Table 1.
Inhibitors of MAP4K4 used in different disease studies.
Name | Target | Effects in Disease/Syndrome | Ref |
---|---|---|---|
GNE-220 | MAP4K4 MAP4K5 (KHS1), MAP4K6 (MINK1), DMPK | Regulation of protrusion formation in human umbilical vein endothelial cells (HUVECs). Suppression of pathological angiogenesis in mice. |
(20) |
GNE-495 | MAP4K4 | Inhibition of migration and invasion in neuron protection medulloblastoma. Suppression of retinal angiogenesis. |
(6) (20) (49) (51) |
PF-06260933 | MAP4K4 | Reduction in glucose levels, amelioration of plaque development and/or plaque reduction in vivo.
Reduction of blood-brain barrier damage in mice, improved neurological recovery. |
(23) |
4-Hydroxy-2-pyridone | MAP4K4 | Enhancement of neurite outgrowth. | (52) |
6-(2-fluoropyridin-4-yl)pyrido[3,2-d]pyrimidin-4-amine, Compound 29 | MAP4K4 | Improved survival of motor neurons. Repression of stress-induced retrograde JNK signaling and protection from neurodegeneration. Pharmacodynamic effects in a human tumor xenograft model. |
(47–49) |
Kenpaullone | CDK1/cyclin B, GSK-3β, MAP4K4, KLF4, CDK2/cyclin A, CDK2/cyclin E, and CDK5/p25 | Inhibition of tumor cell growth. Maintenance of pancreatic β cell survival. Improved cardiomyocyte survival. |
(53, 54) |
Prostetin/12k | MAP4K4 | Protection of motor neurons from ER stress-induced apoptosis in amyotrophic lateral sclerosis (ALS). | (46) |
Bosutinib (Bosulif) | BCR-ABL, MAP4K4 | Protection against inflammation-induced endothelial barrier disruption. Prevention of vascular leakage and attenuation of murine alveolar protein leakage and pulmonary edema. |
(24) |
DMX-5804 | MAP4K4 MAP4K6 (MINK1), MAP4K7 (TNIK) | Prevention of oxidative-stress in cardiac myocyte cell death. Reduction of ischemia-reperfusion injury in mice. |
(54) |