Drought impacts severely crop photosynthesis and productivity. Development of transgenic rice overexpressing maize phosphoenolpyruvate carboxylase (PEPC) is a promising strategy for improving crop production under drought stress. However, the molecular mechanisms of protection from PEPC are not yet clear. The objective of this study was: first, to characterize the response of individual photosynthetic components to drought stress; second, to study the physiological and molecular mechanisms underlying the drought tolerance of transgenic rice (cv. Kitaake) over-expressing maize PEPC. Our results showed that PEPC overexpressing improved the ability of transgenic rice to conserve water and pigments during drying as compared to wild type. Despite the fact that drought induced reactive oxygen species and damaged photosystems (especially, PSI) in both lines, higher intercellular CO2 concentration protected the photosynthetic complexes, peptides, and also ultrastructure of thylakoid membranes against the oxidative damage in transgenic rice. In conclusion, although photosynthetic apparatus suffered an inevitable and asymmetric impairment during drought conditions, PEPC effectively alleviated the oxidative damage on photosystems and enhanced the drought tolerance by increasing intercellular CO2 concentration. Our investigation provided critical clues for exploring the feasibility of using C4 photosynthesis to increase the yield of rice under the aggravated global warming., W. J. Shen, G. X. Chen, J. G. Xu, Y. Jiang, L. Liu, Z. P. Gao, J. Ma, X. Chen, T. H. Chen, and C. F. Lv., and Obsahuje seznam literatury