Quantum Dots (QDs) are a special type of engineered nanomaterials with outstanding optoelectronic properties make them as a very promising alternative to conventional luminescent dyes for biomedical applications, including biomolecule targeting, luminescence imaging as well as in drug delivery.A key parameter to ensure successful biomedical applications of QDs is that the surface of these nanomaterials should be modified with appropriate functional groups to ensure stability in aqueous solutions and conjugated with recognition elements capable to ensure an efficient tagging of the biomolecules of interest.Here, we present a review summarizing most relevant strategies for QDs surface modification and for their conjugation to biomolecules for preparation of nanoplatforms for luminescent biomolecule sensing and imaging-guided targeting. Applications of conjugations of photoluminescent QDs with different biomolecules in both in vitro and in vivo chemical sensing, immunoassays or luminescence imaging are revised. Recent progress in application of functionalized QDs in ultrasensitive detection in bioanalysis, diagnostics and imaging strategies developments are here included. Finally, some key future research goals in the progress of bioconjugation of QDs for diagnosis are identified, including novel synthetic approaches, the need of exhaustive characterization of bioconjugates or the design of signal amplification schemes.