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Last update 08 May 2025

LEDGF

Last update 08 May 2025

Basic Info

Synonyms

CLL-associated antigen KW-7, Dense fine speckles 70 kDa protein, DFS 70

+ [10]

Introduction

Transcriptional coactivator involved in neuroepithelial stem cell differentiation and neurogenesis. Involved in particular in lens epithelial cell gene regulation and stress responses. May play an important role in lens epithelial to fiber cell terminal differentiation. May play a protective role during stress-induced apoptosis. Isoform 2 is a more general and stronger transcriptional coactivator. Isoform 2 may also act as an adapter to coordinate pre-mRNA splicing. Cellular cofactor for lentiviral integration.

Drugs associated with LEDGF

Pirmitegravir

Target

LEDGF

Mechanism

LEDGF inhibitors

Active Org.

ST Pharm Co., Ltd.

Originator Org.

ST Pharm Co., Ltd.

Active Indication

HIV Infections

Inactive Indication-

Drug Highest PhasePhase 2

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

US20240383971

Patent Mining

Target

LEDGF

Mechanism-

Active Org.

McMaster University

Originator Org.

McMaster University

Active Indication

Immune System Diseases [+3]

Inactive Indication-

Drug Highest PhaseDiscovery

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

OCU-100

Target

LEDGF

Mechanism

LEDGF stimulators

Active Org.-

Originator Org.

CU Anschutz Medical Campus

Active Indication-

Inactive Indication

Retinitis Pigmentosa

Drug Highest PhasePending

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

Clinical Trials associated with LEDGF

NCT05869643

/ RecruitingPhase 2

A Phase 2a, Randomized, Double-Blinded, Placebo-Controlled, Multicenter Study to Investigate the Antiviral Effect, Safety, Tolerability, and Pharmacokinetics of STP0404 in Adults with HIV-1 Infection

The purpose of this study is to evaluate the antiviral effect, safety, tolerability, and pharmacokinetics of STP0404 in adult participants living with Human Immunodeficiency Virus Type 1 (HIV-1) infection.

Start Date23 May 2023

Sponsor / Collaborator

ST Pharm Co., Ltd.

NCT03634085

/ CompletedPhase 1

A Single Ascending Dose Trial Investigating the Safety, Tolerability and Pharmacokinetics of Orally Administered BDM-2 in Healthy Male Subjects

This is a first-in-human (FIH), double-blind, placebo-controlled, randomized trial in healthy adult male subjects, to evaluate the safety, tolerability and pharmacokinetics (PK) of single ascending oral doses of BDM-2. The effect of food on the PK of a single dose of BDM-2 will also be evaluated.

Start Date17 May 2018

Sponsor / Collaborator

Hivih

[+1]

100 Clinical Results associated with LEDGF

100 Translational Medicine associated with LEDGF

0 Patents (Medical) associated with LEDGF

674

Literatures (Medical) associated with LEDGF

01 Mar 2025·EJIFCC

International Consensus on ANA Patterns (ICAP) Classification Tree Revisited: A Single Centre Report on Four Nuclear Patterns from a Tertiary Care Centre in India.

Article

Author: Kumar, Avinash ; Prakash, Jyoti ; Ranjan, Aanjik ; Patra, Pratap Kumar ; Kumar, Sushil ; Mahto, Mala ; Ahmad, Shamshad ; Pradhan, Swetalina

BackgroundICAP describes ANA patterns from AC- 0 to AC-29. They are further marked for competent or expertise reporting depending on ease of identification. There are some debatable patterns in ICAP which share similar features with a few others yet have a distinct identity and few others which are not addressed by ICAP but are described by BCA like Quasihomogenous. This study analysed four nuclear patterns with overlapping features, namely Homogenous, speckled, Dense Fine Speckled70(DFS70) and quasi-homogenous to identify challenges posed in their identification due to overlapping features.MethodsAll samples which were reported as positive for the above four nuclear patterns (n=388) by IIF using HEp-2 cell were included in the study. LIA was performed on 103 such samples to look for association between the ANA patterns and specific antibody detected by LIA.ResultsDFS70 pattern is a rare pattern and existed in combination with other autoantibodies thus making its identification difficult on IIF. Homogenous pattern corresponded to AC- 29 (anti-topoisomerase, anti-Scl 70) which was probably due to wrong identification. Mixed pattern i.e speckled and homogenous was associated with Sm and U1sn RNP antibodies.ConclusionsDFS 70 is a pattern with overlapping features of both homogenous and speckled and calls for expertise reporting. More awareness is required about AC 29 pattern as it is an overlap of five different components. Its identification poses significant challenges and is rightly placed in the expert reporting by ICAP. Mixed pattern (speckled and homogenous) referred to as Quasihomogenous by BCA needs to be addressed by ICAP.

12 Feb 2025·Current HIV Research

Integrated Computational Analysis of C-2 Substituted Pyrazolopyrimidine and Amide Isosteres ALLINI: 3D-QSAR, Molecular Docking, and ADMET Studies

Article

Author: Khedkar, Vijay M. ; Kunwar, Aakanksha ; Jha, Prakash C. ; N., Gondaliya Krishna

Introduction:The rapid increase in incidences of drug resistance and off-target toxicity in the case of Human Immunodeficiency Virus (HIV) has increased the demand for drugs with fewer side effects. HIV-1 Integrase (IN) is a promising target that helps integrate viral DNA with human DNA. It acts as a target for strand transfer inhibitors. However, the emergence of resistant mutations in the proteins necessitates the exploration of potent allosteric drugs. The allosteric integrase inhibitors (ALLINI) that interrupt the association of the integrase binding do-main of the lens epithelium growth factor (LEDGF/p75) and LEDGF/p75 binding site of the IN are more promising as they hinder site specificity and viral replication.Objective:In this study, a 3D-QSAR, molecular docking, and ADMET were carried out to investigate the binding of the C2-pyrazolopyrimidine amides and amide isosteres. Method: The 3D-QSAR model was developed using a series of 24 C-2 substituted pyrazolopyrimidine and amide isosteres. A statistically significant model was constructed, showing the determination coefficient (r2) and five-fold cross-validation (q2) at 0.946 and 0.506, respectively. Furthermore, the contour maps of the electrostatic potential and van der Waals coefficient provided structural modifications in the features to improve the inhibitory activity.Result:A molecular docking study was also performed to check the binding of the compounds to the LEDGF/p75 binding site of the IN, along with ADMET evaluation.Conclusion:The outcome of the study will help to prepare the potent molecules with enhanced allosteric inhibitory activity.

01 Feb 2025·Biochimica et Biophysica Acta (BBA) - Reviews on Cancer

Role of LEDGF/p75 (PSIP1) in oncogenesis. Insights in molecular mechanism and therapeutic potential

Review

Author: Van Belle, Siska ; Iervolino, Matteo ; Debyser, Zeger ; Akele, Muluembet ; Christ, Frauke

Aberrant gene expression due to dysfunction in proteins involved in transcriptional regulation is a hallmark of tumor development. Indeed, targeting transcriptional regulators represents an emerging approach in cancer therapeutics. Lens epithelium-derived growth factor (LEDGF/p75, PSIP1) is a co-transcriptional activator that tethers several proteins to the chromatin. LEDGF/p75 has been implicated in diseases such as HIV infection and KMT2A-rearranged leukemia. Notably, LEDGF/p75 is upregulated in various human cancers including prostate and breast cancer. In this review, we discuss the essential role of LEDGF/p75 in different malignancies and explore its mechanistic contribution to tumorigenesis revealing its potential as a therapeutic target for chemotherapy.

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