Small molecule modulators

Brodsky JL, Chiosis G (2006) Hsp70 molecular chaperones emerging roles in human disease and identification of small molecule modulators. Curr Top Med Chem 6 1215-1225... 

Chapman RL, Stanley TB, Hazen R, Garvey EP. Small molecule modulators of HIV Rev/Rev response element interaction identified by random screening. Antiviral Res 2002 54 149-62. 

To date, no small-molecule modulators have been reported for either of these channels. 

No small-molecule modulators of TRPM1, TRPM3, TRPM4, TRPM5, TRPM6, or TRPM7 have been described. 

No small-molecule modulators of the remaining TRPC, TRPP, or TRPML ion channel families have yet been described. 

Several small molecule modulators (SMM) of p300 and PCAF have been developed (Varier et al, 2004). Recently, the first naturally occurring HAT inhibitor anacardic acid was isolated from cashew nut shell liquid, which inhibits the HAT activity of both p300 and PCAF very effectively (Balasubramanyam et al, 2003). By using anacardic acid as a synthon, an amide derivative of anacardic acid, CTPB, has been synthesized, which is the only known small molecule activator of any histone acetyltransferase, in this case, p300. However, cells are impermeable or... 

Balasubramanyam K, Swaminathan V, Ranganathan A, Kundu TK (2003) Small molecule modulators of histone acetyltransferase p300. J Biol Chem 278(21) 19134-19140 Barlow AL, van Drunen CM, Johnson CA, Tweedie S, Bird A, Turner BM (2001) dSIR2 and dHDAC6 two novel, inhibitor-resistant deacetylases in Drosophila melanogaster. Exp Cell Res 265(1) 90-103... 

Balsubramanyam, K, Swaminathan, V., Ranganathan, A. and Kundu, T.K (2003) Small molecule modulators of histone acetyltransferase p300. The Journal of Biological Chemistry, 278, 19134—19140. 

In chemogenomics and drug discovery, the most challenging task is to find small molecule modulators of protein function that specifically modulate the protein function of interest. Combinatorial chemistry has emerged as a powerful tool to address this problem by generation of large compound... 

Compound libraries as sources for small molecule modulators of protein function... 

Small molecules modulating microtubule assembly have played major roles as tools in microtubule research, in a manner closely related to their chemotherapeutic interest [1], Tubulin was first purified in the last century as the colchicine-binding protein proposed to be the subunit of cellular microtubules [2], More recently, a colchicine derivative was employed to help crystallization and determine the structure of tubulin by X-ray diffraction [3], The colchicine, vinblastine [4] and paclitaxel [5] sites are main drug binding sites of tubulin, to which many other substances bind. The discovery of microtubule stabilization by paclitaxel [6] prompted its clinical development [7] and a burst of research on new MSAs, as well as the generalized use of paclitaxel or docetaxel as convenient reagents to assemble (see Fig. 1), stabilize or detect microtubules in the laboratory. One example is the development... 

---