Last update 01 Nov 2024

FOLR2

Last update 01 Nov 2024

Basic Info

Synonyms

叶酸受体2, FBP, Folate receptor 2

+ [8]

Introduction

Binds to folate and reduced folic acid derivatives and mediates delivery of 5-methyltetrahydrofolate and folate analogs into the interior of cells. Has high affinity for folate and folic acid analogs at neutral pH. Exposure to slightly acidic pH after receptor endocytosis triggers a conformation change that strongly reduces its affinity for folates and mediates their release.

Drugs associated with FOLR2

Pafolacianine

Target

FOLR1 x FOLR2

Mechanism

FOLR1 agonists [+2]

Active Org.

University of California, Irvine [+1]

Originator Org.

On Target Laboratories LLC

Active Indication

Lung Cancer [+5]

Inactive Indication

Endometrial Carcinoma [+5]

Drug Highest PhaseApproved

First Approval Ctry. / Loc.

First Approval Date29 Nov 2021

Vintafolide

Target

FOLR1 x FOLR2 x Tubulin

Mechanism

FOLR1 agonists [+2]

Active Org.

Merck Sharp & Dohme Corp. [+1]

Originator Org.

Novartis Pharma AG

Active Indication

Non-Small Cell Lung Cancer

Inactive Indication

Adenocarcinoma of Lung [+7]

Drug Highest PhasePhase 2

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

EC-0305

Target

FOLR1 x FOLR2

Mechanism

FOLR1 agonists [+1]

Active Org.-

Originator Org.

Novartis Pharma AG

Active Indication-

Inactive Indication

Neoplasms

Drug Highest PhasePending

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

Clinical Trials associated with FOLR2

NCT06511037 / Not yet recruitingEarly Phase 1IIT

A Pilot Study of Pafolacianine Injection for Intraoperative Imaging of Gastrointestinal Cancer Peritoneal Carcinomatosis

This is a pilot, single-arm, open label study to evaluate the ability of CYTALUX™ (pafolacianine) to help identify cancerous lesions in subjects with gastrointestinal cancers and peritoneal carcinomatosis during cytoreductive surgery.

Start Date31 Oct 2024

Sponsor / Collaborator

University of California, Irvine

[+1]

NCT06235125 / RecruitingPhase 1IIT

A Pilot Study of Near-Infrared Imaging Using the Novel Imaging Agent Cytalux for Adolescent Patients With Metastatic Osteosarcoma Undergoing Pulmonary Metastasectomy

Pediatric subjects aged 6-17 with biopsy confirmed cancer and imaging findings suspicious for pulmonary metastatic disease scheduled to undergo pulmonary metastasectomy via and open or minimally invasive approach.

Start Date08 Apr 2024

Sponsor / Collaborator

Ann & Robert H. Lurie Children's Hospital of Chicago

[+1]

NCT04941378 / WithdrawnPhase 1IIT

A Pilot, Single Dose, Open-Label Study of OTL38 Injection (OTL38) for Intra-Operative Imaging of Folate Receptor Positive Ovarian Cancer

The primary objective of the study is to compare the performance of different camera imaging systems in assessing the positive predictive values and sensitivity of OTL38 to detect folate positive ovarian cancer cancers using the gold standard of pathologic review.

Start Date28 May 2022

Sponsor / Collaborator

Abramson Cancer Center

100 Clinical Results associated with FOLR2

100 Translational Medicine associated with FOLR2

0 Patents (Medical) associated with FOLR2

274

Literatures (Medical) associated with FOLR2

01 Oct 2024·Biomedicine & Pharmacotherapy

Targeted counteracting of overactive macrophages by melittin stable-loaded solid lipid nanoparticles alleviates cytokine storm and acute inflammatory injury

Article

Author: Yang, Yang ; Shi, Sanyuan ; Peng, Jinliang ; Zhang, Yunxuan ; He, Miao ; Zheng, Yuan ; Xu, Yuhong ; Ye, Ningshuang ; Wei, Xiaohui ; Kesse, Samuel ; Nie, Ping

The continuous activation of macrophages play a critical role in the pathogenesis of cytokine storm (CS). Considering that CS results from the participation of multiple cytokines, the therapeutic effect of a single cytokine or its receptor-targeted blockade therapy remains uncertain. Melittin, which can systematically suppress the overexpression of proinflammatory mediators via inhibiting the mitogen-activated protein kinase and nuclear factor kappa-B pathways in activated macrophages, shows great potential in alleviating CS and acute inflammatory injury (AII). However, its clinical application is limited by its hemolytic activity, non-specific cytotoxicity and lack of targeting. In this study, a folic acid-modified and melittin stable-loaded solid lipid nanoparticle (Fa-MpG@LNP) with a core-shell structure was developed for CS control via targeted inhibition of the overproduction of proinflammatory mediators in activated macrophages with specific expression of folate receptor-β. The resultant Fa-MpG@LNP showed ideal physicochemical properties and stability, low hemolytic activity and non-specific cytotoxicity, and it can specifically bind to lipopolysaccharide (LPS)-stimulated macrophages and effectively reduce the elevated levels of proinflammatory mediators. After intravenous administration, the Fa-MpG@LNP accumulated at inflamed tissue and significantly downregulate the overproduction of proinflammatory cytokines in tissue-infiltrated macrophages, resulting in a significant decrease of cytokine concentration in inflamed tissue and serum in LPS-induced acute pneumonia mice, and finally alleviate AII with undetectable toxic side effects. These results indicate the clinical application potential of Fa-MpG@LNP in alleviating CS and its related symptoms.

