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Molecular medicine aims to understand the molecular mechanisms underlying disease pathogenesis in order to develop suitable diagnostic strategies and disease interventions. From this perspective, chemists can and have to play a pivotal role in the field of molecular medicine as chemists are molecular scientists. In 1949, the internationally renowned chemist Linus Pauling published his seminal work entitled ‘Sickle cell anemia, a molecular disease’, in Science, laying the groundwork for the field of molecular medicine. Over the past 70 years, chemistry has been one of the major forces pushing the field of molecular medicine to grow and evolve. Today, many important contributions made by chemists can be found in different subfields of molecular medicine, including molecular imaging, molecular diagnosis, molecular drug design and gene editing, et al. As in other areas of science and technology development, molecular medicine is thriving with active contributions of chemists and other molecular scientists. This special topic features biomedical scientists, physicians and chemists, mostly from Shanghai Jiao Tong University, to showcase the influence of chemistry on the field of molecular medicine. In their review, Guo-Qiang Chen et al. summarize some recent progress in applying chemical biology to explore the molecular mechanisms of carcinogenesis, outlining several new strategies for chemistry to probe cellular activities. Yingxuan Chen and Jing-Yuan Fang et al. discuss recent findings related to the crosstalk between microbiota and epigenetic modifications in colorectal cancer. Bing Su et al. review Sin1, a key adaptor molecule involved in the regulation and function of the mammalian target of rapamycin (mTOR) signaling pathway. Xinyuan Zhu and Deyue Yan et al. introduce recent advances in supramolecular designs of nanoscale drug delivery systems. In the perspective article by XiaweiWei and YuquanWei et al., opportunities and challenges in the use of nanoparticles for nucleic acid therapeutics are discussed.GuangjunNie andYuliangZhao et al. review some recent trends in nanomedicine design and further discuss challenges and opportunities in the development of next-generation nanomedicines. The research highlight article by Chaoyong Yang et al. reports a recent finding tracking the levels of circulating exosomal PD-L1may help to predict the response of patients and identify the possible reasons for success or failure of anti-PD-1 therapy. An interviewwithFengShao and Weihong Tan is also included in this special topic. They share their personal views of the impact of chemistry on the biomedical sciences, in addition to their opinions onbiomedical research methods and career development. To effectively tackle challenging problems in molecular medicine, interdisciplinary approaches and collaborations are essential. We hope this special topic will inspire more researchers from different disciplines of science, engineering, pharmacy and medicine, as well as commercial companies, to join in the exciting field of molecular medicine. Finally, we would like to take this opportunity to express our gratitude to all the authors, reviewers, and theNSReditorial staff for their efforts in making this special topic possible.