MAP kinases (CMGC kinases) may be divided into three major families: ERK, JNK and p38 MAP kinases.

ERK may be activated by phosphorylation by the dual specificity mitogen-activated kinase kinases, MAP2K1 (Q02750, also known as MEK1) and MAP2K2 (P36507, also known as MEK2). The inhibitors PD98059 [1,3] and U0126 [4-5] act to inhibit these enzymes [2], and are used to inhibit ERK1 and ERK2.

JNK may be activated by phosphorylation by the dual specificity mitogen-activated kinase kinases, MAP2K4 (P45985, also known as JNKK1) and MAP2K7 (O14733, also known as JNKK2) .

p38 may be activated by phosphorylation by the dual specificity mitogen-activated kinase kinases, MAP2K3 (P46734, also known as MEK3) and MAP2K6 (P52564, also known as SAPKK3).

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1. Alessi DR, Cuenda A, Cohen P, Dudley DT, Saltiel AR. (1995) PD 098059 is a specific inhibitor of the activation of mitogen-activated protein kinase kinase in vitro and in vivo. J Biol Chem, 270 (46): 27489-94. [PMID:7499206]

2. Davies SP, Reddy H, Caivano M, Cohen P. (2000) Specificity and mechanism of action of some commonly used protein kinase inhibitors. Biochem J, 351 (Pt 1): 95-105. [PMID:10998351]

3. Dudley DT, Pang L, Decker SJ, Bridges AJ, Saltiel AR. (1995) A synthetic inhibitor of the mitogen-activated protein kinase cascade. Proc Natl Acad Sci USA, 92 (17): 7686-9. [PMID:7644477]

4. Duncia JV, Santella JB, Higley CA, Pitts WJ, Wityak J, Frietze WE, Rankin FW, Sun JH, Earl RA, Tabaka AC et al.. (1998) MEK inhibitors: the chemistry and biological activity of U0126, its analogs, and cyclization products. Bioorg Med Chem Lett, 8 (20): 2839-44. [PMID:9873633]

5. Favata MF, Horiuchi KY, Manos EJ, Daulerio AJ, Stradley DA, Feeser WS, Van Dyk DE, Pitts WJ, Earl RA, Hobbs F et al.. (1998) Identification of a novel inhibitor of mitogen-activated protein kinase kinase. J Biol Chem, 273 (29): 18623-32. [PMID:9660836]