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Weight-reducing effects of the plasma protein encoded by the obese gene.
Injection of wild-type mice twice daily with the mouse protein resulted in a sustained 12 percent weight loss, decreased food intake, and a reduction of body fat from 12.2 to 0.7 percent, suggesting that the OB protein serves an endocrine function to regulate body fat stores.
Winged helix proteins.
Structure of the winged-helix protein hRFX1 reveals a new mode of DNA binding
A 1.5 Å-resolution structure of two copies of the DBD of human RFX1 (hRFX1) binding cooperatively to a symmetrical X-box is presented and a new model for interactions between linker histones and DNA is proposed.
HDEA, a periplasmic protein that supports acid resistance in pathogenic enteric bacteria.
It is suggested that HDEA may support chaperone-like functions during the extremely acidic conditions, and is activated by a dimer-to-monomer transition at acidic pH, leading to suppression of aggregation by acid-denatured proteins.
Forces contributing to the conformational stability of proteins
- C. Pace, B. Shirley, Marsha McNutt, K. Gajiwala
- Biology, ChemistryFASEB journal : official publication of the…
- 1 January 1996
It is suggested that hydrogen bonding and the hydrophobic effect make large but comparable contributions to the stability of globular proteins.
KIT kinase mutants show unique mechanisms of drug resistance to imatinib and sunitinib in gastrointestinal stromal tumor patients
- K. Gajiwala, Joe C. Wu, G. Demetri
- Biology, ChemistryProceedings of the National Academy of Sciences
- 3 February 2009
Results show that sunitinib targets the autoinhibited conformation of WT KIT and that the D816H mutant undergoes a shift in conformational equilibrium toward the active state, providing a structural and enzymologic explanation for the resistance profile observed with the KIT inhibitors.
An oral SARS-CoV-2 Mpro inhibitor clinical candidate for the treatment of COVID-19
The discovery and characterization of a drug against the main protease involved in the cleavage of polyproteins involved in viral replication is reported, which can be administered orally, has good selectivity and safety profiles, and protects against infection in a mouse model.
Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19
Preclinical experiments reveal 4 (PF-00835231) as a potent inhibitor of CoV-2 3CLpro with suitable pharmaceutical properties to warrant further development as an intravenous treatment for COVID-19.
Crystal structures of bacterial FabH suggest a molecular basis for the substrate specificity of the enzyme
Structural analysis of a set of proteins resulting from a bacterial genomics project
This work identified homologs for 49 of the 60 unique sequences represented by the SGX structures, indicating that, for bacterial structures that are relatively easy to express, purify, and crystallize, the structural coverage of gene space is proceeding rapidly.