01 Oct 2024·The Ocular Surface

Changes in conjunctival mononuclear phagocytes and suppressive activity of regulatory macrophages in desiccation induced dry eye

Article

Author: Zuo, Zhen ; Alam, Jehan ; Pflugfelder, Stephen C ; Yaman, Ebru ; de Paiva, Cintia S ; Pflugfelder, Stephen C. ; de Paiva, Cintia S. ; Villalba Silva, Gerda Cristal ; Li, De-Quan

PURPOSETo evaluate the effects of dry eye on conjunctival immune cell number and transcriptional profiles with attention to mononuclear phagocytes.METHODSExpression profiling was performed by single-cell RNA sequencing on sorted conjunctival immune cells from non-stressed and C57BL/6 mice subjected to desiccating stress (DS). Monocle 3 modeled cell trajectory, scATAC-seq assessed chromatin accessibility and IPA identified canonical pathways. Inflammation and goblet cells were measured after depletion of MRC1⁺ MΦs with mannosylated clodronate liposomes.RESULTSMononuclear phagocytes (monocytes, MΦs, DCs) comprised 72 % of immune cells and showed the greatest changes with DS. Distinct DS induced gene expression patterns were seen in phagocytes classified by expression of Ccr2 and [Timd4, Lyve1, Folr2 (TLR)]. Expression of phagocytosis/efferocytosis genes increased in TLF⁺CCR2^- MΦs. Monocytes showed the highest expression of Ace, Cx3cr1, Vegfa, Ifngr1,2, and Stat1 and TLF^-CCR2⁺ cells expressed higher levels of inflammatory mediators (Il1a, Il1b, Il1rn, Nfkb1, Ccl5, MHCII, Cd80, Cxcl10, Icam1). A trajectory from monocyte precursors branched to terminate in regulatory MΦs or in mDCs via transitional MΦ and cDC clusters. Activated pathways in TLF⁺ cells include phagocytosis, PPAR/RXRα activation, IL-10 signaling, alternate MΦ activation, while inflammatory pathways were suppressed. Depletion of MRC1⁺ MΦs increased IL-17 and IFN-γ expression and cytokine-expressing T cells, reduced IL-10 and worsened goblet loss.CONCLUSIONSDryness stimulates distinct gene expression patterns in conjunctival phagocytes, increasing expression of regulatory genes in TLF⁺ cells regulated in part by RXRα, and inflammatory genes in CCR2⁺ cells. Regulatory MΦs depletion worsens DS induced inflammation and goblet cell loss.

01 Oct 2024·Cell Reports

Visualizing the spatial organization of monocytes, interstitial macrophages, and tissue-specific macrophages in situ

Article

Author: Barthélémy, Sandrine ; Combadière, Christophe ; Petit, Maxime ; Boissonnas, Alexandre ; Hume, David A ; Firpion, Marina ; Guillou, Noëlline ; Bonduelle, Olivia ; Lanthiez, François ; Hume, David A. ; Weber-Delacroix, Eléonore

Tissue-resident mononuclear phagocytes (MPs) are an abundant cell population whose localization in situ reflects their identity. To enable assessment of their heterogeneity, we developed the red/green/blue (RGB)-Mac mouse based upon combinations of Cx3cr1 and Csf1r reporter transgenes, providing a complete visualization of their spatial organization in situ. 3D-multi-photon imaging for spatial mapping and spectral cytometry employing the three markers in combination distinguished tissue-associated monocytes, tissue-specific macrophages, and three subsets of connective-tissue-associated MPs, including CCR2⁺ monocyte-derived cell, CX3CR1⁺, and FOLR2⁺ interstitial subsets, associated with distinct sub-anatomic territories. These populations were selectively reduced by blockade of CSF1, CSF2, CCR2, and CX3CR1 and efficiently reconstitute their spatial distribution after transient myelo-ablation, suggesting an autonomous regulatory environment. Our findings emphasize the organization of the MP compartment at the sub-anatomic level under steady-state conditions, thereby providing a holistic understanding of their relative heterogeneity across different tissues.

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FOLR2

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