We report for the first time the chemical synthesis of refolded CFC domain of mouse Cripto (mCFC) and of two variants bearing mutations on residues W107 and H104 involved in Alk4 binding. The domains undergo spontaneous and quantitative refolding in about 4 h, yet with very different kinetics. Disulfide linkages have been assessed by enzyme digestion and mass spectrometry analysis of resulting fragments, and the first experimental studies on structural organization have been conducted by circular dichroism spectroscopy under different pH conditions. Upon refolding, the domains considerably change their conformations, although they do not assume canonical structures, and become highly resistant to enzyme degradation. A comparative study of receptor binding shows that the CFC domain can bind Alk4 and confirms the importance of W107 and H104 for receptor recognition.
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http://dx.doi.org/10.1002/prot.21043 | DOI Listing |
Chem Biol Drug Des
January 2025
Laboratory of Natural Product Chemistry, Department of Pharmacy, Birla Institute of Technology and Science, Pilani (BITS Pilani), Pilani, Rajasthan, India.
A set of coumarin-3-carboxamide analogues were designed, synthesized, and evaluated for their ability to impede pancreatic lipase (PL) activity. Out of all the analogues, 5dh and 5de demonstrated promising inhibitory activity against PL, as indicated by their respective IC values of 9.20 and 11.
View Article and Find Full Text PDFChem Asian J
January 2025
East China University of Science and Technology, Institute of Fine Chemicals, Meilong Road, 200237, Shanghai, CHINA.
Oxidation of thia-pentapyrrane S-P4 with terminal β-linked pyrrole and thiophene units in the presence of various metal ions has been found to afford distinct porphyrinoids. Specifically, N-confused thiasapphyrin (1), Cu(III) norrole (2), neo-confused phlorin (3), and p-benzinorrole (4) were obtained, when S-P4 was oxidized with p-chloranil in acetonitrile in the presence of Ni2+, Cu2+, Cd2+, and Co2+, respectively. The structures of 1-4 have been clearly elucidated by NMR spectroscopy, HRMS, and X-ray crystal diffraction (for 2-4).
View Article and Find Full Text PDFAngew Chem Int Ed Engl
January 2025
Nanjing Tech University, College of Chemical Engineering, Nanjing, CHINA.
The wide application of zeolite Y in petrochemical industry is well known as one of the milestones in zeolite chemistry and heterogeneous catalysis. However, the traditional organic-free synthesis typically produces (hydro)thermally unstable zeolite Y with Si/Al atomic ratio (SAR) less than 2.5.
View Article and Find Full Text PDFArch Pharm (Weinheim)
January 2025
Jiangsu Co-Innovation Center of Efficient Processing and Utilization of Forest Resources, College of Chemical Engineering, Nanjing Forestry University, Nanjing, China.
Macrocycles or medium-sized rings offer diverse functionality and stereochemical complexity in a well-organized ring structure, allowing them to fulfill various biochemical functions, resulting in high affinity and selectivity for protein targets, while preserving sufficient bioavailability to reach intracellular compartments. These features have made macrocycles attractive candidates in organic synthesis and drug discovery. Since the 20th century, more than three-score macrocyclic drugs, including radiopharmaceuticals, have been approved by the US Food and Drug Administration (FDA) for treating bacterial and viral infections, cancer, obesity, immunosuppression, inflammatory, and neurological disorders, managing cardiovascular diseases, diabetes, and more.
View Article and Find Full Text PDFBiopolymers
March 2025
Department of Chemistry, School of Chemical and Physical Sciences, Lovely Professional University, Phagwara, India.
In this paper, we offer a unique green synthetic approach for producing iron sulfide quantum dots (FeS QD)-chitosan composites using gel chemistry. The technique uses the environmental features of chitosan, a biocompatible and biodegradable polysaccharide, and the excellent electrical properties of FeS QDs. By sustainable chemistry principles, the synthesis process is carried out under gentle settings, using aqueous solutions and avoiding hazardous solvents and strong chemicals.
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