Mitogen-activated protein kinase (MAPK)

Mitogen-activated protein kinase (MAPK) refers to a class of conserved serine/threonine kinase that being ubiquitously presented in eukaryotes. MAPK cascade pathway (MAPKKK-MAPKK-MAPK) is capable of transducing environmental signals through sequential phosphorylation, participating in regulating plant growth and development as well as a variety of biotic and abiotic stress signal transduction. MAPKs activation pathway plays a crucial role in the signal transduction process in eukaryotic cells. In 1982, during the study of the platelet-derived growth factor and epidermal growth factor, cooper found that a kind of intracellular protein (with relative molecular mass of 42 × 103) was subject to phosphorylation in its tyrosine residues. He then (in 1988) also found this protein in PMA-stimulated cells through two-dimensional electrophoresis.

At the same time, Ray had also successfully isolated a protein kinase of a molecular weight of 42X103 with its threonine and tyrosine residues being phosphorylated from the 3T3-L1 cells and named it MAPKs. Rossomando (1989) have clarified that this kind of protein that subjects to insulin-stimulated tyrosine / threonine residue phosphorylation is the same protein as the protein that subjects to tyrosine residue phosphorylation due to the stimulation of other growth factors and PMA; threonine / tyrosine residues double phosphorylation is a necessary condition for activation of this protein. Boulton (in 1990) had first cloned the cDNA encoding MAPKs; Crews (In 1993) had successfully identified the upstream kinase (MKKKs and MKKs) of MAPKs in mammalian cells by biochemical and molecular cloning techniques and defined a conservative three-kinase activation mode.

The composition of the MAPKs activation pathway
MAPKs activation pathway can be activated by a variety of factors including growth factors, cytokines, radiation, neurotransmitters, hormones and cell stress, etc. MAPKs activation pathway includes three sequentially activated protein kinase: MKKKs → MKKs → MAPKs. It has been found from mammalian cells of at least 14 kinds of MKKKs, 7 kinds of MKKs and 12 kinds of MAPKs.

(1) MKKKs: MKKKs is a kind of serine / threonine protein kinase. Specific MKKKs can be either activated through phosphorylation mediated by its MKKKs kinase (MKKKKs) or activated through the interaction with Ras or the small G protein in Rho family.
(2) MKKs: Gartner et al have confirmed, MKKs can recognize MAPKs to activate the threonine X tyrosine domain inside the ring, causing phosphorylation of the threonine and tyrosine residues and further being activated. Therefore, MKKs is a kind of protein kinase of dual specificity.
(3) MAPKs: MAPKs are a class of protein kinases that widely presented in the cytoplasm and are able to cause phosphorylation of serine/threonine in the inner substrate protein molecule. The kinase property of MAPKs is mediated by the proline, i.e., only being able to phosphorylate the proline-containing substrate protein in P1 region. The major targeting substrate of MAPKs is transcription factor, also includes a number of protein kinases, phospholipases and cytoskeletal associated proteins. Dual phosphorylation of serine and tyrosine residues is a necessary condition for the activation of MAPKs. Different MKKs are able to recognize the spatial structure of the threonine X tyrosine domain in specific MAPKs, instead of just recognizing the linear sequence in the activation domain.

