Bioorganic Med Chem 11:4881–4889īrown N, Jacoby E (2006) On scaffolds and hopping in medicinal chemistry. J Pept Sci 11:713–726īouget K, Aubin S, Delcros J, Arlot-Bonnemainsc Y, Baudy-Floc’ha M (2003) Hydrazino-Aza and N-Azapeptoids with therapeutic potential as anticancer agents. J Med Chem 51:2468–2480īorghouts C, Kunz C, Groner B (2005) Current strategies for the development of peptide-based anti-cancer therapeutics. J Mol Biol 385:1052–1063īoehm M, Wu T, Claussen H, Lemmen C (2008) Similarity searching and scaffold hopping in synthetically accessible combinatorial chemistry spaces. Chem Biodivers 6:1178–1184īiancalana M, Makabe K, Koide A, Koide S (2009) Molecular mechanism of thioflavin-T binding to the surface of beta-rich peptide self-assemblies. J Med Chem 50:2708–2717īertinetti BV, Pena NI, Cabrera GM (2009) An antifungal tetrapeptide from the culture of Penicillium canescens. Futur Med Chem 3:1787–1808īergmann R, Linusson A, Zamora I (2007) SHOP: scaffold hopping by GRID-based similarity searches. PNAS 106:262–267īaines AT, Xu D, Der CJ (2011) Inhibition of Ras for cancer treatment: the search continues. J Pept Sci 14:524–527Īrtis DR, Lina JJ, Zhang C, Wang W, Mehra U, Perreault M, Erbe D, Krupka HI, England BP, Arnold J, Plotnikova AN, Marimuthua A, Nguyena H, Will S, Signaevskyc M (2009) Scaffold-based discovery of indeglitazar, a PPAR pan-active anti-diabetic agent. FASEB J 18:152–154Īpplet C, Wessolowski A, Dathe M, Schmieder P (2008) Structures of cyclic, antimicrobial peptides in a membrane-mimicking environment define requirements for activity. J Chem Inf Model 45:1313–1323Īli M, Hicks AER, Hellawell PG, Thoma G, Norman KE (2004) Polymers bearing sLex-mimetics are superior inhibitors of E-selectin-dependent leukocyte rolling in vivo. J Med Chem 53:5002–5011Īhlstro MM, Ridderstro M, Luthman K, Zamora I (2005) Virtual screening and scaffold hopping based on GRID molecular interaction fields. The review gives an insight into the future panoramas of drug development and identifies few peptide scaffolds having diverse potential with chemical modifications.Īgrafiotis DK, Wiener JJM (2010) Scaffold explorer: an interactive tool for organizing and mining structure-activity data spanning multiple chemotypes. Diverse forms of such peptidomimetics with respect to their structure and applications are discussed alongwith the mimetics which reached clinical trials. Free energy based conformational analysis of peptidomimetics provides details of their structure–activity relationships. provide an anticipative picture for the therapeutic use of scaffold structures. Synthetic peptidomimetics like aptamers, dendrimers, arylamide foldamers, β peptides, d peptides etc. We have surveyed the scaffold-based compounds being used for anticancer, antiinfective, antiinflammatory and antidiabetic activities. Mimicking the natural scaffolds with desirable modifications i.e., scaffold-hopping will decrease the enormous efforts of chemical syntheses and testing for drug development. Nature modifies a premature peptide with respect to a basic scaffold structure to create a mature and active peptide. Peptide scaffolds are diverse chemical structures providing a major base for drug development.
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