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LncTarD1.0 provides key lncRNA-target regulations, their influenced functions and lncRNA-mediated regulatory mechanisms in human diseases. LncTarD includes 2822 experimentally-supported functional regulations and expression associations in 177 human diseases, including 475 lncRNAs, 391 miRNAs, 774 protein-coding genes and 140 biological functions. We also manually curated a wealth of information: (i) containing key targets and important biological functions (such as cell proliferation, EMT and angiogenesis) driven by disease-related lncRNAs in human diseases. (ii) lncRNA-mediated regulatory mechanisms in human diseases, including transcriptional regulation, epigenetic regulation, chromatin looping, ceRNA or sponge, interacting with mRNA and interacting with protein. (iii) lncRNA-target regulations are responsible for drug resistance or sensitivity involving 52 drugs in 41 human diseases. Additionally, TCGA pan-cancer transcriptome data (33 cancer types) were also integrated into LncTarD to help characterize dynamics of functional lncRNA-target regulations. LncTarD can serve as a timely and valuable resource for understanding functions and molecular mechanisms of lncRNA deregulation in disease pathogenesis, which will help to identify novel and sensitive biomarkers and therapeutic targets in human diseases.