Click on the specific product, view the latest prices of the products, information, serving information
Structure Chemical Name CAS MF
SB 203580 SB 203580 152121-47-6 C21H16FN3OS
Doramapimod Doramapimod 285983-48-4 C31H37N5O3
Trametinib Trametinib 871700-17-3 C26H23FIN5O4
PD 0325901 PD 0325901 391210-10-9 C16H14F3IN2O4
PD 98059 PD 98059 167869-21-8 C16H13NO3
N-[3-[(5-Chloro-1H-pyrrolo[2,3-b]pyridin-3-yl)carbonyl]-2,4-difluorophenyl]-1-propanesulfonamide N-[3-[(5-Chloro-1H-pyrrolo[2,3-b]pyridin-3-yl)carbonyl]-2,4-difluorophenyl]-1-propanesulfonamide 918505-84-7 C17H14ClF2N3O3S
VX-745 VX-745 209410-46-8 C19H9Cl2F2N3OS
Dabrafenib Dabrafenib 1195765-45-7 C23H20F3N5O2S2
PD184352 PD184352 212631-79-3 C17H14ClF2IN2O2
ZM 336372 ZM 336372 208260-29-1 C23H23N3O3
RAF265(CHIR-265) RAF265(CHIR-265) 927880-90-8 C24H16F6N6O
5-[2-[4-[2-(Dimethylamino)ethoxy]phenyl]-5-(4-pyridinyl)-1H-imidazol-4-yl]-2,3-dihydro-1H-inden-1-one oxime 5-[2-[4-[2-(Dimethylamino)ethoxy]phenyl]-5-(4-pyridinyl)-1H-imidazol-4-yl]-2,3-dihydro-1H-inden-1-one oxime 405554-55-4 C27H27N5O2
GW5074 GW5074 220904-83-6 C15H8Br2INO2
BIX 02188 BIX 02188 1094614-84-2 C25H24N4O2
PH 797804 PH 797804 586379-66-0 C22H19BrF2N2O3
SCH772984 SCH772984 942183-80-4 C33H33N9O2
PD318088 PD318088 391210-00-7 C16H13BrF3IN2O4
VX 702 VX 702 745833-23-2 C19H12F4N4O2
CEP-32496 (free base) CEP-32496 (free base) 1188910-76-0 C24H22F3N5O5
(R)-2-((R)-2-acetamido-3-(4-hydroxyphenyl)propanamido)-N-((R)-1-amino-1-oxo-3-phenylpropan-2-yl)-5-guanidinopentanamide (R)-2-((R)-2-acetamido-3-(4-hydroxyphenyl)propanamido)-N-((R)-1-amino-1-oxo-3-phenylpropan-2-yl)-5-guanidinopentanamide 1809784-29-9 C26H35N7O5
AZ 628 AZ 628 878739-06-1 C27H25N5O2
Raf265 derivative Raf265 derivative 1942849-27-5 C23H14F6N6O
Losmapimod (GW856553X) Losmapimod (GW856553X) 585543-15-3 C22H26FN3O2
2-[[2-Ethoxy-4-(4-hydroxy-1-piperidinyl)phenyl]amino]-5,11-dihydro-5,11-dimethyl-6H-pyrimido[4,5-b][1,4]benzodiazepin-6-one 2-[[2-Ethoxy-4-(4-hydroxy-1-piperidinyl)phenyl]amino]-5,11-dihydro-5,11-dimethyl-6H-pyrimido[4,5-b][1,4]benzodiazepin-6-one 1234480-50-2 C26H30N6O3
SL 327 SL 327 305350-87-2 C16H12F3N3S
TAK-733 TAK-733 1035555-63-5 C17H15F2IN4O4
Encorafenib (LGX818) Encorafenib (LGX818) 1269440-17-6 C22H27ClFN7O4S
N-(3-Cyano-4,5,6,7-tetrahydrobenzo[b]thienyl-2-yl)-1-naphthalenecarboxamide N-(3-Cyano-4,5,6,7-tetrahydrobenzo[b]thienyl-2-yl)-1-naphthalenecarboxamide 312917-14-9 C20H16N2OS
BIX 02189 BIX 02189 1094614-85-3 C27H28N4O2
RDEA119 RDEA119 923032-37-5 C19H20F3IN2O5S
Skepinone-L Skepinone-L 1221485-83-1 C24H21F2NO4
TAK-632 TAK-632 1228591-30-7 C27H18F4N4O3S
5-(2-Phenyl-pyrazolo[1,5-a]pyridin-3-yl)-1H-pyrazolo[3,4-c]pyridazin-3-ylamine 5-(2-Phenyl-pyrazolo[1,5-a]pyridin-3-yl)-1H-pyrazolo[3,4-c]pyridazin-3-ylamine 865362-74-9 C18H13N7
U0126-EtOH U0126-EtOH 1173097-76-1 C20H22N6OS2
LY2228820 LY2228820 862507-23-1 C26H37FN6O6S2
Binimetinib Binimetinib 606143-89-9 C17H15BrF2N4O3
JNK-IN-8 JNK-IN-8 1410880-22-6 C29H29N7O2
Email:[email protected] [email protected]
Copyright © 2024 Mywellwork.com All rights reserved.