title: Design, synthesis and characterization of a peptide able to bind proteins of the KCTD family: implications for KCTD-cullin 3 recognition.
abstract: Pox virus Zinc/Bric-à-brac, Tramtrack and Broad (POZ/BTB) is a widespread domain detected in proteins involved in a variety of biological processes. Human genome analyses have unveiled the presence of POZ/BTB domain in a class of proteins (KCTD) whose role as important players in crucial biological processes is emerging. The development of new molecular entities able to interact with these proteins and to modulate their activity is a field of relevant interest. By using molecular modeling and literature mutagenesis analyses, we here designed and characterized a peptide that is able to interact with submicromolar affinities with two different members (KCTD11 and KCTD5) of this family. This finding suggests that the tetrameric KCTD11 and the pentameric KCTD5 are endowed with a similar cavity at the subunit-subunit interface deputed to the Cul3 binding, despite their different oligomeric states.
authors: Institute of Biostructures and Bioimaging, CNR, 80134 Napoli, Italy.
authors: Luciano
authors: L
authors: Pirone
authors: Stefania
authors: S
authors: Correale
authors: Ivan
authors: I
authors: de Paola
authors: Laura
authors: L
authors: Zaccaro
authors: Giuseppina
authors: G
authors: De Simone
authors: Luigi
authors: L
authors: Vitagliano
authors: Emilia
authors: E
authors: Pedone
authors: Sonia
authors: S
authors: Di Gaetano
mesh_terms: D018797:Cell Cycle Proteins; D002942:Circular Dichroism; D044842:Cullin Proteins / Q000378:metabolism*; D004797:Enzyme-Linked Immunosorbent Assay; D006801:Humans; D010455:Peptides / Q000138:chemical synthesis / Q000737:chemistry / Q000378:metabolism*; D015221:Potassium Channels / Q000378:metabolism*; D011485:Protein Binding; D017433:Protein Structure, Secondary; D014166:Transferases
chemical_list: C503645:CUL3 protein, human; D018797:Cell Cycle Proteins; D044842:Cullin Proteins; C521187:KCTD5 protein, human; D010455:Peptides; D015221:Potassium Channels; C488725:KCTD11 protein, human; D014166:Transferases