Madhusoodanan Mottamal

TL;DR: Four major structural classes of HDAC inhibitors that are in clinical trials and different computer modeling tools available for their structural modifications are summarized as a guide to discover additional HDAC inhibitor-based therapies with greater therapeutic utility.

TL;DR: A series of novel pyridine-bridged analogues of combretastatin-A4 (CA-4) were designed and synthesized and binding data are consistent with the observed biological activities in antiproliferation and suppression of angiogenesis but are not predictive of their antitubulin polymerization activities.

TL;DR: The design and synthesis of 63 new thiazole derivatives by further structural modifications in search of more potent fascin inhibitors showed strong antiangiogenesis activity, blocking new blood vessel formation in a chicken embryo membrane assay.

TL;DR: Mechanistic studies analyzing the actin cytoskeleton by microscopy demonstrate that compound 5k substantially reduced cellular f-actin, and prevented localization of fascin to actin-rich membrane protrusions, suggesting that the anti-migration activity may result from impaired actin structures in protrusion that are necessary to drive migration.

TL;DR: The binding details of ZB716 to the estrogen receptor alpha (ERα) are examined by computer modeling to reveal its interactions with the ligand binding domain as a steroidal molecule and it is found that ZB 716 modulates ERα-coregulator interactions in nearly identical manner to fulvestrant.