Professor Kiessling received an Sc.B. degree in chemistry at MIT, where she performed undergraduate research in organic synthesis with Professor Bill Roush. She received a Ph.D. degree in chemistry at Yale University for her research with Stuart L. Schreiber. She was an American Cancer Society postdoctoral fellow with Peter B. Dervan at California Institute of Technology. She then joined the faculty at the University of Wisconsin–Madison, where she became the Steenbock Professor of Chemistry, the Laurens Anderson Professor of Biochemistry, and the Director of the Keck Center for Chemical Genomics. In 2017, she returned to MIT as the Novartis Professor of Chemistry.

Professor Kiessling is a member of the American Academy of Arts & Sciences, the American Academy of Microbiology, the American Philosophical Society, and National Academy of Sciences. She is the founding Editor-In-Chief of the journal ACS Chemical Biology . She is an author of over 140 peer-reviewed journal articles, and an inventor on more than 28 US patents. She has advised approximately 100 graduate students and postdoctorates. Alumni from her research group are contributing through their positions as faculty members of distinguished research universities, medical schools, and colleges and as research scientists at innovative start-up companies, leading corporations, and government laboratories.