In recent years, the use of bioconjugation as strategy for development of more specific and directed drugs has been widely researched. Tetrapyrrolic macrocycles are one of the most common families of organic compounds applied in medicinal chemistry, specifically for diagnosis and therapy. For optimization of their efficiency as therapeutic molecules, it is relevant to promote their linking to biomolecules capable of targeting altered cells. This work brings a new dimension to the literature by combining structural modification of biomolecules and polymers with pyrrole-based compounds. It will be of great interest to academicians, industrialists, and undergraduate and graduate students of chemistry, biosciences, and pharmacy since, as apart from the theoretical aspects, it discusses experimental components. Features: Discusses methods for protein modification Useful for academicians, industrialists and undergraduate and graduated students of chemistry, biosciences, and pharmacy Explains the synthesis of pyrrole-based molecules