[HTML][HTML] Targeted protein degradation: A promise for undruggable proteins

KTG Samarasinghe, CM Crews - Cell chemical biology, 2021 - cell.com
Summary Protein homeostasis, or" proteostasis," is indispensable for a balanced, healthy
environment within the cell. However, when natural proteostasis mechanisms are …

[HTML][HTML] Functional roles of bromodomain proteins in cancer

SP Boyson, C Gao, K Quinn, J Boyd, H Paculova… - Cancers, 2021 - mdpi.com
Simple Summary This review provides an in depth analysis of the role of bromodomain-
containing proteins in cancer development. As readers of acetylated lysine on nucleosomal …

[HTML][HTML] PROTACs: the future of leukemia therapeutics

Z Anwar, MS Ali, A Galvano, A Perez… - Frontiers in Cell and …, 2022 - frontiersin.org
The fight to find effective, long-lasting treatments for cancer has led many researchers to
consider protein degrading entities. Recent developments in PROteolysis TArgeting …

Process Development for the Synthesis of BI 1702135: A Concise Design Enabled by Selective Acylation of a 2-Aminobenzimidazole Intermediate

JP Wu, WT Dong, C Chen, A Sienkiewicz… - … Process Research & …, 2023 - ACS Publications
The route design and process development for the synthesis of BI 1702135 are described.
The synthetic design centers around an amide synthesis involving a 2-amino benzimidazole …

[HTML][HTML] PROTACs in epigenetic cancer therapy: current status and future opportunities

X Liu, A Wang, Y Shi, M Dai, M Liu, HB Cai - Molecules, 2023 - mdpi.com
The epigenetic regulation of gene functions has been proven to be strongly associated with
the development and progression of cancer. Reprogramming the cancer epigenome …

[HTML][HTML] Capsule-based automated synthesis for the efficient assembly of PROTAC like molecules

S Bordi, T Jiang, A Konopka, G Coin, PL Nichols… - Digital …, 2023 - pubs.rsc.org
In recent years, the therapeutically beneficial degradation of proteins using PROteolysis
Targeting Chimeras (PROTACs) has become an increasingly popular approach in drug …

[HTML][HTML] COVID-19 Therapies: Protease Inhibitions and Novel Degrader Strategies

M Reboud-Ravaux, C El Amri - Frontiers in Drug Discovery, 2022 - frontiersin.org
The global spread of severe acute respiratory syndrome corona virus-2 (SARS-CoV-2)
variants is alarming. In addition to vaccines, effective antiviral agents are urgently needed to …

Dégradation induite des protéines par des molécules PROTAC et stratégies apparentées: développements à visée thérapeutique

M Reboud-Ravaux - Biologie Aujourd'hui, 2021 - biologie-journal.org
Alors que, pour la plupart, les médicaments actuels sont de petites molécules inhibant
l'action d'une protéine en bloquant un site d'interaction, la dégradation ciblée des protéines …

[PDF][PDF] 蛋白降解靶向嵌合体(PROTAC) 药物的非临床评价策略分析

韩俊源, 李亚娟, 王海学… - 中国药理学与毒理学杂志, 2021 - cjpt.magtechjournal.com
蛋白降解靶向嵌合体(PROTAC) 将靶向蛋白募集到E3 泛素连接酶进行泛素化标记,
然后通过泛素-蛋白酶体途径将其降解, 从而将过表达和突变的致病蛋白清除 …

Determination of accelerated ageing in critical illness

JA Sullivan - 2023 - etheses.bham.ac.uk
Aims: The primary aim of this research was to test the hypothesis that injury or critical illness
is sufficient to cause an acceleration of the ageing process. This hypothesis is to be tested …