AIMC Topic: Piperazines

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Synergistic drug combinations and machine learning for drug repurposing in chordoma.

Scientific reports
Chordoma is a devastating rare cancer that affects one in a million people. With a mean-survival of just 6 years and no approved medicines, the primary treatments are surgery and radiation. In order to speed new medicines to chordoma patients, a drug...

Endocannabinoid degradation inhibitors ameliorate neuronal and synaptic alterations following traumatic brain injury.

Journal of neurophysiology
Our previous work showed that lateral fluid percussion injury to the sensorimotor cortex (SMC) of anesthetized rats increased neuronal synaptic hyperexcitability in layer 5 (L5) neurons in ex vivo brain slices 10 days postinjury. Furthermore, endocan...

Synthesis of Patient-Specific Transmission Data for PET Attenuation Correction for PET/MRI Neuroimaging Using a Convolutional Neural Network.

Journal of nuclear medicine : official publication, Society of Nuclear Medicine
Attenuation correction is a notable challenge associated with simultaneous PET/MRI, particularly in neuroimaging, where sharp boundaries between air and bone volumes exist. This challenge leads to concerns about the visual and, more specifically, qua...

Prediction of overall in vitro microsomal stability of drug candidates based on molecular modeling and support vector machines. Case study of novel arylpiperazines derivatives.

PloS one
Other than efficacy of interaction with the molecular target, metabolic stability is the primary factor responsible for the failure or success of a compound in the drug development pipeline. The ideal drug candidate should be stable enough to reach i...

Drug-Drug interactions and special considerations in breast cancer patients treated with CDK4/6 inhibitors: A comprehensive review.

Cancer treatment reviews
Cyclin-dependent kinase 4/6 inhibitors (CDK4/6i) have reshaped the treatment paradigm of hormone receptor positive (HR + )/HER2-negative breast cancer in both adjuvant and metastatic settings. However, their metabolism via the cytochrome P450 (CYP3A4...

A Deep Learning-Enabled Workflow to Estimate Real-World Progression-Free Survival in Patients With Metastatic Breast Cancer: Study Using Deidentified Electronic Health Records.

JMIR cancer
BACKGROUND: Progression-free survival (PFS) is a crucial endpoint in cancer drug research. Clinician-confirmed cancer progression, namely real-world PFS (rwPFS) in unstructured text (ie, clinical notes), serves as a reasonable surrogate for real-worl...

Predicting transcriptional changes induced by molecules with MiTCP.

Briefings in bioinformatics
Studying the changes in cellular transcriptional profiles induced by small molecules can significantly advance our understanding of cellular state alterations and response mechanisms under chemical perturbations, which plays a crucial role in drug di...

Efficacy and Tolerability of Tenofovir/Lamivudine/Dolutegravir among Antiretroviral Therapy Naive Human Immunodeficiency Virus Infected Patients of a Tertiary Care Center in Eastern India.

The Journal of the Association of Physicians of India
BACKGROUND: Although many drug regimens have been used in the treatment of human immunodeficiency virus (HIV) infection, the National AIDS Control Organization (NACO) of India recommends the use of a fixed-dose combination of tenofovir/lamivudine/dol...

Principi di farmacodinamica e farmacocinetica nello switch tra antipsicotici: focus su cariprazina.

Rivista di psichiatria
Cariprazina {RGH-188; trans-N- [4- [2- [4- (2,3-diclorofenil) piperazin-1-il] etil] cicloesil] -N_, N_-dimetilurea cloridrato} è un antipsicotico atipico di nuova generazione, con un originale profilo farmacodinamico e farmacocinetico. Cariprazina ha...