Allosteric modulation of class A GPCRs: targets, agents, and emerging concepts

EA Wold, J Chen, KA Cunningham… - Journal of medicinal …, 2018 - ACS Publications
G-protein-coupled receptors (GPCRs) have been tractable drug targets for decades with
over one-third of currently marketed drugs targeting GPCRs. Of these, the class A GPCR …

Salvage regimens using conventional chemotherapy agents for relapsed/refractory adult AML patients: a systematic literature review

JE Megías-Vericat, D Martínez-Cuadrón, MÁ Sanz… - Annals of …, 2018 - Springer
Prognosis in relapsed and refractory acute myeloid leukemia (R/R AML) patients is dismal,
with no satisfactory and standard salvage chemotherapy regimen. We performed a …

A novel cereblon modulator recruits GSPT1 to the CRL4CRBN ubiquitin ligase

ME Matyskiela, G Lu, T Ito, B Pagarigan, CC Lu… - Nature, 2016 - nature.com
Immunomodulatory drugs bind to cereblon (CRBN) to confer differentiated substrate
specificity on the CRL4CRBN E3 ubiquitin ligase. Here we report the identification of a new …

Ex vivo venetoclax sensitivity testing predicts treatment response in acute myeloid leukemia

H Kuusanmäki, S Kytölä, I Vänttinen… - …, 2022 - pmc.ncbi.nlm.nih.gov
The BCL-2 inhibitor venetoclax has revolutionized the treatment of acute myeloid leukemia
(AML) in patients not benefiting from intensive chemotherapy. Nevertheless, treatment …

The p97 inhibitor CB-5083 is a unique disrupter of protein homeostasis in models of multiple myeloma

R Le Moigne, BT Aftab, S Djakovic, E Dhimolea… - Molecular cancer …, 2017 - AACR
Inhibition of the AAA ATPase, p97, was recently shown to be a novel method for targeting
the ubiquitin proteasome system, and CB-5083, a first-in-class inhibitor of p97, has …

Improving NK cell function in multiple myeloma with NKTR-255, a novel polymer-conjugated human IL-15

RA Fernandez, JE Mayoral, L Pierre-Louis… - Blood …, 2023 - ashpublications.org
Multiple myeloma (MM) is characterized by an immunosuppressive microenvironment that
enables tumor development. One of the mechanisms of immune evasion used by MM cells …

Functional role and therapeutic targeting of p21-activated kinase 4 in multiple myeloma

M Fulciniti, J Martinez-Lopez… - Blood, The Journal …, 2017 - ashpublications.org
Dysregulated oncogenic serine/threonine kinases play a pathological role in diverse forms
of malignancies, including multiple myeloma (MM), and thus represent potential therapeutic …

Advancements in oncoproteomics technologies: Treading toward translation into clinical practice

A Punetha, D Kotiya - Proteomes, 2023 - mdpi.com
Proteomics continues to forge significant strides in the discovery of essential biological
processes, uncovering valuable information on the identity, global protein abundance …

Bringing model-based prediction to oncology clinical practice: a review of pharmacometrics principles and applications

N Buil-Bruna, JM López-Picazo, S Martín-Algarra… - The …, 2016 - academic.oup.com
Despite much investment and progress, oncology is still an area with significant unmet
medical needs, with new therapies and more effective use of current therapies needed. The …

Ex vivo assessment of drug activity in patient tumor cells as a basis for tailored cancer therapy

K Blom, P Nygren, J Alvarsson… - Journal of …, 2016 - journals.sagepub.com
Although medical cancer treatment has improved during the past decades, it is difficult to
choose between several first-line treatments supposed to be equally active in the diagnostic …