While some RXR agonists cross-signaled the retinoic acid receptor (RAR), interestingly, many of the new analogs presented in this paper showed reduced activity against RAR. The analogs were tested for their ability to activate liver-X receptor (LXR) and increase the level of triglycerides, as well as LXRE-mediated transcription of brain ApoE expression as a marker of neurodegenerative disorders. Analogs were modeled for RXR binding affinity, and EC 50 and IC 50 values were determined for a leukemia cell line. The ability of the new analogs to agonize RXR compared to bexarotene was evaluated. The bexarotene alicyclic ring, aliphatic linker, and benzoic acid moiety were substituted with an isochroman ring and nitrogen heterocycles, respectively. synthesized analogs of this drug, aiming to retain its key function and avoid harmful side effects.

The main subjects of the communications were manifold: markers in neurodegenerative disorders, mediators of inflammation, non-coding micro-RNAs, enzymes regulating cell division, measures to mitigate post-operative side effects of cancer treatment, genetic disorders such as cystic fibrosis, skin disorders, multifunctional biomaterials, plant-derived topical preparations, crystal forms of active pharmaceutical ingredients, innovative drug product formulations, quality control of drug substances and drug products, including the chemical stability of drug substances and impurity profile, drug membrane permeability and identification of drug candidates by virtual screening a compound library.īexarotene, a drug that is active against cutaneous T-cell lymphoma, interferes with retinoid X-receptor (RXR)-dependent pathways and might cause serious side effects such as hypothyroidism.

Most of the papers published in this Issue were presented, at least in part, at this Conference, as invited lectures, scientific communications, and posters. The interest was shared also by the participants of the Interdisciplinary Conference on Drug Sciences, ACCORD 2022, held at the Medical University of Warsaw. For this reason, anticancer therapy, specifically against leukemia and lymphoma, and solid tumors, including prostate, melanoma, ovarian, lung, urinary bladder, and breast cancers, remains a consistently leading area of interest for researchers worldwide. Despite several decades of intensive research and the development of several generations of increasingly selective and effective drugs, cancer is still the leading cause of death.

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