Proteasome inhibitor drugs

LD Fricker - Annual review of pharmacology and toxicology, 2020 - annualreviews.org
Proteasomes are large, multicatalytic protein complexes that cleave cellular proteins into
peptides. There are many distinct forms of proteasomes that differ in catalytically active …

Protein kinase C (PKC) isoforms in cancer, tumor promotion and tumor suppression

N Isakov - Seminars in cancer biology, 2018 - Elsevier
The AGC family of serine/threonine kinases (PKA, PKG, PKC) includes more than 60
members that are critical regulators of numerous cellular functions, including cell cycle and …

Protein kinase C, an elusive therapeutic target?

D Mochly-Rosen, K Das, KV Grimes - Nature reviews Drug discovery, 2012 - nature.com
Protein kinase C (PKC) has been a tantalizing target for drug discovery ever since it was first
identified as the receptor for the tumour promoter phorbol ester in 1982. Although initial …

Activation of protein kinase C isoforms and its impact on diabetic complications

P Geraldes, GL King - Circulation research, 2010 - ahajournals.org
Both cardio-and microvascular complications adversely affect the life quality of patients with
diabetes and have been the leading cause of mortality and morbidity in this population …

Protein kinase C: poised to signal

AC Newton - American Journal of Physiology …, 2010 - journals.physiology.org
Nestled at the tip of a branch of the kinome, protein kinase C (PKC) family members are
poised to transduce signals emanating from the cell surface. Cell membranes provide the …

Evolving mechanisms of vascular smooth muscle contraction highlight key targets in vascular disease

Z Liu, RA Khalil - Biochemical pharmacology, 2018 - Elsevier
Vascular smooth muscle (VSM) plays an important role in the regulation of vascular function.
Identifying the mechanisms of VSM contraction has been a major research goal in order to …

Storming the gate: New approaches for targeting the dynamic tight junction for improved drug delivery

I Ramirez-Velez, B Belardi - Advanced drug delivery reviews, 2023 - Elsevier
As biologics used in the clinic outpace the number of new small molecule drugs, an
important challenge for their efficacy and widespread use has emerged, namely tissue …

Peptides and peptidomimetics as regulators of protein–protein interactions

AD Cunningham, N Qvit, D Mochly-Rosen - Current opinion in structural …, 2017 - Elsevier
Highlights•Protein–protein interactions are essential for almost all cell processes.•Peptides
are ideal candidates for targeting protein–protein interactions (PPIs).•We survey screening …

Protein kinase C pharmacology: refining the toolbox

AX Wu-Zhang, AC Newton - Biochemical Journal, 2013 - portlandpress.com
PKC (protein kinase C) has been in the limelight since the discovery three decades ago that
it acts as a major receptor for the tumour-promoting phorbol esters. Phorbol esters, with their …

[HTML][HTML] An update on protein kinases as therapeutic targets—part I: protein kinase C activation and its role in cancer and cardiovascular diseases

S Silnitsky, SJS Rubin, M Zerihun, N Qvit - International journal of …, 2023 - mdpi.com
Protein kinases are one of the most significant drug targets in the human proteome,
historically harnessed for the treatment of cancer, cardiovascular disease, and a growing …