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 …

PROTAC'ing oncoproteins: targeted protein degradation for cancer therapy

JM Kelm, DS Pandey, E Malin, H Kansou, S Arora… - Molecular Cancer, 2023 - Springer
Molecularly targeted cancer therapies substantially improve patient outcomes, although the
durability of their effectiveness can be limited. Resistance to these therapies is often related …

PROTACs to address the challenges facing small molecule inhibitors

P Martín-Acosta, X Xiao - European journal of medicinal chemistry, 2021 - Elsevier
Small molecule inhibitors of proteins represent important medicines and critical chemical
tools to investigate the biology of the target proteins. Advances in various-omics …

Bruton's tyrosine kinase inhibitors (Btkis): review of Preclinical studies and evaluation of clinical trials

D Rozkiewicz, JM Hermanowicz, I Kwiatkowska… - Molecules, 2023 - mdpi.com
In the last few decades, there has been a growing interest in Bruton's tyrosine kinase (BTK)
and the compounds that target it. BTK is a downstream mediator of the B-cell receptor (BCR) …

Orally bioavailable BTK PROTAC active against wild-type and C481 mutant BTKs in human lymphoma CDX mouse models

YS Lim, SM Yoo, V Patil, HW Kim, HH Kim… - Blood …, 2023 - ashpublications.org
Bruton tyrosine kinase (BTK) is an important signaling hub that activates the B-cell receptor
(BCR) signaling cascade. BCR activation can contribute to the growth and survival of B-cell …

[HTML][HTML] Pleckstrin Homology [PH] domain, structure, mechanism, and contribution to human disease

G Powis, EJ Meuillet, M Indarte, G Booher… - Biomedicine & …, 2023 - Elsevier
The pleckstrin homology [PH] domain is a structural fold found in more than 250 proteins
making it the 11th most common domain in the human proteome. 25% of family members …

Protein assembly and crowding simulations

L Heo, Y Sugita, M Feig - Current opinion in structural biology, 2022 - Elsevier
Proteins encounter frequent molecular interactions in biological environments. Computer
simulations have become an increasingly important tool in providing mechanistic insights …

Specific interactions of peripheral membrane proteins with lipids: what can molecular simulations show us?

AH Larsen, LH John, MSP Sansom… - Bioscience …, 2022 - portlandpress.com
Peripheral membrane proteins (PMPs) can reversibly and specifically bind to biological
membranes to carry out functions such as cell signalling, enzymatic activity, or membrane …

Progress in the development of small molecular inhibitors of the Bruton's tyrosine kinase (BTK) as a promising cancer therapy

XJ Liu, XJ Pang, XY Yuan, GX Yu, YR Li… - Bioorganic & medicinal …, 2021 - Elsevier
Bruton tyrosine kinase (BTK) is a key kinase in the B cell antigen receptor signal
transduction pathway, which is involved in the regulation of the proliferation, differentiation …

The energetics of protein–lipid interactions as viewed by molecular simulations

RA Corey, PJ Stansfeld… - Biochemical Society …, 2020 - portlandpress.com
Membranes are formed from a bilayer containing diverse lipid species with which membrane
proteins interact. Integral, membrane proteins are embedded in this bilayer, where they …