A new potent and selective CDK9 inhibitor induces the expression of the proto-oncogene MYC via a mechanism that depends on the bromodomain protein BRD4.
Pyridine-based allosteric inhibitors selectively target HIV-1 integrase tetramers and exhibit enhanced antiviral activity against a dolutegravir resistant mutant virus indicating potential clinical benefits for combining these two classes of inhibitors.
Targeting the CRL5 ubiquitin ligase complex in combination with CDK9 or MCL1 inhibition could combat innate and acquired resistance of cancer cells to MCL1-targeting therapeutics.
Delayed inhibition precisely balances excitation from arbitrary combinations of CA3 neurons and controls the gain of CA1 output by reducing inhibitory delay with increasing excitation.
The high affinity α-synuclein-monomer binder AS69 converts into a strong sub-stoichiometric inhibitor of nucleation processes upon formation of the AS69-α-synuclein complex, achieving reduced aggregation in vitro and in vivo.
A large variety of spatial representations implied in rodent navigation could arise robustly and rapidly from inputs with a weak spatial structure, by an interaction of excitatory and inhibitory synaptic plasticity.
Action-selection under response-conflict is buttressed by an inhibitory control signal from the basal ganglia that non-selectively suppresses motor excitability.
High-resolution structures of HIV-1 RT in complex with two newly developed non-nucleoside inhibitors explain how they retain antiviral activities against drug-resistant RT mutants with considerably reduced susceptibility to rilpivirine.
