TM7SF2 Inhibitors
Chemical inhibitors of TM7SF2 can exert their effects through the modulation of the cholesterol biosynthesis pathway. Simvastatin, pravastatin, lovastatin, atorvastatin, rosuvastatin, pitavastatin, fluvastatin, cerivastatin, and mevastatin are all inhibitors of the enzyme HMG-CoA reductase, which is a crucial enzyme upstream of TM7SF2 in the pathway. The inhibition of HMG-CoA reductase by these chemicals leads to a reduction in the production of mevalonate and other essential intermediates that are substrates for subsequent enzymes in the cholesterol synthesis pathway, including TM7SF2. By decreasing the availability of these substrates, these chemicals indirectly decrease the functional activity of TM7SF2. The enzyme is left with insufficient substrates to carry out the synthesis of cholesterol, effectively leading to a decrease in its functional activity within the pathway. Without the necessary substrates, the activity of TM7SF2 is reduced, which is a direct result of the action of these HMG-CoA reductase inhibitors.
In contrast, chemical inhibitors such as lapaquistat, zaragozic acid, and squalestatin 1 target enzymes downstream of TM7SF2. Lapaquistat and zaragozic acid specifically inhibit squalene synthase, whereas squalestatin 1 inhibits the synthesis of squalene. The inhibition of these downstream enzymes can lead to a build-up of intermediates such as farnesyl pyrophosphate. This accumulation of intermediates can lead to a feedback inhibition mechanism, which can decrease the activity of upstream enzymes like TM7SF2. These chemicals do not directly inhibit TM7SF2 but instead alter the concentration of substrates and products in the pathway that can influence the activity of TM7SF2. The resultant increase in intermediates that precede the step catalyzed by squalene synthase in the cholesterol biosynthesis pathway can lead to a decrease in the activity of TM7SF2 due to the regulatory mechanisms within the pathway that maintain homeostasis of cholesterol synthesis.
SEE ALSO...
| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Simvastatin | 79902-63-9 | sc-200829 sc-200829A sc-200829B sc-200829C | 50 mg 250 mg 1 g 5 g | $31.00 $89.00 $135.00 $443.00 | 13 | |
Simvastatin inhibits HMG-CoA reductase, which is upstream in the cholesterol biosynthesis pathway. TM7SF2 is involved in cholesterol biosynthesis; by inhibiting the upstream enzyme, simvastatin reduces the availability of precursors necessary for TM7SF2 to function, leading to a functional inhibition of TM7SF2's activity. | ||||||
Pravastatin, Sodium Salt | 81131-70-6 | sc-203218 sc-203218A sc-203218B | 25 mg 100 mg 1 g | $69.00 $162.00 $787.00 | 2 | |
Pravastatin, similar to simvastatin, inhibits HMG-CoA reductase and by doing so decreases the substrate availability for cholesterol biosynthesis. This action reduces the functional activity of TM7SF2 as it plays a role in this pathway, leading to its inhibition due to a lack of substrates required for its enzymatic activity. | ||||||
Lovastatin | 75330-75-5 | sc-200850 sc-200850A sc-200850B | 5 mg 25 mg 100 mg | $29.00 $90.00 $339.00 | 12 | |
Lovastatin is another HMG-CoA reductase inhibitor that limits the availability of essential substrates for cholesterol synthesis. The inhibition of this upstream enzyme by lovastatin causes a consequential decrease in TM7SF2 activity by starving it of the substrates it requires to synthesize cholesterol. | ||||||
Atorvastatin | 134523-00-5 | sc-337542A sc-337542 | 50 mg 100 mg | $257.00 $505.00 | 9 | |
Atorvastatin acts by inhibiting HMG-CoA reductase, leading to a reduction in cholesterol synthesis precursors. Since TM7SF2 is a key protein in cholesterol biosynthesis, atorvastatin indirectly inhibits TM7SF2 by reducing the pool of substrates it needs for its enzymatic action. | ||||||
Rosuvastatin | 287714-41-4 | sc-481834 | 10 mg | $145.00 | 8 | |
Rosuvastatin targets and inhibits HMG-CoA reductase. The inhibition of this critical enzyme in the cholesterol biosynthesis pathway by rosuvastatin leads to a decrease in the substrates required by TM7SF2, thereby functionally inhibiting the protein's activity in the pathway. | ||||||
Fluvastatin | 93957-54-1 | sc-279169 | 50 mg | $250.00 | ||
Fluvastatin selectively inhibits HMG-CoA reductase, which is a precursor enzyme necessary for the pathway in which TM7SF2 operates. The inhibition of substrate production upstream by fluvastatin leads to a functional inhibition of TM7SF2 as it reduces the compound's availability that TM7SF2 requires for its activity. | ||||||
Mevastatin (Compactin) | 73573-88-3 | sc-200853 sc-200853A | 10 mg 50 mg | $77.00 $179.00 | 18 | |
Mevastatin is a compactin that inhibits HMG-CoA reductase. The inhibition of this crucial enzyme in cholesterol biosynthesis by mevastatin reduces the availability of substrates for TM7SF2, thus functionally inhibiting the protein due to insufficient substrate availability for its enzymatic action. | ||||||