The inhibition of protein-protein interactions using small molecules is a viable approach for the treatment of a range of pathological conditions that result from a malfunctioning of these interactions. Our strategy for the design of such agents involves the mimicry of side-chain residues on one face of the alpha-helix; these residues frequently play a key role in mediating protein-protein inte...

Tethering has been extensively used to study small molecule interactions with proteins through reversible disulfide bond forming reactions to cysteine residues. We describe the adaptation of Tethering to the study of small molecule binding to RNA using a thiol-containing adenosine analog (ASH). Among 30 disulfide-containing small molecules screened for efficient Tethering to ASH-bearing RNAs de...

background: antifungal drug resistance and few numbers of available drugs limit therapeutic options against fungal infections. the present study was designed to discover new antifungal drugs.   m aterials and methods: this study was carried out in two separate steps, that is, in silico lead identification and in vitro assaying of antifungal potential. a structural data file of a ternary complex...

The tumor suppressor p53 is inactivated by mutation in about half of all tumors, making mutant a prime target for cancer therapy. Missense mutations R248W, R273H and R248Q are included the five most frequent total lead to more than 630 000 new diagnosed cases diseases world every year. These mutations, located at or near protein-DNA interface, inactivation loss direct p53-DNA interactions, caus...

A chemical ligation method for construction of DNA-encoded small-molecule libraries has been developed. Taking advantage of the ability of the Klenow fragment of DNA polymerase to accept templates with triazole linkages in place of phosphodiesters, we have designed a strategy for chemically ligating oligonucleotide tags using cycloaddition chemistry. We have utilized this strategy in the constr...