Chemical synthesis of mouse cripto CFC variants.

Proteins

Istituto di Biostrutture e Bioimmagini del CNR, Sezione Biostrutture, Napoli, Italy.

Published: August 2006

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.

Download full-text PDF

Source
http://dx.doi.org/10.1002/prot.21043DOI Listing

Publication Analysis

Top Keywords

chemical synthesis
8
mouse cripto
8
cfc domain
8
w107 h104
8
synthesis mouse
4
cripto cfc
4
cfc variants
4
variants report
4
report time
4
time chemical
4

Similar Publications

Coumarin Analogues as Promising Anti-Obesity Agents: In Silico Design, Synthesis, and In Vitro Pancreatic Lipase Inhibitory Activity.

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 PDF

Metal-Assisted Synthesis of Diverse Porphyrinoids by Cyclization of an N-Confused Thia-Pentapyrrane.

Chem 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 PDF

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 PDF

FDA-approved drugs featuring macrocycles or medium-sized rings.

Arch 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 PDF

Eco-Friendly Fabrication of FeS QD-Chitosan Biopolymer Composites: Green Synthetic Approach.

Biopolymers

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.

View Article and Find Full Text PDF

Want AI Summaries of new PubMed Abstracts delivered to your In-box?

Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!