Inspired by the great impact of chemical probes in exploring biology and by the synergism of interdisciplinary approaches, the research in the Hong Group focuses on developing chemical tools and strategies to expand pharmacological modulation of biological processes. (1) First, we synthesize biologically important natural products. Then, we explore their modes of action in order to investigate intracellular signaling pathways and identify novel drug targets. (2) To rapidly construct the molecular complexity and structural diversity of target molecules, we develop unique and efficient synthetic strategies. (3) In addition, we design and develop small molecule probes to both interrogate and manipulate biological systems important to human health. Many of these research activities in the Hong Group have been built upon interdisciplinary and collaborative efforts. Through interdisciplinary approaches, including organic synthesis, molecular and cell biology, and in vivo studies, the cellular components and molecular events that embody cancer, autoimmune disease, and anticancer and antibiotics resistance have been systematically explored. Small molecules employed in these studies could also advance the development of novel therapeutics for treatment of human diseases.