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Receptors for Targeting Gastrointestinal Tract Cancer

  • Tejal Pant
  • Nikita Aware
  • Padma V. Devarajan
  • Ratnesh JainEmail author
  • Prajakta DandekarEmail author
Chapter
Part of the AAPS Advances in the Pharmaceutical Sciences Series book series (AAPS, volume 39)

Abstract

Cancers of the gastrointestinal tract (GIT) are among the most prevalent and fatal cancers. Historically, surgical resection was the only effective treatment of operable GIT tumors. However, more than half of these patients present locally advanced, recurrent, or metastatic disease, necessitating development of alternate strategies for possible therapy. Cellular receptors are instrumental in controlling the basic traits of a cell. Binding of specific ligands to these receptors results in changes in gene expression and increase in cell metabolism, cell growth, or cell death. The therapeutic prospects of ligands for somatostatin receptors (SSTRs), c-Kit, and peroxisome proliferator-activated receptors (PPARs) along with receptor-mediated strategies have been discussed in this chapter. Ligands for these receptors include peptides, small molecules, and oligonucleotides that can be delivered using nanoparticulate delivery systems tailored for specific application. Some important drug candidates undergoing clinical trials have also been mentioned to convey the potential of these receptors as targets for GIT cancer therapy.

Keywords

Gastrointestinal tract Cancer Receptor Somatostatin c-Kit PPAR 

Abbreviations

CML

Chronic myeloid leukemia

CXC

C-X-C motif chemokine

DBD

DNA-binding domain

DRIP

vitamin D3 receptor-interacting protein

EGFR

Epidermal growth factor receptor

GEP-NET

Gastroenteropancreatic neuroendocrine tumors

GIST

Gastrointestinal stromal tumors

GIT

Gastrointestinal tract

LBD

Ligand-binding domain

MAPK

Mitogen-activated protein kinase

mTOR

Mammalian target of rapamycin

NCoR

Nuclear receptor corepressor

NF-κB

Nuclear factor kappa light chain

NPs

Nanoparticles

PDGFR

Platelet-derived growth factor receptor

PGC-1

PPARγ coactivator-1

PIP3

Phosphatidylinositol 3,4,5 triphosphate

PL

Phospholipase

PPAR

Peroxisome proliferator-activated receptors

PRI

Peptide receptor imaging

PRRT

Peptide receptor radionuclide therapy

PTP

Phosphotyrosine phosphatases

PTX

Pertussis toxin

QDs

Quantum dots

RTK

Receptor tyrosine kinase

RXR

Retinoid X receptor

SCF

Stem cell factor

SFK

Src family of tyrosine kinases

SH2

Src homology 2

SHP

Small heterodimer partner

SRIF

Somatotropin release-inhibiting factor

SS

Somatostatin

SSTR

Somatostatin receptors

TLR

Toll-like receptors

TMD

Transmembrane domains

TRAP

Thyroid hormone receptor-associated protein

TZD

Thiazolidinedione

USFDA

The food and drug administration

VEGF

Vascular endothelial growth factor

VEGFR

Vascular endothelial growth factor receptor

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Copyright information

© American Association of Pharmaceutical Scientists 2019

Authors and Affiliations

  1. 1.Department of Chemical EngineeringInstitute of Chemical TechnologyMumbaiIndia
  2. 2.Department of Pharmaceutical Sciences & TechnologyInstitute of Chemical TechnologyMumbaiIndia
  3. 3.Department of Pharmaceutical SciencesInsitute of Chemical Technology, Deemed University, Elite Status and Centre of Excellence, Government of MaharashtraMumbaiIndia

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