RAB3GAP1: A Promising Drug Target and Biomarker for G protein-Coupled Signaling in Cancer

Target Name: RAB3GAP1

NCBI ID: G22930

RAB3GAP1

RAB3GAP1: A Promising Drug Target and Biomarker for G protein-Coupled Signaling in Cancer

Introduction

G protein-coupled signaling (GCS) is a widely established signaling pathway that plays crucial roles in various cellular processes, including cell survival, proliferation, and angiogenesis. The RAB3GAP1 (Rab3 GTPase-activating protein catalytic subunit) gene is located on chromosome 18q21 and encodes a protein that functions as a critical regulator of GCS signaling. RAB3GAP1 has been implicated in the development and progression of numerous diseases, including cancer. As a result, targeting RAB3GAP1 has become an attractive research focus to explore new therapeutic approaches for cancer treatment.

RAB3GAP1: Structure and Function

The RAB3GAP1 gene encodes a protein with a molecular weight of approximately 42 kDa. The protein has a unique open-loop structure that is formed by the removal of the N-terminal region and the C-terminal region, which contain the catalytic subunit and a N-terminal domain, respectively. The catalytic subunit consists of two distinct domains: a N-terminal alpha-helical domain and a C-terminal beta-sheet domain. The N-terminal domain contains a critical GTP-binding site, which is essential for the catalytic activity of the protein.

The RAB3GAP1 protein functions as a GTPase-activating protein (GAP) in the GCS pathway. GAPs are a family of transmembrane proteins that play a crucial role in regulating various cellular processes, including the signaling pathways that regulate cell growth, differentiation, and survival. As a GAP, RAB3GAP1 activates the GTPase activity of other proteins, leading to the regulation of protein-protein interactions, DNA replication, and other cellular processes.

RAB3GAP1 has been shown to play a critical role in the regulation of cell proliferation and survival. Several studies have demonstrated that RAB3GAP1 is highly expressed in various tissues and cell types, including cancer cells. Additionally, overexpression of RAB3GAP1 has been shown to promote the growth and survival of cancer cells, suggesting that it may be a potential drug target for cancer treatment.

Drug Targeting Strategies

Several drug targeting strategies have been proposed to target RAB3GAP1, including inhibition of the N-terminal domain, the catalytic subunit, or the entire protein. One of the most promising strategies is the inhibition of RAB3GAP1 directly using small molecules or antibodies.

Inhibition of the N-terminal domain of RAB3GAP1 has been shown to be effective in inhibiting the protein's catalytic activity. Several studies have demonstrated that inhibitors of the N-terminal domain, such as point mutants or chemical compounds, can significantly reduce the activity of RAB3GAP1 . This suggests that targeting the N-terminal domain of RAB3GAP1 may be an effective strategy for cancer treatment.

Antibodies against RAB3GAP1 have also been shown to be effective in inhibiting the protein's catalytic activity. Several studies have demonstrated that antibodies against RAB3GAP1 can significantly reduce the activity of RAB3GAP1, both in cultured cells and in live animals. These results suggest that targeting RAB3GAP1 using antibodies may be an effective strategy for cancer treatment.

Biomarker Development

The development of biomarkers for cancer treatment is a critical step in the clinical trial process. RAB3GAP1 has been suggested as a potential biomarker for cancer treatment due to its involvement in the regulation of GCS signaling. Several studies have demonstrated that RAB3GAP1 levels are significantly elevated in various

Protein Name: RAB3 GTPase Activating Protein Catalytic Subunit 1

Functions: Catalytic subunit of the Rab3 GTPase-activating (Rab3GAP) complex composed of RAB3GAP1 and RAB3GAP2, which has GTPase-activating protein (GAP) activity towards various Rab3 subfamily members (RAB3A, RAB3B, RAB3C and RAB3D), RAB5A and RAB43, and guanine nucleotide exchange factor (GEF) activity towards RAB18 (PubMed:9030515, PubMed:10859313, PubMed:24891604). As part of the Rab3GAP complex, acts as a GAP for Rab3 proteins by converting active RAB3-GTP to the inactive form RAB3-GDP (PubMed:10859313). Rab3 proteins are involved in regulated exocytosis of neurotransmitters and hormones (PubMed:15696165). The Rab3GAP complex, acts as a GEF for RAB18 by promoting the conversion of inactive RAB18-GDP to the active form RAB18-GTP (PubMed:24891604). Required for recruiting and activating RAB18 at the endoplasmic reticulum (ER) membrane where it maintains proper ER structure (PubMed:24891604). Required for normal eye and brain development (PubMed:15696165, PubMed:23420520). May participate in neurodevelopmental processes such as proliferation, migration and differentiation before synapse formation, and non-synaptic vesicular release of neurotransmitters (PubMed:9030515, PubMed:9852129)

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•   general information;
•   protein structure and compound binding;
•   protein biological mechanisms;
•   its importance;
•   the target screening and validation;
•   expression level;
•   disease relevance;
•   drug resistance;
•   related combination drugs;
•   pharmacochemistry experiments;
•   related patent analysis;
•   advantages and risks of development, etc.
The report is helpful for project application, drug molecule design, research progress updates, publication of research papers, patent applications, etc. If you are interested to get a full version of this report, please feel free to contact us at BD@silexon.ai

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