Browsing ICR Divisions by author "Chopra, Rajesh"
Now showing items 1-7 of 7
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A critical evaluation of the approaches to targeted protein degradation for drug discovery.
Chopra, R; Sadok, A; Collins, I (Elsevier BV, 2019-04-03)There is a great deal of excitement around the concept of targeting proteins for degradation as an alternative to conventional inhibitory small molecules and antibodies. Protein degradation can be undertaken by bifunctional ... -
A First-in-Human Study of Novel Cereblon Modulator Avadomide (CC-122) in Advanced Malignancies.
Rasco, DW; Papadopoulos, KP; Pourdehnad, M; Gandhi, AK; Hagner, PR; et al. (AMER ASSOC CANCER RESEARCH, 2019-01-01)PURPOSE: Avadomide is a novel, small-molecule therapeutic agent that modulates cereblon E3 ligase activity and exhibits potent antitumor and immunomodulatory activities. This first-in-human phase I study (NCT01421524) ... -
Apremilast is a selective PDE4 inhibitor with regulatory effects on innate immunity.
Schafer, PH; Parton, A; Capone, L; Cedzik, D; Brady, H; et al. (ELSEVIER SCIENCE INC, 2014-09-01)Apremilast, an oral small molecule inhibitor of phosphodiesterase 4 (PDE4), is in development for chronic inflammatory disorders, and has shown efficacy in psoriasis, psoriatic arthropathies, and Behçet's syndrome. In March ... -
Chemical approaches to targeted protein degradation through modulation of the ubiquitin-proteasome pathway.
Collins, I; Wang, H; Caldwell, JJ; Chopra, R (PORTLAND PRESS LTD, 2017-03-15)Manipulation of the ubiquitin-proteasome system to achieve targeted degradation of proteins within cells using chemical tools and drugs has the potential to transform pharmacological and therapeutic approaches in cancer ... -
Differential effects of lenalidomide during plasma cell differentiation.
Jourdan, M; Cren, M; Schafer, P; Robert, N; Duperray, C; et al. (IMPACT JOURNALS LLC, 2016-05-10)Thalidomide, lenalidomide and pomalidomide have greatly improved the outcome of patients with multiple myeloma. However, their effects on plasma cells, the healthy counterpart of myeloma cells, are unknown. Here, we ... -
Immunomodulatory agents lenalidomide and pomalidomide co-stimulate T cells by inducing degradation of T cell repressors Ikaros and Aiolos via modulation of the E3 ubiquitin ligase complex CRL4(CRBN.).
Gandhi, AK; Kang, J; Havens, CG; Conklin, T; Ning, Y; et al. (WILEY, 2014-03-01)Cereblon (CRBN), the molecular target of lenalidomide and pomalidomide, is a substrate receptor of the cullin ring E3 ubiquitin ligase complex, CRL4(CRBN) . T cell co-stimulation by lenalidomide or pomalidomide is cereblon ... -
JNK inhibition reduces lung remodeling and pulmonary fibrotic systemic markers.
van der Velden, JLJ; Ye, Y; Nolin, JD; Hoffman, SM; Chapman, DG; et al. (Wiley, 2016-12-01)BACKGROUND: Lung remodeling and pulmonary fibrosis are serious, life-threatening conditions resulting from diseases such as chronic severe asthma and idiopathic pulmonary fibrosis (IPF). Preclinical evidence suggests that ...