Knowledge deriving from the biochemical signalling controlling tissue morphogenesis in embryonic and adult tissues offers the potential for the development of new therapeutic tools in regenerative medicine. To facilitate and control the cell-to-cell communication pathways, peptides and polymers can be synthesised that are capable of exposing to the damaged tissue either specific cell bioligands or functional groups able to bind bioactive molecules. These macromolecules would thus act as biomimetic pro-morphogens contributing to the generation of biochemical signalling gradients. In the first case, biomaterial scaffolds would be tethered with bioligands specifically encouraging the colonisation of “intermediate organisers” able to process morphogens/growth factors secreted by the “organiser” cells. In the second case, the exposure of functional groups of natural or synthetic origin able to capture endogenous morphogens could contribute to the establishment of biochemical gradients. Finally, in the clinical cases where tissue regeneration potential has significantly been comporomise, the use of these so-called synthetic pro-morphogens could be combined with that of specific peptidic growth factor analogues to generate ex novo completely synthetic gradients.