PROTACs of cyclin-dependent kinases DOI

Denisa Veselá,

Eva Řezníčková, Václav Mik

et al.

Annual reports in medicinal chemistry, Journal Year: 2024, Volume and Issue: unknown

Published: Jan. 1, 2024

Language: Английский

Advances in designing ternary complexes: Integrating in-silico and biochemical methods for PROTAC optimisation in target protein degradation DOI Creative Commons
Shareef Shaik,

Prasanna Kumar Reddy Gayam,

Manish Chaudhary

et al.

Bioorganic Chemistry, Journal Year: 2024, Volume and Issue: 153, P. 107868 - 107868

Published: Oct. 4, 2024

Language: Английский

Citations

5
EXPLORING AZETIDINE CONTAINING HETEROCYCLES: FROM GREEN SYNTHESIS TO APPLICATIONS DOI
Shivangi Jaiswal,

Nikhilesh Arya,

Dharma Kishore

et al.

Tetrahedron, Journal Year: 2025, Volume and Issue: unknown, P. 134491 - 134491

Published: Jan. 1, 2025

Language: Английский

Citations

0
MALT1 Inhibitors and Degraders: Strategies for NF-κB-Driven Malignancies DOI
Ruyue Zhang,

Zixuan Wang,

Mengyuan Zhang

et al.

Journal of Medicinal Chemistry, Journal Year: 2025, Volume and Issue: unknown

Published: Feb. 25, 2025

Mucosa-associated lymphoid tissue protein 1 (MALT1), a cysteine protease and the sole paracaspase in humans, plays pivotal role survival proliferation of NF-κB-dependent malignant cancers, particularly MALT lymphoma diffuse large B-cell (DLBCL). Dysregulated MALT1 activity is implicated various malignancies, highlighting its importance as therapeutic target. This Perspective provides an overview MALT1's structural functional characteristics, summarizes recent advancements small-molecule inhibitors degraders targeting this protein, discusses compound structures, structure–activity relationship (SAR) analyses, biological activities. We aim to inform future research efforts enhance activity, selectivity, pharmacological properties MALT1-targeting compounds, establishing foundational framework for drug development critical area cancer therapy.

Language: Английский

Citations

0
A Comprehensive Primer and Review of PROTACs and Their In Silico Design DOI Creative Commons

Jacopo Zattoni,

Paola Vottero,

Gea Carena

et al.

Computer Methods and Programs in Biomedicine, Journal Year: 2025, Volume and Issue: 264, P. 108687 - 108687

Published: Feb. 27, 2025

Language: Английский

Citations

0
Production of polysubstituted pyrroles from lignin β-O-4 models via a one-pot multicomponent reaction DOI
Qiang Qian, Yangming Ding, Qi Luo

et al.

International Journal of Biological Macromolecules, Journal Year: 2025, Volume and Issue: unknown, P. 142283 - 142283

Published: March 1, 2025

Language: Английский

Citations

0
Pt(IV)-PROTAC Complexes with Synergistic Antitumor Activity and Enhanced Membrane Permeability DOI
Chang‐Jiu Li,

Z. Q. Zou,

Shan Xu

et al.

Journal of Medicinal Chemistry, Journal Year: 2025, Volume and Issue: unknown

Published: April 4, 2025

A class of Pt(IV)-PROTAC complexes was designed and synthesized with dual aims inducing DNA strand damage inhibiting repair. These showed good antiproliferative activity against a range cancer cell lines. Enhanced intracellular uptake platinum PROTAC observed. Multiple mechanisms action were identified, including the induction damage, disruption repair, activation mitochondrial-dependent apoptosis. One Pt(IV)-PROTACs, CW-2, excellent antitumor in xenograft mouse model. results suggest that represents promising strategy for development novel therapeutics.

Language: Английский

Citations

0
Recent advances in degraders engaging lysosomal pathways and related nanomedicine DOI

Runxin Lu,

Xiaofeng Ni, Sha Diao

et al.

European Journal of Medicinal Chemistry, Journal Year: 2025, Volume and Issue: 292, P. 117701 - 117701

Published: April 28, 2025

Language: Английский

Citations

0
Recent advances in dual PROTACs degrader strategies for disease treatment DOI
Jianyu Liu, Yanzhuo Liu,

Jiao Tang

et al.

European Journal of Medicinal Chemistry, Journal Year: 2024, Volume and Issue: 279, P. 116901 - 116901

Published: Sept. 27, 2024

Language: Английский

Citations

2
Assembly line library synthesis in flow: A multistep and multivectorial approach DOI Creative Commons
Brenda Pijper, Irini Abdiaj,

Javier Mazuela

et al.

Published: June 11, 2024

In drug discovery, traditional automated library synthesis has typically involved single-step synthetic procedures targeting a single vector of interest. However, achieving greater structural diversity requires exploring multistep and multivectorial approaches. These methodologies enable the preparation compounds with varying structures in experiment. Here, we present novel method for continuous flow. This approach offers unique opportunities, such as linkers between two defined vectors or rapidly mapping synergistic structure-activity relationship (SAR) by concurrently multiple vectors. Our incorporates up to eight different methodologies, including established chemistries, metal-catalysed transformations, modern metallaphotoredox couplings. broad range ensures high level generated, providing powerful tool accelerate exploration chemical space discovery programs.

Language: Английский

Citations

1
Multistep and multivectorial assembly line library synthesis in flow DOI Creative Commons
Brenda Pijper, Irini Abdiaj,

Javier Mazuela

et al.

Chem Catalysis, Journal Year: 2024, Volume and Issue: unknown, P. 101118 - 101118

Published: Sept. 1, 2024

Language: Английский

Citations

1