The pharmacological and adverse effect profiles of the two approved therapies for IPF make the development of new therapies challenging. Considering the similarity of the characteristics of drug candidates to Standard of Care is important in defining positioning and development strategies for this disease.
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http://dx.doi.org/10.1016/j.drudis.2020.09.019 | DOI Listing |
J Med Chem
January 2025
Department of Organic Chemistry and Technology, Budapest University of Technology and Economics, Műegyetem rkp. 3, H-1111Budapest, Hungary.
The binding ability of human serum albumin (HSA) on active pharmaceutical ingredients (APIs) is one of the most important parameters in the early stages of drug discovery. In this study, an immobilized HSA-based tool was developed for the rapid and easy in vitro screening of API binding. The work explored the serious incompleteness in the identification of HSA used for in vitro screening published in the last five years.
View Article and Find Full Text PDFJ Med Chem
January 2025
Department of Drug Discovery and Biomedical Sciences, College of Pharmacy, University of South Carolina, Columbia SC-29208, United States.
The physiopathology of cardiac and related disorders is strongly associated with BCAA metabolic imbalance. BDK, a negative regulator of the BCKDH complex, is significant in BCAA catabolic dysfunction. A Clinically potential BDK inhibitor, PF-07328948, with excellent drug-like properties, is under phase-1 clinical trials for CVD metabolic disorders.
View Article and Find Full Text PDFJ Med Chem
January 2025
Department of Chemical Biology and Therapeutics, St. Jude Children's Research Hospital, Memphis, Tennessee 38105, United States.
PROTACs usually occupy physicochemical space outside the one defined by classical drug-like molecules, which often presents considerable challenges in their optimization and development for oral administration. We have previously reported phenyl glutarimide (PG)-based BET PROTAC SJ995973, with improved overall degradation and antiproliferative activities compared to its direct thalidomide-based analogue dBET1, but similarly poor pharmacokinetic profile. To further demonstrate the PG utility, we describe here optimization efforts that led to the discovery of an orally bioavailable BET-PROTAC SJ44236 (), and results of a comprehensive comparative study with analogues containing alternative CRBN-directing warheads.
View Article and Find Full Text PDFJ Chromatogr Sci
January 2025
School of Pharmacy, Shanghai University of Medicine and Health Sciences, 279 Zhouzhu Road, Pudong New District, Shanghai 201318, China.
As a traditional Chinese medicine, Sanao decoction (SAD) has been used to treat chronic obstructive pulmonary disease (COPD) for multi-years. However, the potential mechanism and targets for its effects of SAD remain unknown. The 94 components of SAD were identified by UPLC-LTQ-Orbitrap MS.
View Article and Find Full Text PDFSci Adv
January 2025
Department of Biophysics, Institute of Quantum Biophysics, Sungkyunkwan University, Suwon 16419, Republic of Korea.
Optical resolution photoacoustic imaging of uneven samples without z-scanning is transformative for the fast analysis and diagnosis of diseases. However, current approaches to elongate the depth of field (DOF) typically imply cumbersome postprocessing procedures, bulky optical element ensembles, or substantial excitation beam side lobes. Metasurface technology allows for the phase modulation of light and the miniaturization of imaging systems to wavelength-size thickness.
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