WebRas, from "Rat sarcoma virus", is a family of related proteins that are expressed in all animal cell lineages and organs. All Ras protein family members belong to a class of protein called small GTPase, and are involved in transmitting signals within cells (cellular signal transduction).Ras is the prototypical member of the Ras superfamily of proteins, which … The binding of GTP to the nucleotide binding pocket of membrane anchored Rho GTPases leads to a conformational change that stimulates their interaction with various downstream effectors, including protein kinases and scaffold/adaptor-like proteins. The activity of most Rho GTPases is terminated by the … See more Rho GTPases are a family of highly conserved GTPases that are encoded by 20 genes in humans and regulate a range of cellular functions, including vesicular transport, gene expression, neuronal development, and … See more The best characterized Rho GTPase effectors are the highly conserved p21-activated kinases (PAKs), which are found in almost all eukaryotes except plants (Hofmann et al., 2004). In humans, the PAKs comprise a … See more In humans, myotonic dystrophy kinase-related Cdc42-binding kinases (MRCKs) form a family of three serine/threonine protein kinases that are evolutionarily related to ROCKs and play a key role in the regulation of … See more The Rho GTPase effectors ROCK1 and ROCK2 are AGC-family serine/threonine kinases that are involved in a diverse range of cellular processes, including cell motility, cell survival … See more
SEC Filing - Turning Point Therapeutics, Inc.
WebOct 7, 2024 · Introduction Athena Countouriotis, M.D.President & Chief Executive Officer Lead Candidate: Repotrectinib with 2 Breakthrough Therapy Designations¹ NSCLC Other Solid Tumors Robust Pipeline with Four Clinical Stage Drug Candidates Developing potential best-in-class drug candidates Inhibitor of JAK2, SRC and FAK Combination … WebMay 20, 2012 · Conclusions: We conclude that syndecan-1 is a novel target of the oncomiR miR-10b. Rho-GTPase dependent modulation of cytoskeletal function and downregulation of E-cadherin expression are identified as relevant effectors of the miR-10b-syndecan-1 axis, which emerges as a promising target for the development of new therapeutic … twilight forks self guided tour
Covalent inhibitors: a rational approach to drug discovery
WebAtypically for GTPase family members, dynamin is large (∼96 kDa) and has a modular domain structure (Fig. 1) consisting of an N-terminal GTPase domain, a middle domain … WebSep 8, 2024 · HPK1 is an important immuno-oncology drug target that may induce superior anti-tumor immunity through the multiple roles HPK1 may play at multiple steps of the cancer immunity cycle. ... forming an indispensable supramolecular complex of SLP-76, SKAP55 and Rap1 GTPase that translocate to the plasma membrane to activate LFA-1 … WebMar 16, 2024 · 1. Introduction. Small GTPases are a large family of hydrolases that bind and hydrolyze GTP to GDP in order to regulate many cellular activities (e.g., cell … twilight forks background