Delving into the Latest Updates on Pelitrexol with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Pelitrexol (USAN/INN)

Target

GART

Action

inhibitors

Mechanism

GART inhibitors(GAR transformylase inhibitors)

Therapeutic Areas

NeoplasmsDigestive System DisordersRespiratory Diseases

Active Indication-

Inactive Indication

Metastatic Colorectal Carcinomametastatic non-small cell lung cancer

Originator Organization

Agouron Pharmaceuticals LLC

Active Organization-

Inactive Organization

Pfizer Inc.

License Organization-

Drug Highest PhaseDiscontinuedPhase 2

First Approval Date-

Regulation-

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Structure/Sequence

Molecular FormulaC20H25N5O6S

InChIKeyQXOPTIPQEVJERB-JQWIXIFHSA-N

CAS Registry446022-33-9

Centromere protein I (CENPI) is an important member of centromeric proteins family, which is crucial to chromosome alignment and segregation. Nevertheless, the interrelation between CENPI expression and tumor progression is in the shadows. In this reserch, we carried out a panoramic bioinformatic analysis about CENPI with TCGA, Timer 2.0, Oncomine, GEPIA, Cbioportal, LinkedOmics and CancerSEA databases. Besides, our bioinformatic results have been further confirmed through in vitro experiments, including Real-Time quantitative PCR (RT-qPCR), immunofluorescence (IF), immunohistochemistry (IHC), western blotting (WB), cell proliferation assays, EdU, cell cycle and apoptosis test. Our results suggested that CENPI was increased in most of the cancers, and may serve as a potential biomarker. What's more, the knock down of CENPI inhibited the expression of CDK2 in lung adenocarcinoma (LUAD), and resulted in the arrest of G0/G1 phase and apoptosis. Besides, CENPI was related to immune cells infiltration and drug sensitivity in pan-cancer, and can act as a potential treatment target to cure cancer patients.

01 Dec 2022·Cancer Cell International

PTH2R is related to cell proliferation and migration in ovarian cancer: a multi-omics analysis of bioinformatics and experiments

Article

Author: Tong, Lu ; Yanjun, Qu ; Xiaowei, Wang ; Lili, Fan

AbstractBackgroundOvarian cancer is a common gynecological disease and seriously endangers women's health. Currently, there is still a lack of effective molecular markers for the diagnosis and treatment of ovarian cancer. The present study aimed to investigate the molecular markers associated with ovarian cancer.MethodsThe molecular and gene related to ovarian cancer were extracted from GEO database and TCGA database by bioinformatics, and the related genes and functions were further analyzed. The results were verified by qPCR, WB, CCK-8 and Transwell experiments.ResultsData analysis showed that PTH2R gene was highly expressed in tumors, and 51 HUB genes were obtained. Finally, experimental verification showed that PTH2R gene was highly expressed in ovarian cancer, and PTH2R gene was involved in the proliferation, invasion and metastasis of ovarian cancer cells.ConclusionsAfter experimental verification, we found that knocking down the expression of PTH2R can inhibit the proliferation, invasion and migration of tumor cells.PTH2R is expected to become a new molecular marker for ovarian cancer.

01 Jun 2017·Cell ReportsQ1 · BIOLOGY

Purine Nucleotide Availability Regulates mTORC1 Activity through the Rheb GTPase

Q1 · BIOLOGY

ArticleOA

Author: Jin, Guixian ; Giannakou, Andreas ; Unsal-Kacmaz, Keziban ; Myers, Jeremy ; Shan, Qin ; Abraham, Robert T ; Wang, Fang ; Emmanuel, Natasha ; Huser, Nanni ; Ragunathan, Shoba

Pharmacologic agents that interfere with nucleotide metabolism constitute an important class of anticancer agents. Recent studies have demonstrated that mTOR complex 1 (mTORC1) inhibitors suppress de novo biosynthesis of pyrimidine and purine nucleotides. Here, we demonstrate that mTORC1 itself is suppressed by drugs that reduce intracellular purine nucleotide pools. Cellular treatment with AG2037, an inhibitor of the purine biosynthetic enzyme GARFT, profoundly inhibits mTORC1 activity via a reduction in the level of GTP-bound Rheb, an obligate upstream activator of mTORC1, because of a reduction in intracellular guanine nucleotides. AG2037 treatment provokes both mTORC1 inhibition and robust tumor growth suppression in mice bearing non-small-cell lung cancer (NSCLC) xenografts. These results indicate that alterations in purine nucleotide availability affect mTORC1 activity and suggest that inhibition of mTORC1 contributes to the therapeutic effects of purine biosynthesis inhibitors.

100 Deals associated with Pelitrexol

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External Link

KEGG	Wiki	ATC	Drug Bank
D05400	-	-	DB12757

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
metastatic non-small cell lung cancer	Phase 2	United States	Pfizer Inc.	01 Sep 2004
Metastatic Colorectal Carcinoma	Phase 2	United States	Pfizer Inc.	01 Dec 2003