated, which not only boosted metabolic stability but also resulted in increased potency of “compound 17” An earlier example of how to manage glucuronidation by steric hindrance is illustrated in “compound 25” in the paper by Zhang et al.,

Metabolic Stability 52

Metabolic Stability Drugs Disease 52

Drug Target Review

JUNE 12, 2023

The system optimised the molecules that were most likely to succeed in terms of potency, metabolic stability, synthetic accessibility, and more. The novel molecules were further ranked based on their ADME and selectivity profiles.

Metabolic Stability 92

Metabolic Stability Clinical Trials Small Molecule Pharmacokinetics 92

Drug Target Review

SEPTEMBER 20, 2023

Complex challenges such as metabolic stability or absorption, distribution, metabolism or excretion (ADME) properties could be better predicted, accurately filtering out poor candidates and streamlining discovery. To really benefit from AI, the pharmaceutical industry must be more open to data sharing.

Drugs 105

Drugs Metabolic Stability Computational Chemistry Pharmaceuticals 105