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Angiogenesis is a complex process of development of new vessels from pre-existing vasculature. In human pathology, neovascularization is associated with excessive or insufficient vessel growth that results in initiation and development of a variety of diseases. The major pharmacological approach for the investigation of excessive angiogenesis is directed to designing new pharmaceutics to inhibit pathological vessel growth. In this context, blocking of the vascularization process in cancer progression gets the most attention. This type of biomedical research resulted in FDA approval of an anti-VEGF therapy in metastatic colorectal cancer by the humanized monoclonal antibody, bevacizumab, which is also in clinical trials for other types of tumors such as malignant gliomas. Surface receptors that are expressed on endothelial cells are also considered as a potential target for angiostatic therapy. Much attention is devoted to growth factor receptors, as well as certain integrins. In these cases, the most advanced clinical studies ongoing are with VEGFRs and αvβ3 integrin, although FGFRs and α5β1, α1β1 and α2β1 integrins are also in consideration. Targeting of intracellular signaling molecules in angiogenesis also has a long history of investigation. The pharmacological blocking of pro-angiogenic factors is mainly achieved by using humanized monoclonal antibodies or low molecular weight, synthetic compounds. Use of these compounds in therapy is usually associated with balancing of effectiveness and side effects, as well as their half-life time in the blood of patients. In the case of brain tumors, penetration of the blood brain barrier by these anti-angiogenesis agents is also very important. Analogical strategy is applied for developing pharmaceutics that will be useful in the promotion of angiogenesis. This treatment is essential for human diseases, in which insufficient angiogenesis is an important factor for progression of pathology. In this context, the most investigated are heart diseases, which require restoration of vasculature. The review articles included to this issue of Current Pharmaceutical Design, summarize recent information from the field of pharmacology of angiogenesis that may be useful for readers working in basic biomedical science and for clinicians to update information about the trends in modern cancer and heart disease therapies. In the first paper [1], the author summarizes the major approaches that were investigated during a history of angiogenesis research. Targeting vessel growth in developing solid cancers was initially proposed by Judah Folkman in the early seventies of XX century. As a surgeon he observed an increased vascularization ratio of tumor in comparison with adjacent non pathologically affected tissue. Following his ideas, angiogenesis generated a lot of attention in biomedical laboratories around the word, and each year reveals new knowledge about this process including explanation of a basic mechanism, as well as the discovery of new pharmaceutical compounds that positively or negatively regulate neovascularization. The past almost four decades of angiogenesis research definitely proved its importance for tumor growth, and showed that other diseases such as autoimmune are strongly affected by this process. In this paper the author presents all major endogenous regulators of angiogenesis with special attention to the therapy of cancer.